Target Information

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 Attention deficit hyperactivity disorder [ICD9: 314; ICD10: F90]
Alcohol use disorders [ICD9: 303; ICD10: F10.2]
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]
Cognitive disorders [ICD9: 290-294, 294.0, 780.09, 780.9, 780.93; ICD10: F01-F07, F04, F05, R41.3]
Central nervous system disease [ICD10: G00-G99]
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]
Narcolepsy [ICD9: 347; ICD10: G47.4]
Neurological disease [ICD9: 338, 338.2, 410, 782.3,780; ICD10: I21, I22, R52, R52.1-R52.2, R60.9, G89]
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
Q9Y5N1
Sequence
MERAPPDGPLNASGALAGEAAAAGGARGFSAAWTAVLAALMALLIVATVLGNALVMLAFV
ADSSLRTQNNFFLLNLAISDFLVGAFCIPLYVPYVLTGRWTFGRGLCKLWLVVDYLLCTS
SAFNIVLISYDRFLSVTRAVSYRAQQGDTRRAVRKMLLVWVLAFLLYGPAILSWEYLSGG
SSIPEGHCYAEFFYNWYFLITASTLEFFTPFLSVTFFNLSIYLNIQRRTRLRLDGAREAA
GPEPPPEAQPSPPPPPGCWGCWQKGHGEAMPLHRYGVGEAAVGAEAGEATLGGGGGGGSV
ASPTSSSGSSSRGTERPRSLKRGSKPSASSASLEKRMKMVSQSFTQRFRLSRDRKVAKSL
AVIVSIFGLCWAPYTLLMIIRAACHGHCVPDYWYETSFWLLWANSAVNPVLYPLCHHSFR
RAFTKLLCPQKLKIQPHSSLEHCWK
Drugs and Mode of Action
Drug(s) Pitolisant Drug Info Phase 3 Schizophrenia [1]
ABT-288 Drug Info Phase 2 Alzheimer disease; Schizophrenia [2], [3]
ABT-652 Drug Info Phase 2 Diabetic neuropathy; Musculoskeletal pain [4]
AZD-5213 Drug Info Phase 2 Alzheimer disease [5]
Bavisant Drug Info Phase 2 Attention deficit hyperactivity disorder [6]
GSK239512 Drug Info Phase 2 Mild to moderate alzheimer disease; Dementia [7]
JNJ-17216498 Drug Info Phase 2 Narcolepsy [8]
JNJ-39220675 Drug Info Phase 2 Alcohol use disorders [9]
S-38093 Drug Info Phase 2 Alzheimer disease [10]
SAR-110894 Drug Info Phase 2 Alzheimer disease [11]
ABT-239 Drug Info Phase 1 Cognitive disorders [12], [13]
APD-916 Drug Info Phase 1 Sleep disorders [14]
HPP404 Drug Info Phase 1 Allergic rhinitis [15]
Irdabisant Drug Info Phase 1 Cognitive disorders [16]
MK-3134 Drug Info Phase 1 Dementia [17]
MK-7288 Drug Info Phase 1 Excessive daytime sleepiness [18]
MK-0249 Drug Info Clinical trial Obese insulin-resistant disorders [19]
BP-2.94 Drug Info Discontinued in Phase 2 Pain [20]
Cipralisant Drug Info Discontinued in Phase 2 Attention deficit hyperactivity disorder [21], [22]
GSK835726 Drug Info Discontinued in Phase 2 Allergic rhinitis [23]
GSK1004723 Drug Info Discontinued in Phase 1 Allergic rhinitis [24]
SAR-152954 Drug Info Discontinued in Phase 1 Sleep disorders [25]
GR-175737 Drug Info Terminated Discovery agent [26], [27]
GT-2016 Drug Info Terminated Alzheimer disease [28]
GT-2203 Drug Info Terminated Anxiety disorder [29]
Thioperamide Drug Info Terminated Cognitive disorders [30], [31]
UCL-1390 Drug Info Terminated Eating disorder; Epilepsy; Pain [32]
Inhibitor (1H-indol-2-yl)(piperazin-1-yl)methanone Drug Info [33]
(1R,2R)-2-(1H-Imidazol-4-yl)-1-methyl-propylamine Drug Info [34]
(1R,2S)-2-(1H-Imidazol-4-yl)-1-methyl-propylamine Drug Info [34]
(1S,2S)-2-(1H-Imidazol-4-yl)-cyclopentylamine Drug Info [34]
(R)-1-(2-methoxyphenethyl)-2-methylpyrrolidine Drug Info [35]
(R)-1-(3-methoxyphenethyl)-2-methylpyrrolidine Drug Info [35]
(R)-1-(4-methoxyphenethyl)-2-methylpyrrolidine Drug Info [35]
(R)-1-(4-nitrophenethyl)-2-methylpyrrolidine Drug Info [35]
(R)-2-(2-(2-methylpyrrolidin-1-yl)ethyl)phenol Drug Info [35]
(R)-2-(2-(2-methylpyrrolidin-1-yl)ethyl)pyridine Drug Info [35]
(R)-2-methyl-1-(2-m-tolyl-ethyl)-pyrrolidine Drug Info [35]
(R)-2-methyl-1-(2-p-tolyl-ethyl)-pyrrolidine Drug Info [35]
(R)-3-(1H-imidazol-4-yl)propyl sec-butylcarbamate Drug Info [36]
(R)-3-(2-(2-methylpyrrolidin-1-yl)ethyl)pyridine Drug Info [35]
(R)-4-(2-(2-methylpyrrolidin-1-yl)ethyl)pyridine Drug Info [35]
(R)-6-(2-(2-methylpyrrolidin-1-yl)ethyl)quinoline Drug Info [37]
(S)-1-(2-methoxyphenethyl)-2-methylpyrrolidine Drug Info [35]
(S)-1-(3-methoxyphenethyl)-2-methylpyrrolidine Drug Info [35]
(S)-1-(4-methoxyphenethyl)-2-methylpyrrolidine Drug Info [35]
(S)-1-(4-nitrophenethyl)-2-methylpyrrolidine Drug Info [35]
(S)-2-(2-(2-methylpyrrolidin-1-yl)ethyl)phenol Drug Info [35]
(S)-2-(2-(2-methylpyrrolidin-1-yl)ethyl)pyridine Drug Info [35]
(S)-2-methyl-1-(2-m-tolyl-ethyl)-pyrrolidine Drug Info [35]
(S)-2-methyl-1-(2-p-tolyl-ethyl)-pyrrolidine Drug Info [35]
(S)-3-(1H-imidazol-4-yl)propyl sec-butylcarbamate Drug Info [36]
(S)-4-(2-(2-methylpyrrolidin-1-yl)ethyl)pyridine Drug Info [35]
1-(2-(naphthalen-2-yl)ethyl)pyrrolidine Drug Info [35]
1-(2-m-tolyl-ethyl)-pyrrolidine Drug Info [35]
1-(2-methoxyphenethyl)pyrrolidine Drug Info [35]
1-(2-p-tolyl-ethyl)-pyrrolidine Drug Info [35]
1-(3-(2-(3-methoxyphenoxy)ethoxy)propyl)azepane Drug Info [38]
1-(3-(3-phenylpropoxy)propyl)piperidine Drug Info [39]
1-(3-(4-(2-fluoroethyl)phenoxy)propyl)piperidine Drug Info [40]
1-(3-(4-(fluoromethyl)phenoxy)propyl)piperidine Drug Info [40]
1-(3-methoxyphenethyl)pyrrolidine Drug Info [35]
1-(4-(benzyloxy)phenethyl)pyrrolidine Drug Info [35]
1-(4-methoxyphenethyl)pyrrolidine Drug Info [35]
1-(4-nitrophenethyl)pyrrolidine Drug Info [35]
1-[2-(2,4,6-trimethyl-phenyl)-ethyl]-pyrrolidine Drug Info [35]
2-((1H-imidazol-4-yl)methyl)pyridine Drug Info [41]
2-((2-ethoxyphenoxy)methyl)-4-isopropylmorpholine Drug Info [42]
2-(1,4'-bipiperidin-1'-yl)thiazolo[4,5-b]pyridine Drug Info [43]
2-(1,4'-bipiperidin-1'-yl)thiazolo[4,5-c]pyridine Drug Info [43]
2-(1H-Imidazol-4-yl)-cyclopropylamine Drug Info [44]
2-(2-(4-tert-Butylphenylthio)ethyl)-1H-imidazole Drug Info [41]
2-(2-(pyrrolidin-1-yl)ethyl)-1H-indole Drug Info [35]
2-(2-(pyrrolidin-1-yl)ethyl)phenol Drug Info [35]
2-(2-(pyrrolidin-1-yl)ethyl)pyridine Drug Info [35]
2-(3-Methyl-3H-imidazol-4-yl)-ethylamine Drug Info [45]
2-(4-Cyclopentyl-piperazin-1-yl)-quinoline Drug Info [46]
2-(4-Cyclopropyl-piperazin-1-yl)-quinoline Drug Info [46]
2-(4-Isopropyl-piperazin-1-yl)-quinoline Drug Info [46]
2-(4-Methyl-piperazin-1-yl)-quinoline Drug Info [46]
2-(4-Propyl-piperazin-1-yl)-quinoline Drug Info [46]
2-(ethoxycarbonyl)-1H-indole-5-carboxylic acid Drug Info [47]
2-[2-(1H-Imidazol-4-yl)-cyclopropyl]-ethylamine Drug Info [44]
2-[4-(1-Ethyl-propyl)-piperazin-1-yl]-quinoline Drug Info [46]
3-((1H-imidazol-4-yl)methyl)pyridine Drug Info [41]
4-((1H-imidazol-4-yl)methyl)-1-heptylpiperidine Drug Info [48]
4-((1H-Imidazol-4-yl)methyl)-1-phenylpiperidine Drug Info [49]
4-((2R,3S)-2-Methyl-pyrrolidin-3-yl)-1H-imidazole Drug Info [34]
4-((2S,3R)-2-Methyl-pyrrolidin-3-yl)-1H-imidazole Drug Info [34]
4-(2-(3,4-Dimethylphenylamino)ethyl)-1H-imidazole Drug Info [50]
4-(2-(3-tert-Butylphenylamino)ethyl)-1H-imidazole Drug Info [50]
4-(2-(4-Cyclohexylphenylamino)ethyl)-1H-imidazole Drug Info [50]
4-(2-(4-Methoxyphenylamino)ethyl)-1H-imidazole Drug Info [50]
4-(2-(4-Methylphenylamino)ethyl)-1H-imidazole Drug Info [50]
4-(2-(4-tert-Butylphenylamino)ethyl)-1H-imidazole Drug Info [50]
4-(2-(Cyclohexylamino)ethyl)-1H-imidazole Drug Info [50]
4-(2-(Phenylamino)ethyl)-1H-imidazole Drug Info [50]
4-(2-(pyrrolidin-1-yl)ethyl)pyridine Drug Info [35]
4-(3-Phenoxy-propyl)-1H-imidazole Drug Info [51]
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one Drug Info [52]
4-(4-Phenyl-butyl)-1H-imidazole Drug Info [51]
4-(6-Cyclohexyl-hex-3-ynyl)-1H-imidazole Drug Info [45]
4-(6-Cyclopentyl-hex-3-ynyl)-1H-imidazole Drug Info [45]
4-(7,7-Dimethyl-oct-3-ynyl)-1H-imidazole Drug Info [45]
4-(7-Methyl-oct-3-ynyl)-1H-imidazole Drug Info [45]
4-(8-Phenyl-oct-3-ynyl)-1H-imidazole Drug Info [45]
4-Benzyl-1-[3-phenylpropoxy)propyl]piperidine Drug Info [39]
4-Butyl-1-[3-(phenylpropoxy)propyl]piperidine Drug Info [39]
4-Hept-3-ynyl-1H-imidazole Drug Info [45]
4-Hex-3-ynyl-1H-imidazole Drug Info [45]
4-isopropyl-2-(phenoxymethyl)morpholine Drug Info [42]
4-Propyl-1-[3-(phenylpropoxy)propyl]piperidine Drug Info [39]
4-[3-(4-Butyl-phenoxy)-propyl]-1H-imidazole Drug Info [53]
4-[3-(4-Ethynyl-phenoxy)-propyl]-1H-imidazole Drug Info [53]
4-[3-(4-Methoxy-phenoxy)-propyl]-1H-imidazole Drug Info [51]
5-(2-(pyrrolidin-1-yl)ethyl)isothiazole Drug Info [35]
5-ethyl-2-(2-(pyrrolidin-1-yl)ethyl)pyridine Drug Info [35]
5-methoxy-2-(2-(pyrrolidin-1-yl)ethyl)-1H-indole Drug Info [35]
5-phenyl-2-(4-(piperidin-1-yl)butyl)oxazole Drug Info [54]
Aerophobin-1 Drug Info [55]
APLYSAMINE Drug Info [56]
C-[2-(1H-Imidazol-4-yl)-cyclopropyl]-methylamine Drug Info [44]
CARCININE Drug Info [56]
CONESSINE Drug Info [57]
Des-bromoaplysamine-1 Drug Info [58]
GR-175737 Drug Info [45]
GT-2016 Drug Info [45]
IODOPROXYFAN Drug Info [51]
JNJ-28583867 Drug Info [59]
N-benzyl-4-cyclopentylpiperazine-1-carboxamide Drug Info [60]
N-methyl-2-(pyridin-2-yl)ethanamine Drug Info [47]
ST-1025 Drug Info [54]
ST-1093 Drug Info [54]
UCL-2138 Drug Info [40]
VERONGAMINE Drug Info [55]
VUF-10214 Drug Info [61]
VUF-5296 Drug Info [44]
VUF-5297 Drug Info [44]
Agonist (R)-alpha-methylhistamine Drug Info [62], [12]
(S)-alpha-methylhistamine Drug Info [63]
GT-2203 Drug Info [64]
H3 receptor inverse agonists Drug Info [64]
imbutamine Drug Info [65]
Imetit Drug Info [12]
Immepip Drug Info [12]
Immethridine Drug Info [12]
impentamine Drug Info [65]
impromidine Drug Info [66]
Methimepip Drug Info [12]
MK-0249 Drug Info [67]
MK-3134 Drug Info [68]
MK-7288 Drug Info [69]
N-methylhistamine Drug Info [66]
N-[3H]alpha-methylhistamine Drug Info [70]
N-[3H]methylhistamine Drug Info [66]
Pitolisant Drug Info [71]
VUF 5207 Drug Info [72]
VUF 8328 Drug Info [72]
[3H](R)-alpha-methylhistamine Drug Info [66]
Antagonist A-304121 Drug Info [73]
A-317920 Drug Info [12]
A-331440 Drug Info [12]
ABT-239 Drug Info [12], [74], [75]
APD-916 Drug Info [76]
ATH-90879 Drug Info [64]
AZD-5213 Drug Info [77]
Bavisant Drug Info [78]
burimamide Drug Info [66]
Ciproxifan Drug Info [12]
Clobenpropit Drug Info [79], [12]
EVT-501 Drug Info [64]
FUB 349 Drug Info [80]
FUB-130 Drug Info [64]
GSK-334429 Drug Info [64]
GSK1004723 Drug Info [81]
GSK189254A Drug Info [12]
GSK239512 Drug Info [81]
GSK835726 Drug Info [81]
GT2394 Drug Info [63]
HPP404 Drug Info [15]
Irdabisant Drug Info [82]
JB 98064 Drug Info [63]
JNJ-17216498 Drug Info [83]
JNJ-39220675 Drug Info [84]
JNJ-5207852 Drug Info [12]
PF-3900422 Drug Info [64]
Proxyfan Drug Info [12]
S-38093 Drug Info [85]
SAR-110894 Drug Info [77]
SAR-152954 Drug Info [86]
SCH79687 Drug Info [12]
SUVN-G1031 Drug Info [64]
Thioperamide Drug Info [79], [12]
UCB-2892 Drug Info [64]
UCL-1390 Drug Info [21]
UCL1972 Drug Info [12]
VUF 4904 Drug Info [72]
VUF 5681 Drug Info [12]
VUF5391 Drug Info [12]
[123I]iodoproxyfan Drug Info [80]
[125I]iodophenpropit Drug Info [87]
Modulator ABT-288 Drug Info
ABT-652 Drug Info [88]
BP-2.94 Drug Info [89]
Binder Cipralisant Drug Info [90]
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 1ClinicalTrials.gov (NCT01800045) Pitolisant to Assess Weekly Frequency of Cataplexy Attacks and EDS in Narcoleptic Patients (HARMONY CTP). U.S. National Institutes of Health.
REF 2ClinicalTrials.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 3(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 4ClinicalTrials.gov (NCT01207115) A Study of ABT-652 in Adults With Osteoarthritis Pain of the Knee. U.S. National Institutes of Health.
REF 5ClinicalTrials.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 6ClinicalTrials.gov (NCT00566449) A Safety and Effectiveness Study of JNJ-31001074 in Adults With Attention-Deficit/Hyperactivity Disorder.. U.S. National Institutes of Health.
REF 7ClinicalTrials.gov (NCT01772199) Study to Assess Whether GSK239512 Can Remyelinate Lesions in Subjects With Relapsing Remitting Multiple Sclerosis. U.S. National Institutes of Health.
REF 8ClinicalTrials.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 9ClinicalTrials.gov (NCT00804687) An Efficacy Study of JNJ-39220675 and Pseudoephedrine in Participants With Allergic Rhinitis. U.S. National Institutes of Health.
REF 10Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800032202)
REF 11ClinicalTrials.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 12The histamine H3 receptor: from gene cloning to H3 receptor drugs. Nat Rev Drug Discov. 2005 Feb;4(2):107-20.
REF 13(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 14ClinicalTrials.gov (NCT01093508) Single-dose Safety Study of APD916 in Healthy Volunteers. U.S. National Institutes of Health.
REF 15Clinical pipeline report, company report or official report of TransTech Pharma (2011).
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REF 18ClinicalTrials.gov (NCT01092780) Pharmacodynamics and Efficacy of MK7288 (MK-7288-010). U.S. National Institutes of Health.
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REF 20Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008192)
REF 21Emerging drugs for eating disorder treatment. Expert Opin Emerg Drugs. 2006 May;11(2):315-36.
REF 22(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 23Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800028154)
REF 24Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800028155)
REF 25Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800033674)
REF 26(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 27Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007507)
REF 28Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001957)
REF 29Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008938)
REF 30(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 31Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004362)
REF 32Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005172)
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REF 36Bioorg Med Chem Lett. 2009 Dec 1;19(23):6682-5. Epub 2009 Oct 6.Histamine H3 and H4 receptor affinity of branched 3-(1H-imidazol-4-yl)propyl N-alkylcarbamates.
REF 37Bioorg Med Chem Lett. 2010 Jun 1;20(11):3295-300. Epub 2010 Apr 18.In vitro studies on a class of quinoline containing histamine H3 antagonists.
REF 38Bioorg Med Chem. 2009 Apr 15;17(8):3037-42. Epub 2009 Mar 14.Diether derivatives of homo- or substituted piperidines as non-imidazole histamine H3 receptor ligands.
REF 39Bioorg Med Chem. 2008 Sep 15;16(18):8729-36. Epub 2008 Jul 29.Piperidine variations in search for non-imidazole histamine H(3) receptor ligands.
REF 40Bioorg Med Chem Lett. 2009 Apr 15;19(8):2172-5. Epub 2009 Mar 3.Fluorinated non-imidazole histamine H3 receptor antagonists.
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REF 43Bioorg Med Chem Lett. 2009 Nov 1;19(21):6176-80. Epub 2009 Sep 6.Synthesis and structure-activity relationships of 2-(1,4'-bipiperidin-1'-yl)thiazolopyridine as H3 receptor antagonists.
REF 44J 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 45Bioorg Med Chem Lett. 1998 May 19;8(10):1133-8.New acetylene based histamine H3 receptor antagonists derived from the marine natural product verongamine.
REF 46J 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 47J Med Chem. 2009 Jul 9;52(13):3855-68.5-hydroxyindole-2-carboxylic acid amides: novel histamine-3 receptor inverse agonists for the treatment of obesity.
REF 48Bioorg 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 49Synthesis and structure-activity relationships of N-aryl-piperidine derivatives as potent (partial) agonists for human histamine H3 receptor. Bioorg Med Chem. 2010 Jul 15;18(14):5441-8. doi: 10.1016/j.bmc.2010.04.052. Epub 2010 Apr 21.
REF 50J Med Chem. 2010 May 13;53(9):3840-4.Role of hydrophobic substituents on the terminal nitrogen of histamine in receptor binding and agonist activity: development of an orally active histamine type 3 receptor agonist and evaluation of its antistress activity in mice.
REF 51Bioorg Med Chem Lett. 2001 Apr 9;11(7):951-4.Different antagonist binding properties of human and rat histamine H3 receptors.
REF 52J 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 53Bioorg 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 54Bioorg Med Chem Lett. 2010 Oct 1;20(19):5883-6. Epub 2010 Aug 1.Azole derivatives as histamine H3 receptor antagonists, part 2: C-C and C-S coupled heterocycles.
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