Target General Infomation
Target ID
T64765
Former ID
TTDC00079
Target Name
Histamine H3 receptor
Gene Name
HRH3
Synonyms
G protein-coupled receptor 97; HH3R; Histamine receptor 3; HRH3
Target Type
Clinical Trial
Disease Anxiety disorder [ICD9: 300, 311; ICD10: F32, F40-F42]
Alzheimer disease; Schizophrenia [ICD9:331, 295; ICD10: G30, F20]
Allergic rhinitis [ICD9: 472.0, 477, 995.3; ICD10: J00, J30, J31.0, T78.4]
Alzheimer disease [ICD9: 331; ICD10: G30]
Attention deficit hyperactivity disorder [ICD9: 314; ICD10: F90]
Alcohol use disorders [ICD9: 303; ICD10: F10.2]
Central nervous system disease [ICD10: G00-G99]
Cognitive disorders [ICD9: 290-294, 294.0, 780.09, 780.9, 780.93; ICD10: F01-F07, F04, F05, R41.3]
Dementia; Obesity [ICD9:290-294, 278; ICD10: F01-F07, E66]
Diabetic neuropathy; Musculoskeletal pain [ICD9:250, 250.6, 356.0, 356.8, 338, 780; ICD10: E11.40, R52, G89]
Dementia [ICD9: 290-294; ICD10: F01-F07]
Eating disorder; Epilepsy; Pain [ICD9: 307.5, 338,780; ICD10: F50, R52, G89]
Excessive daytime sleepiness [ICD9: 291.82, 292.85, 307.43-307.44, 327.1, 780.53-780.54; ICD10: F51.1, G47.1]
Metabolic disorders [ICD9: 270-279; ICD10: E70-E89]
Mild to moderate alzheimer disease; Dementia [ICD9: 290-294, 331.0; ICD10: F01-F07, G30]
Neurological disease [ICD9: 338, 338.2, 410, 782.3,780; ICD10: I21, I22, R52, R52.1-R52.2, R60.9, G89]
Narcolepsy [ICD9: 347; ICD10: G47.4]
Obese insulin-resistant disorders [ICD9: 250; ICD10: E11]
Obesity [ICD9: 278; ICD10: E66]
Pain [ICD9: 338, 356.0, 356.8,780; ICD10: G64, G90.0, R52, G89]
Schizophrenia [ICD9: 295; ICD10: F20]
Sleep disorders [ICD9: 307.4, 327, 780.5; ICD10: F51, G47]
Function
The H3 subclass of histamine receptors could mediate the histamine signals in CNS and peripheral nervous system. Signals through the inhibition of adenylate cyclase and displays high constitutive activity (spontaneous activity in the absence of agonist). Agonist stimulation of isoform 3 neither modified adenylate cyclase activity nor induced intracellular calcium mobilization.
BioChemical Class
GPCR rhodopsin
Target Validation
T64765
UniProt ID
Sequence
MERAPPDGPLNASGALAGEAAAAGGARGFSAAWTAVLAALMALLIVATVLGNALVMLAFV
ADSSLRTQNNFFLLNLAISDFLVGAFCIPLYVPYVLTGRWTFGRGLCKLWLVVDYLLCTS
SAFNIVLISYDRFLSVTRAVSYRAQQGDTRRAVRKMLLVWVLAFLLYGPAILSWEYLSGG
SSIPEGHCYAEFFYNWYFLITASTLEFFTPFLSVTFFNLSIYLNIQRRTRLRLDGAREAA
GPEPPPEAQPSPPPPPGCWGCWQKGHGEAMPLHRYGVGEAAVGAEAGEATLGGGGGGGSV
ASPTSSSGSSSRGTERPRSLKRGSKPSASSASLEKRMKMVSQSFTQRFRLSRDRKVAKSL
AVIVSIFGLCWAPYTLLMIIRAACHGHCVPDYWYETSFWLLWANSAVNPVLYPLCHHSFR
RAFTKLLCPQKLKIQPHSSLEHCWK
Drugs and Mode of Action
Drug(s) Pitolisant Drug Info Phase 3 Schizophrenia [524221]
ABT-288 Drug Info Phase 2 Alzheimer disease; Schizophrenia [522864], [541972]
ABT-652 Drug Info Phase 2 Diabetic neuropathy; Musculoskeletal pain [523180]
AZD-5213 Drug Info Phase 2 Alzheimer disease [523825]
Bavisant Drug Info Phase 2 Attention deficit hyperactivity disorder [522173]
GSK239512 Drug Info Phase 2 Mild to moderate alzheimer disease; Dementia [524191]
JNJ-17216498 Drug Info Phase 2 Narcolepsy [521955]
JNJ-39220675 Drug Info Phase 2 Alcohol use disorders [522512]
S-38093 Drug Info Phase 2 Alzheimer disease [549097]
SAR-110894 Drug Info Phase 2 Alzheimer disease [523311]
ABT-239 Drug Info Phase 1 Cognitive disorders [536039], [538729]
APD-916 Drug Info Phase 1 Sleep disorders [522988]
HPP404 Drug Info Phase 1 Allergic rhinitis [551746]
Irdabisant Drug Info Phase 1 Cognitive disorders [524373]
MK-3134 Drug Info Phase 1 Dementia [522645]
MK-7288 Drug Info Phase 1 Excessive daytime sleepiness [522986]
MK-0249 Drug Info Clinical trial Obese insulin-resistant disorders [532558]
BP-2.94 Drug Info Discontinued in Phase 2 Pain [546450]
Cipralisant Drug Info Discontinued in Phase 2 Attention deficit hyperactivity disorder [536225], [538758]
GSK835726 Drug Info Discontinued in Phase 2 Allergic rhinitis [548731]
GSK1004723 Drug Info Discontinued in Phase 1 Allergic rhinitis [548732]
SAR-152954 Drug Info Discontinued in Phase 1 Sleep disorders [549206]
GR-175737 Drug Info Terminated Discovery agent [538757], [546329]
GT-2016 Drug Info Terminated Alzheimer disease [545044]
GT-2203 Drug Info Terminated Anxiety disorder [546559]
Thioperamide Drug Info Terminated Cognitive disorders [538782], [545719]
UCL-1390 Drug Info Terminated Eating disorder; Epilepsy; Pain [545875]
Inhibitor (1H-indol-2-yl)(piperazin-1-yl)methanone Drug Info [527934]
(1R,2R)-2-(1H-Imidazol-4-yl)-1-methyl-propylamine Drug Info [533720]
(1R,2S)-2-(1H-Imidazol-4-yl)-1-methyl-propylamine Drug Info [533720]
(1S,2S)-2-(1H-Imidazol-4-yl)-cyclopentylamine Drug Info [533720]
(R)-1-(2-methoxyphenethyl)-2-methylpyrrolidine Drug Info [529212]
(R)-1-(3-methoxyphenethyl)-2-methylpyrrolidine Drug Info [529212]
(R)-1-(4-methoxyphenethyl)-2-methylpyrrolidine Drug Info [529212]
(R)-1-(4-nitrophenethyl)-2-methylpyrrolidine Drug Info [529212]
(R)-2-(2-(2-methylpyrrolidin-1-yl)ethyl)phenol Drug Info [529212]
(R)-2-(2-(2-methylpyrrolidin-1-yl)ethyl)pyridine Drug Info [529212]
(R)-2-methyl-1-(2-m-tolyl-ethyl)-pyrrolidine Drug Info [529212]
(R)-2-methyl-1-(2-p-tolyl-ethyl)-pyrrolidine Drug Info [529212]
(R)-3-(1H-imidazol-4-yl)propyl sec-butylcarbamate Drug Info [530465]
(R)-3-(2-(2-methylpyrrolidin-1-yl)ethyl)pyridine Drug Info [529212]
(R)-4-(2-(2-methylpyrrolidin-1-yl)ethyl)pyridine Drug Info [529212]
(R)-6-(2-(2-methylpyrrolidin-1-yl)ethyl)quinoline Drug Info [530904]
(S)-1-(2-methoxyphenethyl)-2-methylpyrrolidine Drug Info [529212]
(S)-1-(3-methoxyphenethyl)-2-methylpyrrolidine Drug Info [529212]
(S)-1-(4-methoxyphenethyl)-2-methylpyrrolidine Drug Info [529212]
(S)-1-(4-nitrophenethyl)-2-methylpyrrolidine Drug Info [529212]
(S)-2-(2-(2-methylpyrrolidin-1-yl)ethyl)phenol Drug Info [529212]
(S)-2-(2-(2-methylpyrrolidin-1-yl)ethyl)pyridine Drug Info [529212]
(S)-2-methyl-1-(2-m-tolyl-ethyl)-pyrrolidine Drug Info [529212]
(S)-2-methyl-1-(2-p-tolyl-ethyl)-pyrrolidine Drug Info [529212]
(S)-3-(1H-imidazol-4-yl)propyl sec-butylcarbamate Drug Info [530465]
(S)-4-(2-(2-methylpyrrolidin-1-yl)ethyl)pyridine Drug Info [529212]
1-(2-(naphthalen-2-yl)ethyl)pyrrolidine Drug Info [529212]
1-(2-m-tolyl-ethyl)-pyrrolidine Drug Info [529212]
1-(2-methoxyphenethyl)pyrrolidine Drug Info [529212]
1-(2-p-tolyl-ethyl)-pyrrolidine Drug Info [529212]
1-(3-(2-(3-methoxyphenoxy)ethoxy)propyl)azepane Drug Info [530044]
1-(3-(3-phenylpropoxy)propyl)piperidine Drug Info [529673]
1-(3-(4-(2-fluoroethyl)phenoxy)propyl)piperidine Drug Info [530019]
1-(3-(4-(fluoromethyl)phenoxy)propyl)piperidine Drug Info [530019]
1-(3-methoxyphenethyl)pyrrolidine Drug Info [529212]
1-(4-(benzyloxy)phenethyl)pyrrolidine Drug Info [529212]
1-(4-methoxyphenethyl)pyrrolidine Drug Info [529212]
1-(4-nitrophenethyl)pyrrolidine Drug Info [529212]
1-[2-(2,4,6-trimethyl-phenyl)-ethyl]-pyrrolidine Drug Info [529212]
2-((1H-imidazol-4-yl)methyl)pyridine Drug Info [531088]
2-((2-ethoxyphenoxy)methyl)-4-isopropylmorpholine Drug Info [529751]
2-(1,4'-bipiperidin-1'-yl)thiazolo[4,5-b]pyridine Drug Info [530397]
2-(1,4'-bipiperidin-1'-yl)thiazolo[4,5-c]pyridine Drug Info [530397]
2-(1H-Imidazol-4-yl)-cyclopropylamine Drug Info [526614]
2-(2-(4-tert-Butylphenylthio)ethyl)-1H-imidazole Drug Info [531088]
2-(2-(pyrrolidin-1-yl)ethyl)-1H-indole Drug Info [529212]
2-(2-(pyrrolidin-1-yl)ethyl)phenol Drug Info [529212]
2-(2-(pyrrolidin-1-yl)ethyl)pyridine Drug Info [529212]
2-(3-Methyl-3H-imidazol-4-yl)-ethylamine Drug Info [534790]
2-(4-Cyclopentyl-piperazin-1-yl)-quinoline Drug Info [527370]
2-(4-Cyclopropyl-piperazin-1-yl)-quinoline Drug Info [527370]
2-(4-Isopropyl-piperazin-1-yl)-quinoline Drug Info [527370]
2-(4-Methyl-piperazin-1-yl)-quinoline Drug Info [527370]
2-(4-Propyl-piperazin-1-yl)-quinoline Drug Info [527370]
2-(ethoxycarbonyl)-1H-indole-5-carboxylic acid Drug Info [530151]
2-[2-(1H-Imidazol-4-yl)-cyclopropyl]-ethylamine Drug Info [526614]
2-[4-(1-Ethyl-propyl)-piperazin-1-yl]-quinoline Drug Info [527370]
3-((1H-imidazol-4-yl)methyl)pyridine Drug Info [531088]
4-((1H-imidazol-4-yl)methyl)-1-heptylpiperidine Drug Info [527818]
4-((1H-Imidazol-4-yl)methyl)-1-phenylpiperidine Drug Info [551227]
4-((2R,3S)-2-Methyl-pyrrolidin-3-yl)-1H-imidazole Drug Info [533720]
4-((2S,3R)-2-Methyl-pyrrolidin-3-yl)-1H-imidazole Drug Info [533720]
4-(2-(3,4-Dimethylphenylamino)ethyl)-1H-imidazole Drug Info [530846]
4-(2-(3-tert-Butylphenylamino)ethyl)-1H-imidazole Drug Info [530846]
4-(2-(4-Cyclohexylphenylamino)ethyl)-1H-imidazole Drug Info [530846]
4-(2-(4-Methoxyphenylamino)ethyl)-1H-imidazole Drug Info [530846]
4-(2-(4-Methylphenylamino)ethyl)-1H-imidazole Drug Info [530846]
4-(2-(4-tert-Butylphenylamino)ethyl)-1H-imidazole Drug Info [530846]
4-(2-(Cyclohexylamino)ethyl)-1H-imidazole Drug Info [530846]
4-(2-(Phenylamino)ethyl)-1H-imidazole Drug Info [530846]
4-(2-(pyrrolidin-1-yl)ethyl)pyridine Drug Info [529212]
4-(3-Phenoxy-propyl)-1H-imidazole Drug Info [526023]
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one Drug Info [531079]
4-(4-Phenyl-butyl)-1H-imidazole Drug Info [526023]
4-(6-Cyclohexyl-hex-3-ynyl)-1H-imidazole Drug Info [534790]
4-(6-Cyclopentyl-hex-3-ynyl)-1H-imidazole Drug Info [534790]
4-(7,7-Dimethyl-oct-3-ynyl)-1H-imidazole Drug Info [534790]
4-(7-Methyl-oct-3-ynyl)-1H-imidazole Drug Info [534790]
4-(8-Phenyl-oct-3-ynyl)-1H-imidazole Drug Info [534790]
4-Benzyl-1-[3-phenylpropoxy)propyl]piperidine Drug Info [529673]
4-Butyl-1-[3-(phenylpropoxy)propyl]piperidine Drug Info [529673]
4-Hept-3-ynyl-1H-imidazole Drug Info [534790]
4-Hex-3-ynyl-1H-imidazole Drug Info [534790]
4-isopropyl-2-(phenoxymethyl)morpholine Drug Info [529751]
4-Propyl-1-[3-(phenylpropoxy)propyl]piperidine Drug Info [529673]
4-[3-(4-Butyl-phenoxy)-propyl]-1H-imidazole Drug Info [525896]
4-[3-(4-Ethynyl-phenoxy)-propyl]-1H-imidazole Drug Info [525896]
4-[3-(4-Methoxy-phenoxy)-propyl]-1H-imidazole Drug Info [526023]
5-(2-(pyrrolidin-1-yl)ethyl)isothiazole Drug Info [529212]
5-ethyl-2-(2-(pyrrolidin-1-yl)ethyl)pyridine Drug Info [529212]
5-methoxy-2-(2-(pyrrolidin-1-yl)ethyl)-1H-indole Drug Info [529212]
5-phenyl-2-(4-(piperidin-1-yl)butyl)oxazole Drug Info [531116]
Aerophobin-1 Drug Info [551359]
APLYSAMINE Drug Info [529632]
C-[2-(1H-Imidazol-4-yl)-cyclopropyl]-methylamine Drug Info [526614]
CARCININE Drug Info [529632]
CONESSINE Drug Info [530254]
Des-bromoaplysamine-1 Drug Info [527879]
GR-175737 Drug Info [534790]
GT-2016 Drug Info [534790]
IODOPROXYFAN Drug Info [526023]
JNJ-28583867 Drug Info [529199]
N-benzyl-4-cyclopentylpiperazine-1-carboxamide Drug Info [528367]
N-methyl-2-(pyridin-2-yl)ethanamine Drug Info [530151]
ST-1025 Drug Info [531116]
ST-1093 Drug Info [531116]
UCL-2138 Drug Info [530019]
VERONGAMINE Drug Info [551359]
VUF-10214 Drug Info [529387]
VUF-5296 Drug Info [526614]
VUF-5297 Drug Info [526614]
Agonist (R)-alpha-methylhistamine Drug Info [535262], [536039]
(S)-alpha-methylhistamine Drug Info [526445]
GT-2203 Drug Info [543673]
H3 receptor inverse agonists Drug Info [543673]
imbutamine Drug Info [526894]
Imetit Drug Info [536039]
Immepip Drug Info [536039]
Immethridine Drug Info [536039]
impentamine Drug Info [526894]
impromidine Drug Info [535111]
Methimepip Drug Info [536039]
MK-0249 Drug Info [529576]
MK-3134 Drug Info [531503]
MK-7288 Drug Info [532509]
N-methylhistamine Drug Info [535111]
N-[3H]alpha-methylhistamine Drug Info [526605]
N-[3H]methylhistamine Drug Info [535111]
Pitolisant Drug Info [532787]
VUF 5207 Drug Info [526200]
VUF 8328 Drug Info [526200]
[3H](R)-alpha-methylhistamine Drug Info [535111]
Antagonist A-304121 Drug Info [527161]
A-317920 Drug Info [536039]
A-331440 Drug Info [536039]
ABT-239 Drug Info [536039], [536761], [537279]
APD-916 Drug Info [531737]
ATH-90879 Drug Info [543673]
AZD-5213 Drug Info [531888]
Bavisant Drug Info [531879]
burimamide Drug Info [535111]
Ciproxifan Drug Info [536039]
Clobenpropit Drug Info [534934], [536039]
EVT-501 Drug Info [543673]
FUB 349 Drug Info [525918]
FUB-130 Drug Info [543673]
GSK-334429 Drug Info [543673]
GSK1004723 Drug Info [550963]
GSK189254A Drug Info [536039]
GSK239512 Drug Info [550963]
GSK835726 Drug Info [550963]
GT2394 Drug Info [526445]
HPP404 Drug Info [551746]
Irdabisant Drug Info [531661]
JB 98064 Drug Info [526445]
JNJ-17216498 Drug Info [527237]
JNJ-39220675 Drug Info [531268]
JNJ-5207852 Drug Info [536039]
PF-3900422 Drug Info [543673]
Proxyfan Drug Info [536039]
S-38093 Drug Info [549954]
SAR-110894 Drug Info [531888]
SAR-152954 Drug Info [551862]
SCH79687 Drug Info [536039]
SUVN-G1031 Drug Info [543673]
Thioperamide Drug Info [534934], [536039]
UCB-2892 Drug Info [543673]
UCL-1390 Drug Info [536225]
UCL1972 Drug Info [536039]
VUF 4904 Drug Info [526200]
VUF 5681 Drug Info [536039]
VUF5391 Drug Info [536039]
[123I]iodoproxyfan Drug Info [525918]
[125I]iodophenpropit Drug Info [533760]
Modulator ABT-288 Drug Info
ABT-652 Drug Info [549101]
BP-2.94 Drug Info [534203]
Binder Cipralisant Drug Info [536066]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway Neuroactive ligand-receptor interaction
Reactome Histamine receptors
G alpha (i) signalling events
WikiPathways Monoamine Transport
GPCRs, Class A Rhodopsin-like
GPCR ligand binding
GPCR downstream signaling
References
Ref 521955ClinicalTrials.gov (NCT00424931) A Safety and Effectiveness Study of a Single Dose of JNJ-17216498 in Patients With Narcolepsy. U.S. National Institutes of Health.
Ref 522173ClinicalTrials.gov (NCT00566449) A Safety and Effectiveness Study of JNJ-31001074 in Adults With Attention-Deficit/Hyperactivity Disorder.. U.S. National Institutes of Health.
Ref 522512ClinicalTrials.gov (NCT00804687) An Efficacy Study of JNJ-39220675 and Pseudoephedrine in Participants With Allergic Rhinitis. U.S. National Institutes of Health.
Ref 522645ClinicalTrials.gov (NCT00887601) BOLD Functional Magnetic Resonance Imaging (fMRI) and Cerebral Blood Flow Measurements as Biomarkers for Cognition Enhancing Drugs (3134-006). U.S. National Institutes of Health.
Ref 522864ClinicalTrials.gov (NCT01018875) Efficacy and Safety Study of ABT-288 in Subjects With Mild-to-Moderate Alzheimer's Disease. U.S. National Institutes of Health.
Ref 522986ClinicalTrials.gov (NCT01092780) Pharmacodynamics and Efficacy of MK7288 (MK-7288-010). U.S. National Institutes of Health.
Ref 522988ClinicalTrials.gov (NCT01093508) Single-dose Safety Study of APD916 in Healthy Volunteers. U.S. National Institutes of Health.
Ref 523180ClinicalTrials.gov (NCT01207115) A Study of ABT-652 in Adults With Osteoarthritis Pain of the Knee. U.S. National Institutes of Health.
Ref 523311ClinicalTrials.gov (NCT01266525) Effect of Different Doses of SAR110894D on Cognition in Patients With Mild to Moderate Alzheimer's Disease on Donepezil. U.S. National Institutes of Health.
Ref 523825ClinicalTrials.gov (NCT01548287) A Study of the Safety and Tolerability of AZD5213 Effect on Sleep for Patients With Alzheimer's/Cognitive Impairment. U.S. National Institutes of Health.
Ref 524191ClinicalTrials.gov (NCT01772199) Study to Assess Whether GSK239512 Can Remyelinate Lesions in Subjects With Relapsing Remitting Multiple Sclerosis. U.S. National Institutes of Health.
Ref 524221ClinicalTrials.gov (NCT01800045) Pitolisant to Assess Weekly Frequency of Cataplexy Attacks and EDS in Narcoleptic Patients (HARMONY CTP). U.S. National Institutes of Health.
Ref 524373ClinicalTrials.gov (NCT01903824) Pharmacokinetics and Pharmacodynamics (PK/PD) of CEP-26401 in Healthy Subjects. U.S. National Institutes of Health.
Ref 532558(11)C-MK-8278 PET as a tool for pharmacodynamic brain occupancy of histamine 3 receptor inverse agonists. J Nucl Med. 2014 Jan;55(1):65-72.
Ref 536039The histamine H3 receptor: from gene cloning to H3 receptor drugs. Nat Rev Drug Discov. 2005 Feb;4(2):107-20.
Ref 536225Emerging drugs for eating disorder treatment. Expert Opin Emerg Drugs. 2006 May;11(2):315-36.
Ref 538729(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: 1218).
Ref 538757(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: 1243).
Ref 538758(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: 1244).
Ref 538782(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: 1267).
Ref 541972(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: 6927).
Ref 545044Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001957)
Ref 545719Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004362)
Ref 545875Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005172)
Ref 546329Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007507)
Ref 546450Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008192)
Ref 546559Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008938)
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 549097Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800032202)
Ref 549206Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800033674)
Ref 551746Clinical pipeline report, company report or official report of TransTech Pharma (2011).
Ref 525896Bioorg Med Chem Lett. 2000 Oct 16;10(20):2379-82.Analogues and derivatives of ciproxifan, a novel prototype for generating potent histamine H3-receptor antagonists.
Ref 525918Distinct pharmacology of rat and human histamine H(3) receptors: role of two amino acids in the third transmembrane domain. Br J Pharmacol. 2000 Dec;131(7):1247-50.
Ref 526023Bioorg Med Chem Lett. 2001 Apr 9;11(7):951-4.Different antagonist binding properties of human and rat histamine H3 receptors.
Ref 526200Constitutive activity of histamine h(3) receptors stably expressed in SK-N-MC cells: display of agonism and inverse agonism by H(3) antagonists. J Pharmacol Exp Ther. 2001 Dec;299(3):908-14.
Ref 526445Characteristics of recombinantly expressed rat and human histamine H3 receptors. Eur J Pharmacol. 2002 Oct 18;453(1):33-41.
Ref 526605Molecular and pharmacological characterization of the mouse histamine H3 receptor. Eur J Pharmacol. 2003 Apr 25;467(1-3):57-65.
Ref 526614J Med Chem. 2003 May 8;46(10):1980-8.Cyclopropane-based conformational restriction of histamine. (1S,2S)-2-(2-aminoethyl)-1-(1H-imidazol-4-yl)cyclopropane, a highly selective agonist for the histamine H3 receptor, having a cis-cyclopropane structure.
Ref 526894Synthesis and structure-activity relationships of conformationally constrained histamine H(3) receptor agonists. J Med Chem. 2003 Dec 4;46(25):5445-57.
Ref 527161Pharmacological and behavioral properties of A-349821, a selective and potent human histamine H3 receptor antagonist. Biochem Pharmacol. 2004 Sep 1;68(5):933-45.
Ref 527237Acute wake-promoting actions of JNJ-5207852, a novel, diamine-based H3 antagonist. Br J Pharmacol. 2004 Nov;143(5):649-61. Epub 2004 Oct 4.
Ref 527370J Med Chem. 2005 Jan 13;48(1):306-11.2-(4-alkylpiperazin-1-yl)quinolines as a new class of imidazole-free histamine H3 receptor antagonists.
Ref 527818Bioorg Med Chem Lett. 2006 Jan 15;16(2):395-9. Epub 2005 Oct 21.Novel histamine H3 receptor antagonists based on the 4-[(1H-imidazol-4-yl)methyl]piperidine scaffold.
Ref 527879Bioorg Med Chem Lett. 2006 Feb 15;16(4):897-900. Epub 2005 Nov 21.Aplysamine-1 and related analogs as histamine H3 receptor antagonists.
Ref 527934J Med Chem. 2005 Dec 29;48(26):8289-98.Preparation and biological evaluation of indole, benzimidazole, and thienopyrrole piperazine carboxamides: potent human histamine h(4) antagonists.
Ref 528367Bioorg Med Chem Lett. 2006 Oct 15;16(20):5303-8.Ureas with histamine H3-antagonist receptor activity--a new scaffold discovered by lead-hopping from cinnamic acid amides.
Ref 529199Bioorg Med Chem Lett. 2008 Jan 1;18(1):39-43. Epub 2007 Nov 13.Synthesis and biological activity of piperazine and diazepane amides that are histamine H3 antagonists and serotonin reuptake inhibitors.
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