Target Information

Target General Infomation
Target ID
T77913
Former ID
TTDS00086
Target Name
Histamine H1 receptor
Gene Name
HRH1
Synonyms
H1 Histamine receptor; Histamine receptor 1; HRH1
Target Type
Successful
Disease Allergic conjunctivitis [ICD9: 204.0, 372.0, 372.14, 995.3; ICD10: C91.0, H10, H10.45, T78.4]
Allergic disorders; Itching; Nausea [ICD9: 698, 787, 787.0, 995.3; ICD10: L29, R11, T78.4]
Allergic rhinitis; Urticaria [ICD9: 477, 708; ICD10: J30, L50]
Allergy [ICD9: 995.3; ICD10: T78.4]
Asthma [ICD10: J45]
Anxiety disorder; Morning sickness [ICD9: 300, 643.0; ICD10: F40-F42, O21.0]
Allergic rhinitis; Urticaria; Pruritus [ICD9: 477, 708; ICD10: J30, L50]
Anesthesia [ICD9: 338; ICD10: R20.0]
Allergic skin disorders [ICD10: L00-L99]
Allergic rhinitis [ICD9: 472.0, 477, 995.3; ICD10: J00, J30, J31.0, T78.4]
Anxiety disorder [ICD9: 300, 311; ICD10: F32, F40-F42]
Common cold; Allergies [ICD9: 460, 995.3; ICD10: J00, T78.4]
Depression [ICD9: 311; ICD10: F30-F39]
Dry cough [ICD10: R05]
Hypersensitivity reactions; Coughs; Common colds [ICD10: R05]
Hay fever [ICD9: 477; ICD10: J30]
Hay fever; Allergic rhinitis [ICD9:477, 472.0, 995.3; ICD10: J30, J00, J31.0, T78.4]
Hay fever; Cough [ICD9:477, 786.2; ICD10: J30, R05]
Insomnia; Anxiety disorder [ICD9:307.41, 307.42, 327.0, 780.51, 780.52, 300, 311; ICD10: F51.0, G47.0, F32, F40-F42]
Insomnia [ICD9: 307.41, 307.42, 327.0, 780.51, 780.52; ICD10: F51.0, G47.0]
Nausea; Vomiting [ICD9: 787, 787.0; ICD10: R11]
Nasal congestion [ICD9: 478.19; ICD10: J34.89]
Obesity [ICD9: 278; ICD10: E66]
Ocular allergy [ICD9: 360-379; ICD10: H00-H59]
Parkinson's disease [ICD9: 332; ICD10: G20]
Perennial and seasonal allergic rhinitis; Vasomotor rhinitis; Allergic conjunctivitis [ICD10: H10]
Pruritus [ICD9: 698; ICD10: L29]
Pain [ICD9: 338, 356.0, 356.8,780; ICD10: G64, G90.0, R52, G89]
Rhinitis; Urticaria; Allergy [ICD10: J00, J30, J31.0, L50, T78.4]
Respiratory allergies; Allergic rhinitis [ICD9:460-519, 472.0, 477, 995.3; ICD10: J00-J99, J00, J30, J31.0, T78.4]
Respiratory allergies; Cancer [ICD9:460-519, 140-229; ICD10: J00-J99, C00-C96]
Rhinitis [ICD9: 472.0, 477; ICD10: J00, J30, J31.0]
Respiratory disease [ICD10: J00-J99]
Seasonal and perennial allergic rhinitis and vasomotor rhinitis [ICD10: J30]
Sleep disorders [ICD9: 307.4, 327, 780.5; ICD10: F51, G47]
Vertigo's disease; Meniere's disease [ICD10: H81.09]
Vertigo meniere's disease [ICD9: 386.0, 438.85, 780.4; ICD10: H81, H81.0, R42]
Unspecified [ICD code not available]
Function
In peripheral tissues, the H1 subclass of histamine receptors mediates the contraction of smooth muscles, increase in capillary permeability due to contraction of terminal venules, and catecholamine release from adrenal medulla, as well as mediating neurotransmission in the central nervous system.
BioChemical Class
GPCR rhodopsin
Target Validation
T77913
UniProt ID
P35367
Sequence
MSLPNSSCLLEDKMCEGNKTTMASPQLMPLVVVLSTICLVTVGLNLLVLYAVRSERKLHT
VGNLYIVSLSVADLIVGAVVMPMNILYLLMSKWSLGRPLCLFWLSMDYVASTASIFSVFI
LCIDRYRSVQQPLRYLKYRTKTRASATILGAWFLSFLWVIPILGWNHFMQQTSVRREDKC
ETDFYDVTWFKVMTAIINFYLPTLLMLWFYAKIYKAVRQHCQHRELINRSLPSFSEIKLR
PENPKGDAKKPGKESPWEVLKRKPKDAGGGSVLKSPSQTPKEMKSPVVFSQEDDREVDKL
YCFPLDIVHMQAAAEGSSRDYVAVNRSHGQLKTDEQGLNTHGASEISEDQMLGDSQSFSR
TDSDTTTETAPGKGKLRSGSNTGLDYIKFTWKRLRSHSRQYVSGLHMNRERKAAKQLGFI
MAAFILCWIPYFIFFMVIAFCKNCCNEHLHMFTIWLGYINSTLNPLIYPLCNENFKKTFK
RILHIRS
Drugs and Mode of Action
Drug(s) (S)-(+)-Dimethindene maleate Drug Info Approved Pruritus [535933]
Aceprometazine Drug Info Approved Sleep disorders [550730]
Acrivastine Drug Info Approved Allergic rhinitis [534869]
Alcaftadine Drug Info Approved Allergic conjunctivitis [531351], [542577]
Antazoline Drug Info Approved Nasal congestion [538515], [542123]
Azatadine Drug Info Approved Allergic rhinitis [538492], [542126]
Azelastine Drug Info Approved Allergic conjunctivitis [536119], [542129]
Bepotastine Drug Info Approved Allergic rhinitis; Urticaria; Pruritus [536119], [542491]
Bromodiphenhydramine Drug Info Approved Hay fever; Cough [538416], [542139], [551871]
Brompheniramine Drug Info Approved Allergic rhinitis [538351], [542140]
Buclizine Drug Info Approved Nausea; Vomiting [542141], [550717]
Carbinoxamine Drug Info Approved Seasonal and perennial allergic rhinitis and vasomotor rhinitis [551871]
Cetirizine Drug Info Approved Allergic rhinitis [534869], [538734]
Chlophedianol Drug Info Approved Dry cough [551871]
Chlorpheniramine Drug Info Approved Allergic rhinitis; Urticaria [538228], [542007]
Cinnarizine Drug Info Approved Vertigo meniere's disease [550678]
Clemastine Drug Info Approved Allergic rhinitis [538250], [541312]
Cyclizine Drug Info Approved Nausea; Vomiting [538421], [542159]
Cyproheptadine Drug Info Approved Perennial and seasonal allergic rhinitis; Vasomotor rhinitis; Allergic conjunctivitis [551871]
Desloratadine Drug Info Approved Allergic rhinitis [536542], [542165]
Dexbrompheniramine Drug Info Approved Hay fever; Allergic rhinitis [538375], [542578], [551871]
Dexchlorpheniramine Maleate Drug Info Approved Rhinitis; Urticaria; Allergy [551871]
Dimenhydrinate Drug Info Approved Nausea; Vomiting [538185]
Dimethindene Drug Info Approved Respiratory allergies; Allergic rhinitis [535933], [551871]
Diphenhydramine Drug Info Approved Vertigo's disease; Meniere's disease [551871]
Diphenylpyraline Drug Info Approved Allergic rhinitis [542174], [550716]
Doxepin Drug Info Approved Depression [536306], [538737]
Doxylamine Drug Info Approved Anxiety disorder; Morning sickness [538170], [542181]
Emedastine Drug Info Approved Allergic conjunctivitis [536119], [542184]
Epinastine Drug Info Approved Allergic conjunctivitis [536119], [542186]
Ergotidine Drug Info Approved Respiratory allergies; Cancer [535111], [538761], [551871]
Ethopropazine Drug Info Approved Parkinson's disease [536923], [542192]
Fexofenadine Drug Info Approved Allergic rhinitis [468050], [534869]
Hydroxyzine Drug Info Approved Anxiety disorder [538358], [542211]
Ketotifen Drug Info Approved Allergic conjunctivitis [536119], [542220]
Levocabastine Drug Info Approved Allergic conjunctivitis [536119], [538963]
Levocetirizine dihydrochloride Drug Info Approved Allergic rhinitis [538587], [538725]
Loratadine Drug Info Approved Allergy [536542], [542231]
Mepyramine Drug Info Approved Allergy [537515], [538732]
Mepyramine maleate Drug Info Approved Allergy [537515]
Mequitazine Drug Info Approved Allergic rhinitis [550725]
Methdilazine Drug Info Approved Allergic rhinitis [542247], [550689]
Mizolastine Drug Info Approved Allergic rhinitis [535216]
Olopatadine Drug Info Approved Allergic conjunctivitis [536119], [542266]
Oxatomide Drug Info Approved Hay fever [536700]
Pemirolast Drug Info Approved Allergic conjunctivitis [536119], [542352], [551871]
Phenindamine Drug Info Approved Common cold; Allergies [550767]
Pheniramine Drug Info Approved Hay fever [536119], [542286]
Promethazine Drug Info Approved Allergic disorders; Itching; Nausea [538374], [542302]
Propiomazine Drug Info Approved Insomnia; Anxiety disorder [538458], [542304], [551871]
Pyrilamine Maleate Drug Info Approved Headache [536700], [537884]
Tranilast Drug Info Approved Ocular allergy [536119], [541472]
Trimeprazine Drug Info Approved Allergic rhinitis [542253], [550775]
Tripelennamine Drug Info Approved Hypersensitivity reactions; Coughs; Common colds [551871]
Triprolidine Drug Info Approved Hay fever [536361], [538740]
RUPATADINE Drug Info Phase 4 Discovery agent [521763]
AC-170 Drug Info Phase 3 Allergic conjunctivitis [524743]
Carebastine Drug Info Phase 3 Ocular allergy [536119]
Olopatadine Drug Info Phase 3 Ocular allergy [536119], [542266]
E-4716 Drug Info Phase 2 Respiratory disease [527345]
LY-2624803 Drug Info Phase 2 Insomnia [522475]
Noberastine Drug Info Phase 2 Asthma [544807]
OBE-101 Drug Info Phase 2 Obesity [521932]
UCB-35440 Drug Info Phase 2 Rhinitis [549930]
Vapitadine Drug Info Phase 2 Allergic skin disorders [547977]
Astemizole Drug Info Withdrawn from market Allergic rhinitis [534869], [539680]
Chlophedianol Drug Info Withdrawn from market Anesthesia [542347], [550773]
Terfenadine Drug Info Withdrawn from market Allergy [534869], [539685]
Norastemizole Drug Info Discontinued in Preregistration Discovery agent [546280]
GSK835726 Drug Info Discontinued in Phase 2 Allergic rhinitis [548731]
HSR-609 Drug Info Discontinued in Phase 2 Rhinitis [545924]
Loratadine Drug Info Discontinued in Phase 2 Allergic rhinitis [547333]
Mequitamium iodide Drug Info Discontinued in Phase 2 Asthma [544538]
ReN-1869 Drug Info Discontinued in Phase 2 Pain [547211]
SUN-1334H Drug Info Discontinued in Phase 2 Allergic rhinitis [548589]
AZD-1744 Drug Info Discontinued in Phase 1 Asthma [548471]
GSK1004723 Drug Info Discontinued in Phase 1 Allergic rhinitis [548732]
KA-398 Drug Info Terminated Asthma [546278]
Selenotifen Drug Info Terminated Asthma [544859]
SUN-1334H Drug Info Investigative Unspecified [529341]
Antagonist (+)-cis-H2-PAT Drug Info [526358]
(+)-trans-H2-PAT Drug Info [526358]
(+/-)-cis-H2-PAT Drug Info [526358]
(+/-)-trans-H2-PAT Drug Info [526358]
(-)-trans-H2-PAT Drug Info [526358]
(S)-(+)-Dimethindene maleate Drug Info [535859], [535933], [537168], [537884]
(S)-cetirizine Drug Info [527113]
9-OH-risperidone Drug Info [534281]
AC-170 Drug Info [551442]
Aceprometazine Drug Info [536284]
Acrivastine Drug Info [534875], [537691]
Alcaftadine Drug Info [531351]
Antazoline Drug Info [534867], [535973], [537070], [537691]
arpromidine Drug Info [526569]
Astemizole Drug Info [537070], [537328]
Azatadine Drug Info [537651]
Azelastine Drug Info [536700], [537714]
Bepotastine Drug Info [536767]
Bromodiphenhydramine Drug Info [537648]
Brompheniramine Drug Info [537912]
BU-E 47 Drug Info [526569]
Buclizine Drug Info [535805]
Carbinoxamine Drug Info [537829]
Carebastine Drug Info [536119]
Cetirizine Drug Info [535660], [537488]
Chlophedianol Drug Info [537715]
Chlorpheniramine Drug Info [534934], [536700], [537884]
Cinnarizine Drug Info [534845], [535477]
Clemastine Drug Info [536618], [536744]
Cyclizine Drug Info [535368], [535716], [537890]
Cyproheptadine Drug Info [536089], [536720]
Desloratadine Drug Info [537072], [537098]
Dexbrompheniramine Drug Info [538137]
Dimenhydrinate Drug Info [535364], [536878]
Dimethindene Drug Info [535859], [535933], [537168], [537884]
Diphenhydramine Drug Info [534958], [536700]
Diphenylpyraline Drug Info [537891]
Doxylamine Drug Info [536000], [536430]
Emedastine Drug Info [537537]
Epinastine Drug Info [537248]
Fexofenadine Drug Info [535660], [537072]
GSK1004723 Drug Info [550963]
GSK835726 Drug Info [550963]
HSR-609 Drug Info [534391], [551871]
Hydroxyclemastine Drug Info [536618], [536744]
Hydroxyzine Drug Info [536846], [536963]
impromidine Drug Info [527955]
Ketotifen Drug Info [535339], [536700]
Levocabastine Drug Info [535848], [536800]
Levocetirizine dihydrochloride Drug Info [535339], [536700], [537072]
Loratadine Drug Info [537347], [538066], [538157]
Mepyramine Drug Info [537488], [537502], [537515]
Mepyramine maleate Drug Info [537488], [537502], [537515]
Mequitazine Drug Info [536811]
Methdilazine Drug Info [537703]
Mizolastine Drug Info [536717]
Noberastine Drug Info [528242]
Olopatadine Drug Info [536119]
Oxatomide Drug Info [535848], [536700]
Pemirolast Drug Info [536707]
Phenindamine Drug Info [537846]
Pheniramine Drug Info [535251]
Promethazine Drug Info [536700], [537884]
Propiomazine Drug Info [536316]
Pyrilamine Maleate Drug Info [536700], [537884]
ReN-1869 Drug Info [526246]
SUN-1334H Drug Info [529341]
Terfenadine Drug Info [536727], [538157]
Tranilast Drug Info [536119]
Trimeprazine Drug Info [536153]
Tripelennamine Drug Info [535112], [535869], [536003], [536086]
Triprolidine Drug Info [536896]
Vapitadine Drug Info [547978]
[11C]doxepin Drug Info [527045]
[11C]pyrilamine Drug Info [543664]
Inhibitor 1-(4-p-Tolyl-butyl)-piperidine Drug Info [530299]
1-[(Furan-2(5H)-one)-4-methyl]-desloratadine Drug Info [530666]
2-(9,10-dihydroanthracen-9-yl)-N-methylethanamine Drug Info [530331]
3,3-diphenylpropan-1-amine Drug Info [530331]
4,4-Diphenylbutan-1-amine Drug Info [530331]
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one Drug Info [531079]
9-(2-aminoethyl)-9,10-dihydroanthracene Drug Info [530331]
9-(2-aminopropyl)-9,10-dihydroanthracene Drug Info [530331]
9-(Aminomethyl)-9,10-dihydroanthracene Drug Info [530331]
9-Phenyl-2,3-dihydro-1H-indeno[2,1-c]pyridine Drug Info [525803]
DIMEBOLIN Drug Info [530547]
Diphenyl(piperidin-4-yl)methanol Drug Info [530299]
Doxepin Drug Info [536469]
KF-A6 Drug Info [529032]
MDL-28163 Drug Info [527799]
N,N-dimethyl-2,2-diphenylethanamine Drug Info [530331]
N,N-Dimethyl-3,3-diphenylpropan-1-amine Drug Info [530331]
N,N-dimethyl-4,4-diphenylbutan-1-amine Drug Info [530331]
N-hydroxycarbamate derivative Drug Info [527411]
N-methyl-3,3-diphenylpropan-1-amine Drug Info [530331]
N-methyl-4,4-diphenylbutan-1-amine Drug Info [530331]
OCTOCLOTHEPIN Drug Info [531171]
R-226161 Drug Info [528772]
R-dimethindene Drug Info [530300]
RUPATADINE Drug Info [527799]
VUF-10148 Drug Info [529387]
Agonist 2-(2-thiazolyl)ethanamine Drug Info [526569]
2-(3-bromophenyl)histamine Drug Info [526569]
2-(3-chlorophenyl)histamine Drug Info [526569]
2-(3-iodophenyl)histamine Drug Info [526569]
2-pyridylethylamine Drug Info [527113]
8R-Lisuride Drug Info [535914]
dimethylhistaprodifen Drug Info [526569]
Ergotidine Drug Info [535111]
histaprodifen Drug Info [527589]
methylhistaprodifen Drug Info [526569]
oxo-arpromidine Drug Info [527955]
S-(-)-Lisuride Drug Info [535914]
UR-PG131A Drug Info [527955]
UR-PG146 Drug Info [527955]
UR-PG153 Drug Info [527955]
UR-PG55B Drug Info [527955]
Modulator AZD-1744 Drug Info [1572591]
Dexchlorpheniramine Maleate Drug Info [556264]
E-4716 Drug Info [527345]
Ethopropazine Drug Info [556264]
KA-398 Drug Info [543664]
LY-2624803 Drug Info [533039]
Mequitamium iodide Drug Info [531768]
Norastemizole Drug Info
OBE-101 Drug Info [544069]
Selenotifen Drug Info [527929]
UCB-35440 Drug Info [527359]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway Calcium signaling pathway
Neuroactive ligand-receptor interaction
Inflammatory mediator regulation of TRP channels
PANTHER Pathway Histamine H1 receptor mediated signaling pathway
Reactome Histamine receptors
G alpha (q) signalling events
WikiPathways Monoamine GPCRs
GPCRs, Class A Rhodopsin-like
IL-4 Signaling Pathway
Gastrin-CREB signalling pathway via PKC and MAPK
GPCR ligand binding
GPCR downstream signaling
References
Ref 468050(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 4819).
Ref 521763ClinicalTrials.gov (NCT00258141) Study With Rupatadine in Mosquito-Bite Allergic Adult Subjects. U.S. National Institutes of Health.
Ref 521932ClinicalTrials.gov (NCT00409305) The Effect of Betahistine on Body Weight in Obese Subjects. U.S. National Institutes of Health.
Ref 522475ClinicalTrials.gov (NCT00784875) An Efficacy Study of Compound LY2624803 in the Treatment of Patients With Chronic Insomnia. U.S. National Institutes of Health.
Ref 524743ClinicalTrials.gov (NCT02132169) A Multi-Center Study Evaluating the Safety of AC-170 0.24%. U.S. National Institutes of Health.
Ref 527345Population pharmacokinetics of epinastine, a histamine H1 receptor antagonist, in adults and children. Br J Clin Pharmacol. 2005 Jan;59(1):43-53.
Ref 529341Preclinical efficacy and safety pharmacology of SUN-1334H, a potent orally active antihistamine agent. Drugs R D. 2008;9(2):93-112.
Ref 531351Mullard A: 2010 FDA drug approvals. Nat Rev Drug Discov. 2011 Feb;10(2):82-5.
Ref 534869Comparative tolerability of second generation antihistamines. Drug Saf. 1999 May;20(5):385-401.
Ref 535111Cloning and pharmacological characterization of a fourth histamine receptor (H(4)) expressed in bone marrow. Mol Pharmacol. 2001 Mar;59(3):420-6.
Ref 535216Population pharmacokinetic analysis and optimization of the experimental design for mizolastine solution in children. J Pharmacokinet Pharmacodyn. 2001 Jun;28(3):299-319.
Ref 535933Prescription and safety of dimethindene maleate micropellet capsules in Hungary. Orv Hetil. 2004 Feb 15;145(7):327-9.
Ref 536119Emerging drugs for ocular allergy. Expert Opin Emerg Drugs. 2005 Aug;10(3):505-20.
Ref 536306Emerging treatments for depression. Expert Opin Pharmacother. 2006 Dec;7(17):2323-39.
Ref 536361Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77. Epub 2007 Feb 20.
Ref 536542Desloratadine treatment for intermittent and persistent allergic rhinitis: a review. Clin Ther. 2007 Sep;29(9):1795-802.
Ref 536700Intact cell binding for in vitro prediction of sedative and non-sedative histamine H1-receptor antagonists based on receptor internalization. J Pharmacol Sci. 2008 May;107(1):66-79. Epub 2008 Apr 29.
Ref 536923Drugs used to treat Parkinson's disease, present status and future directions. CNS Neurol Disord Drug Targets. 2008 Oct;7(4):321-42.
Ref 537515Antinociception induced by central administration of histamine in the formalin test in rats. Indian J Physiol Pharmacol. 2008 Jul-Sep;52(3):249-54.
Ref 537884Inhibition by histamine H1 receptor antagonists of endogenous glibenclamide-sensitive K+ channels in follicle-enclosed Xenopus oocytes. Eur J Pharmacol. 1994 Jan 1;266(1):99-102.
Ref 538170FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 040167.
Ref 538185FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 040519.
Ref 538228FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 070797.
Ref 538250FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 073283.
Ref 538351FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 083821.
Ref 538358FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 085551.
Ref 538374FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 089013.
Ref 538375FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 089116.
Ref 538416FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 009319.
Ref 538421FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 009495.
Ref 538458FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 012382.
Ref 538492FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 017601.
Ref 538515FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 018746.
Ref 538587FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 022064.
Ref 538725(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 1214).
Ref 538732(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 1220).
Ref 538734(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 1222).
Ref 538737(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 1225).
Ref 538740(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 1228).
Ref 538761(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 1247).
Ref 538963(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 1586).
Ref 539680(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 2603).
Ref 539685(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 2608).
Ref 541312(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6063).
Ref 541472(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6326).
Ref 542007(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6976).
Ref 542123(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7116).
Ref 542126(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7119).
Ref 542129(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7121).
Ref 542139(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7132).
Ref 542140(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7133).
Ref 542141(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7134).
Ref 542159(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7151).
Ref 542165(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7157).
Ref 542174(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7165).
Ref 542181(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7171).
Ref 542184(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7174).
Ref 542186(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7176).
Ref 542192(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7181).
Ref 542211(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7199).
Ref 542220(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7206).
Ref 542231(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7216).
Ref 542247(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7231).
Ref 542253(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7237).
Ref 542266(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7249).
Ref 542286(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7267).
Ref 542302(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7282).
Ref 542304(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7284).
Ref 542347(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7324).
Ref 542352(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7329).
Ref 542491(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7466).
Ref 542577(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7587).
Ref 542578(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7588).
Ref 544538Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000086)
Ref 544807Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001178)
Ref 544859Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001341)
Ref 545924Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005369)
Ref 546278Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007218)
Ref 546280Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007228)
Ref 547211Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800014046)
Ref 547333Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800015252)
Ref 547977Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800020866)
Ref 548471Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800025772)
Ref 548589Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800026836)
Ref 548731Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800028154)
Ref 548732Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800028155)
Ref 549930Clinical pipeline report, company report or official report of UCB.
Ref 550678Drug information of Cinnarizine, 2008. eduDrugs.
Ref 550689Drug information of Methdilazine, 2008. eduDrugs.
Ref 550716Drug information of Diphenylpyraline, 2008. eduDrugs.
Ref 550717Drug information of Buclizine, 2008. eduDrugs.
Ref 550725Drug information of Mequitazine, 2008. eduDrugs.
Ref 550730Drug information of Aceprometazine, 2008. eduDrugs.
Ref 550767Drug information of Phenindamine, 2008. eduDrugs.
Ref 550773Drug information of Chlophedianol, 2008. eduDrugs.
Ref 550775Drug information of Trimeprazine, 2008. eduDrugs.
Ref 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
Ref
Ref 525803Bioorg Med Chem Lett. 2000 Jun 5;10(11):1277-9.Conformationally-restricted ligands for the histamine H1 receptor.
Ref 526246ReN 1869, a novel tricyclic antihistamine, is active against neurogenic pain and inflammation. Eur J Pharmacol. 2002 Jan 18;435(1):43-57.
Ref 526358J Pharmacol Exp Ther. 2002 Jul;302(1):328-36.A novel phenylaminotetralin radioligand reveals a subpopulation of histamine H(1) receptors.
Ref 526569Multiple differences in agonist and antagonist pharmacology between human and guinea pig histamine H1-receptor. J Pharmacol Exp Ther. 2003 Jun;305(3):1104-15. Epub 2003 Mar 6.
Ref 527045Evaluation of in vivo selective binding of [11C]doxepin to histamine H1 receptors in five animal species. Nucl Med Biol. 2004 May;31(4):493-502.
Ref 527113Large-scale overproduction, functional purification and ligand affinities of the His-tagged human histamine H1 receptor. Eur J Biochem. 2004 Jul;271(13):2636-46.
Ref 527345Population pharmacokinetics of epinastine, a histamine H1 receptor antagonist, in adults and children. Br J Clin Pharmacol. 2005 Jan;59(1):43-53.
Ref 527359The effect of a novel, dual function histamine H1 receptor antagonist/5-lipoxygenase enzyme inhibitor on in vivo dermal inflammation and extravasation. Eur J Pharmacol. 2005 Jan 4;506(3):265-71. Epub 2004 Dec 1.
Ref 527411Bioorg Med Chem Lett. 2005 Feb 15;15(4):1083-5.5-Lipoxygenase inhibition by N-hydroxycarbamates in dual-function compounds.
Ref 527589Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and selective H4 receptor agonist. J Pharmacol Exp Ther. 2005 Sep;314(3):1310-21. Epub 2005 Jun 9.
Ref 527799J Med Chem. 2005 Oct 20;48(21):6523-43.Designed multiple ligands. An emerging drug discovery paradigm.
Ref 527929Effect of BN 52256 and other mediator antagonists on ouabain-induced cardiac arrhythmia in a model of anaphylaxis in guinea-pigs. Pharmacol Res. 1992 Feb-Mar;25(2):173-80.
Ref 527955Probing ligand-specific histamine H1- and H2-receptor conformations with NG-acylated Imidazolylpropylguanidines. J Pharmacol Exp Ther. 2006 Apr;317(1):139-46. Epub 2006 Jan 4.
Ref 528242A double-blind placebo controlled dose response study of noberastine on histamine induced weal and flare. Eur J Clin Pharmacol. 1991;40(1):83-5.
Ref 528772Bioorg Med Chem. 2007 Jun 1;15(11):3649-60. Epub 2007 Mar 21.Tricyclic isoxazolines: identification of R226161 as a potential new antidepressant that combines potent serotonin reuptake inhibition and alpha2-adrenoceptor antagonism.
Ref 529032Antimicrob Agents Chemother. 2007 Nov;51(11):4133-40. Epub 2007 Sep 10.Design, synthesis, and evaluation of 10-N-substituted acridones as novel chemosensitizers in Plasmodium falciparum.
Ref 529341Preclinical efficacy and safety pharmacology of SUN-1334H, a potent orally active antihistamine agent. Drugs R D. 2008;9(2):93-112.
Ref 529387J Med Chem. 2008 Apr 24;51(8):2457-67. Epub 2008 Mar 22.Fragment based design of new H4 receptor-ligands with anti-inflammatory properties in vivo.
Ref 530299Bioorg Med Chem Lett. 2009 Sep 1;19(17):5043-7. Epub 2009 Aug 5.Structural determinants for histamine H(1) affinity, hERG affinity and QTc prolongation in a series of terfenadine analogs.
Ref 530300J Med Chem. 2009 Sep 10;52(17):5307-10.Characterization of novel selective H1-antihistamines for clinical evaluation in the treatment of insomnia.
Ref 530331Bioorg Med Chem. 2009 Sep 15;17(18):6496-504. Epub 2009 Aug 13.Synthesis, structure-affinity relationships, and modeling of AMDA analogs at 5-HT2A and H1 receptors: structural factors contributing to selectivity.
Ref 530547Bioorg Med Chem Lett. 2010 Jan 1;20(1):78-82. Epub 2009 Nov 14.Synthesis and biological activity of 5-styryl and 5-phenethyl-substituted 2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indoles.
Ref 530666Bioorg Med Chem. 2010 Feb 15;18(4):1626-32. Epub 2010 Jan 4.Stereoselective synthesis of desloratadine derivatives as antagonist of histamine.
Ref 531079J Med Chem. 2010 Sep 9;53(17):6386-97.Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 receptor agonist with unprecedented selectivity and procognitive potential.
Ref 531171J Med Chem. 2010 Oct 14;53(19):7021-34.Exploring the neuroleptic substituent in octoclothepin: potential ligands for positron emission tomography with subnanomolar affinity for |A(1)-adrenoceptors.
Ref 531351Mullard A: 2010 FDA drug approvals. Nat Rev Drug Discov. 2011 Feb;10(2):82-5.
Ref 531768High-affinity binding of mequitamium iodide (LG 30435) to muscarinic and histamine H1 receptors. Eur J Pharmacol. 1990 Jul 17;182(3):413-20.
Ref 533039Current Phase II investigational therapies for insomnia. Expert Opin Investig Drugs. 2015 Mar;24(3):401-11.
Ref 534281Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding. Psychopharmacology (Berl). 1996 Mar;124(1-2):57-73.
Ref 534391Studies on the novel antiallergic agent HSR-609: its penetration into the central nervous system in mice and guinea pigs and its selectivity for the histamine H1-receptor. Jpn J Pharmacol. 1997 Apr;73(4):291-8.
Ref 534845Effects of calcium-antagonistic drugs on the stimulation by carbamoylcholine and histamine of phosphatidylinositol turnover in longitudinal smooth muscle of guinea-pig ileum. Biochem J. 1976 Nov 15;160(2):163-9.
Ref 534867A current appreciation of sites for pharmacological intervention in allergic conjunctivitis: effects of new topical ocular drugs. Acta Ophthalmol Scand Suppl. 1999;(228):33-7.
Ref 534875Clinical pharmacology of new histamine H1 receptor antagonists. Clin Pharmacokinet. 1999 May;36(5):329-52.
Ref 534934Combined histamine H1 and H3 receptor blockade produces nasal decongestion in an experimental model of nasal congestion. Am J Rhinol. 1999 Sep-Oct;13(5):391-9.
Ref 534958Histamine as an autocrine regulator of leukemic cell proliferation. Leuk Lymphoma. 2000 Jan;36(3-4):367-73.
Ref 535111Cloning and pharmacological characterization of a fourth histamine receptor (H(4)) expressed in bone marrow. Mol Pharmacol. 2001 Mar;59(3):420-6.
Ref 535112Histamine H1 and H2 receptor antagonists accelerate skin barrier repair and prevent epidermal hyperplasia induced by barrier disruption in a dry environment. J Invest Dermatol. 2001 Feb;116(2):261-5.
Ref 535251Role of central histaminergic system in lorazepam withdrawal syndrome in rats. Pharmacol Biochem Behav. 2001 Apr;68(4):777-82.
Ref 535339Influence of chronic treatment with H1 receptor antagonists on the anticonvulsant activity of antiepileptic drugs. Pol J Pharmacol. 2001 Jan-Feb;53(1):93-6.
Ref 535364Mechanisms and abuse liability of the anti-histamine dimenhydrinate. Neurosci Biobehav Rev. 2002 Jan;26(1):61-7.
Ref 535368Comparison of cyclizine and ondansetron for the prevention of postoperative nausea and vomiting in laparoscopic day-case gynaecological surgery. Anaesthesia. 2002 Jan;57(1):61-5.
Ref 535477Central effects of cinnarizine: restricted use in aircrew. Aviat Space Environ Med. 2002 Jun;73(6):570-4.
Ref 535660Knockouts model the 100 best-selling drugs--will they model the next 100? Nat Rev Drug Discov. 2003 Jan;2(1):38-51.
Ref 535716Histamine H1-receptor antagonists, promethazine and homochlorcyclizine, increase the steady-state plasma concentrations of haloperidol and reduced haloperidol. Ther Drug Monit. 2003 Apr;25(2):192-6.
Ref 535805Toxicologic and clinical appraisal of buclizine, a new antihistaminic compound. J Allergy. 1956 Jan;27(1):63-7.
Ref 535848Effects of fexofenadine and other antihistamines on components of the allergic response: adhesion molecules. J Allergy Clin Immunol. 2003 Oct;112(4 Suppl):S78-82.
Ref 535859Effects of dimethindene maleate nasal spray on the quality of life in seasonal allergic rhinitis. Rhinology. 2003 Sep;41(3):159-66.
Ref 535869Prostaglandin E2 aggravates gastric mucosal injury induced by histamine in rats through EP1 receptors. Life Sci. 2003 Dec 19;74(5):629-41.
Ref 5359148R-lisuride is a potent stereospecific histamine H1-receptor partial agonist. Mol Pharmacol. 2004 Mar;65(3):538-49.
Ref 535933Prescription and safety of dimethindene maleate micropellet capsules in Hungary. Orv Hetil. 2004 Feb 15;145(7):327-9.
Ref 535973Influence of antazoline and ketotifen on the anticonvulsant activity of conventional antiepileptics against maximal electroshock in mice. Eur Neuropsychopharmacol. 2004 Aug;14(4):307-18.
Ref 536000Steady-state brain concentrations of antihistamines in rats: interplay of membrane permeability, P-glycoprotein efflux and plasma protein binding. Pharmacology. 2004 Oct;72(2):92-8.
Ref 536003Role of N-methyl-D-aspartate receptors in gastric mucosal blood flow induced by histamine. J Neurosci Res. 2004 Sep 1;77(5):730-8.
Ref 536086Involvement of histamine H1 and H2 receptors in the regulation of STAT-1 phosphorylation: inverse agonism exhibited by the receptor antagonists. Int Immunopharmacol. 2005 Jul;5(7-8):1299-309.
Ref 536089Antihistamines in the treatment of dermatitis. J Cutan Med Surg. 2003 Nov-Dec;7(6):467-73.
Ref 536119Emerging drugs for ocular allergy. Expert Opin Emerg Drugs. 2005 Aug;10(3):505-20.
Ref 536153Effectiveness of alimemazine in controlling retching after Nissen fundoplication. J Pediatr Surg. 2005 Nov;40(11):1737-40.
Ref 536284Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34.
Ref 536316How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
Ref 536430First-generation H1 antihistamines found in pilot fatalities of civil aviation accidents, 1990-2005. Aviat Space Environ Med. 2007 May;78(5):514-22.
Ref 536469Novel therapeutic usage of low-dose doxepin hydrochloride. Expert Opin Investig Drugs. 2007 Aug;16(8):1295-305.
Ref 536618Stereoselective synthesis of (-)-hydroxyclemastine as a versatile intermediate for the H1 receptor antagonist clemastine. Arch Pharm Res. 2007 Dec;30(12):1521-5.
Ref 536700Intact cell binding for in vitro prediction of sedative and non-sedative histamine H1-receptor antagonists based on receptor internalization. J Pharmacol Sci. 2008 May;107(1):66-79. Epub 2008 Apr 29.
Ref 536707The effect of a combined therapy with a histamine H1 antagonist and a chemical mediator release inhibitor on allergic conjunctivitis. Ophthalmologica. 2008;222(4):232-9. Epub 2008 May 8.
Ref 536717Histamine H1-receptor antagonists inhibit nuclear factor-kappaB and activator protein-1 activities via H1-receptor-dependent and -independent mechanisms. Clin Exp Allergy. 2008 Jun;38(6):947-56.
Ref 536720Cyproheptadine displays preclinical activity in myeloma and leukemia. Blood. 2008 Aug 1;112(3):760-9. Epub 2008 May 23.
Ref 536727Small mouse cholangiocytes proliferate in response to H1 histamine receptor stimulation by activation of the IP3/CaMK I/CREB pathway. Am J Physiol Cell Physiol. 2008 Aug;295(2):C499-513. Epub 2008 May 28.
Ref 536744Histamine upregulates keratinocyte MMP-9 production via the histamine H1 receptor. J Invest Dermatol. 2008 Dec;128(12):2783-91. Epub 2008 Jun 12.
Ref 536767Mast cells play a critical role in the pathogenesis of viral myocarditis. Circulation. 2008 Jul 22;118(4):363-72. Epub 2008 Jul 7.
Ref 536800Contribution of alpha4beta1 integrin to the antiallergic effect of levocabastine. Biochem Pharmacol. 2008 Sep 15;76(6):751-62. Epub 2008 Jul 15.
Ref 536811Efficiency of mequitazine in the treatment of allergic rhinitis and chronic urticaria in children. A bibliographic systematic review. Rev Alerg Mex. 2008 Jan-Feb;55(1):3-9.
Ref 536846Physicochemical, pharmacological and pharmacokinetic properties of the zwitterionic antihistamines cetirizine and levocetirizine. Curr Med Chem. 2008;15(21):2173-91.
Ref 536878Histamine 1 receptor antagonist in symptomatic treatment of renal colic accompanied by nausea: two birds with one stone? Urology. 2009 Jan;73(1):32-6. Epub 2008 Oct 11.
Ref 536896Histamine excites rat lateral vestibular nuclear neurons through activation of post-synaptic H2 receptors. Neurosci Lett. 2008 Dec 19;448(1):15-9. Epub 2008 Oct 14.
Ref 536963Hydroxyzine, a first generation H(1)-receptor antagonist, inhibits human ether-a-go-go-related gene (HERG) current and causes syncope in a patient with the HERG mutation. J Pharmacol Sci. 2008 Dec;108(4):462-71. Epub 2008 Dec 5.
Ref 537070Histamine and the convulsive threshold or effectiveness of antiepileptic drugs. Przegl Lek. 2008;65(11):803-6.
Ref 537072Update on prescription and over-the-counter histamine inverse agonists in rhinitis therapy. Curr Allergy Asthma Rep. 2009 Mar;9(2):140-8.
Ref 537098Examining the tolerability of the non-sedating antihistamine desloratadine: a prescription-event monitoring study in England. Drug Saf. 2009;32(2):169-79. doi: 10.2165/00002018-200932020-00009.
Ref 537168Analytical method for simultaneously measuring ex vivo drug receptor occupancy and dissociation rate: application to (R)-dimethindene occupancy of central histamine H1 receptors. J Recept Signal Transduct Res. 2009;29(2):84-93.
Ref 537248Influence of epinastine hydrochloride, an H1-receptor antagonist, on the function of mite allergen-pulsed murine bone marrow-derived dendritic cells in vitro and in vivo. Mediators Inflamm. 2009;2009:738038. Epub 2009 Apr 9.
Ref 537328Histamine H1 receptor induces cytosolic calcium increase and aquaporin translocation in human salivary gland cells. J Pharmacol Exp Ther. 2009 Aug;330(2):403-12. Epub 2009 May 14.
Ref 537347Clinical research of Ibudilast on treating the steroid resistant allergic rhinitis. Lin Chung Er Bi Yan Hou Tou Jing Wai Ke Za Zhi. 2009 Jan;23(2):63-6.
Ref 537488Design, synthesis and histamine H1-receptor antagonistic activity of some novel 4-amino-2-(substituted)-5-(substituted) aryl-6-[(substituted aryl) amino] pyrimidines. Arzneimittelforschung. 2009;59(5):243-7.
Ref 537502Receptor mediation and nociceptin inhibition of bradykinin-induced plasma extravasation in the knee joint of the rat. Inflamm Res. 2009 Jun 21.
Ref 537515Antinociception induced by central administration of histamine in the formalin test in rats. Indian J Physiol Pharmacol. 2008 Jul-Sep;52(3):249-54.
Ref 537537Emedastine difumarate: a review of its potential ameliorating effect for tissue remodeling in allergic diseases. Expert Opin Pharmacother. 2009 Aug;10(11):1859-67.
Ref 537648Studies on synergism between penicillins and ambodryl (bromodiphenhydramine HCl), an antihistamine with antimicrobial property. Indian J Exp Biol. 1990 Mar;28(3):253-8.
Ref 537651Comparative effects of loratadine and azatadine in the treatment of seasonal allergic rhinitis. Asian Pac J Allergy Immunol. 1990 Dec;8(2):103-7.
Ref 537691Nonsedating histamine H1-receptor antagonists. Clin Pharm. 1989 May;8(5):331-44.
Ref 537703Effect of H1 blockers alone and in combination with morphine to produce antinociception in mice. Neuropharmacology. 1985 Jan;24(1):1-4.
Ref 537714The in vivo potency and selectivity of azelastine as an H1 histamine-receptor antagonist in human airways and skin. J Allergy Clin Immunol. 1988 Dec;82(6):1113-8.
Ref 537715Identification and differentiation of alkylamine antihistamines and their metabolites in urine by computerized gas chromatography-mass spectrometry. J Chromatogr. 1988 Aug 19;430(1):31-41.
Ref 537829Comparison of the effects of eleven histamine H1-receptor antagonists on monoamine turnover in the mouse brain. Naunyn Schmiedebergs Arch Pharmacol. 1994 Feb;349(2):140-4.
Ref 537846The histamine H1-receptor antagonist binding site. A stereoselective pharmacophoric model based upon (semi-)rigid H1-antagonists and including a known interaction site on the receptor. J Med Chem. 1995 Aug 18;38(17):3351-60.
Ref 537884Inhibition by histamine H1 receptor antagonists of endogenous glibenclamide-sensitive K+ channels in follicle-enclosed Xenopus oocytes. Eur J Pharmacol. 1994 Jan 1;266(1):99-102.
Ref 537890Synthesis and combined H1-/H2 antagonist activity of mepyramine, pheniramine and cyclizine derivatives with cyanoguanidine, urea and nitroethenediamine partial structures. Arch Pharm (Weinheim). 1994Jul;327(7):455-62.
Ref 537891Transport mechanism of an H1-antagonist at the blood-brain barrier: transport mechanism of mepyramine using the carotid injection technique. Biol Pharm Bull. 1994 May;17(5):676-9.
Ref 537912Histamine-induced venodilation in human beings involves both H1 and H2 receptor subtypes. J Allergy Clin Immunol. 1994 Mar;93(3):606-14.
Ref 538066Effect of descarboethoxyloratadine, the major metabolite of loratadine, on the human cardiac potassium channel Kv1.5. Br J Pharmacol. 1997 Nov;122(5):796-8.
Ref 538137H2 histaminergic control of inhibition of eating induced by intragastric NaCl in rats. Physiol Behav. 1998 Aug;65(1):105-13.
Ref 538157Second-generation antihistamines: a comparative review. Drugs. 1999 Jan;57(1):31-47.
Ref 543664(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 262).
Ref 544069Betahistine in the treatment of M?ni?re's disease. Neuropsychiatr Dis Treat. 2007 August; 3(4): 429-440.
Ref 547978Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800020866)
Ref 550963Clinical pipeline report, company report or official report of GlaxoSmithKline (2009).
Ref 551442Clinical pipeline report, company report or official report of NicOx SA.
Ref 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
Ref 556264Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
Ref 1572591Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.
Ref 1587926URL: https://www.ebi.ac.uk/chembl/ The ChEMBL database in 2017

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