Details of the Drug-Related molecule(s) Interaction Atlas

General Information of DTT (ID: TTTIBOJ)

• DTT Name: Histamine H1 receptor (H1R) DTT Info
• Gene Name: HRH1

Molecule-Related Drug & Molecule List

55 Approved Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
(S)-(+)-Dimethindene maleate	DMMHNU2	Pruritus	EC90	Approved	[1]
Aceprometazine	DM1SRQT	Sleep-wake disorder	7A00-7B2Z	Approved	[2]
Acrivastine	DMTIGA0	Allergic rhinitis	CA08.0	Approved	[3]
Alcaftadine	DM5J1NH	Allergic conjunctivitis	9A60.02	Approved	[4]
Antazoline	DMA04JS	Allergic rhinitis	CA08.0	Approved	[5]
Azatadine	DMZ80SB	Allergic rhinitis	CA08.0	Approved	[6]
Azelastine	DMXTMBJ	Allergic conjunctivitis	9A60.02	Approved	[7]
Bepotastine	DMXDZAQ	Allergic rhinitis	CA08.0	Approved	[8]
Bromodiphenhydramine	DMNDJT5	Common cold	CA00	Approved	[9]
Brompheniramine	DMFOVSD	Allergic rhinitis	CA08.0	Approved	[10]
Buclizine	DMXKZT3	Nausea	MD90	Approved	[11]
Carbinoxamine	DMCT31R	Allergic rhinitis	CA08.0	Approved	[12]
Cetirizine	DMOMP9U	Allergic rhinitis	CA08.0	Approved	[13]
Chlophedianol	DMXGJEI	Allergic rhinitis	CA08.0	Approved	[14]
Chlorpheniramine	DM5URA2	Allergic rhinitis	CA08.0	Approved	[7]
Cinnarizine	DM7U5QJ	Meniere disease	AB31.0	Approved	[15]
Clemastine	DMBZWQL	Allergic rhinitis	CA08.0	Approved	[16]
Cyclizine	DM9G7BS	Allergic rhinitis	CA08.0	Approved	[17]
Cyproheptadine	DM92AH3	Allergic rhinitis	CA08.0	Approved	[18]
Desloratadine	DM56YN7	Allergic rhinitis	CA08.0	Approved	[19]
Dexbrompheniramine	DMKVWGE	Allergic rhinitis	CA08.0	Approved	[20]
Dexchlorpheniramine Maleate	DMA8DPN	Allergic rhinitis	CA08.0	Approved	[21]
Dimenhydrinate	DM264B3	Meniere disease	AB31.0	Approved	[22]
Dimethindene	DM32YAI	Respiratory allergy	4A80	Approved	[1]
Diphenhydramine	DMKQTBA	Hyperemesis gravidarum		Approved	[7]
Diphenylpyraline	DMW4X37	Allergic rhinitis	CA08.0	Approved	[23]
Doxepin	DMPI98T	Anxiety		Approved	[24]
Doxylamine	DMKOXFE	Allergic rhinitis	CA08.0	Approved	[25]
Emedastine	DM36LAJ	Allergic conjunctivitis	9A60.02	Approved	[26]
Epinastine	DMX0K3Q	Allergic conjunctivitis	9A60.02	Approved	[27]
Ergotidine	DM78IME	Osteoarthritis	FA00-FA05	Approved	[28]
Ethopropazine	DM0N3L7	Parkinson disease	8A00.0	Approved	[21]
Fexofenadine	DM17ONX	Allergic rhinitis	CA08.0	Approved	[29]
Hydroxyzine	DMF8Y74	Allergic rhinitis	CA08.0	Approved	[30]
Ketotifen	DM74XKS	Allergic conjunctivitis	9A60.02	Approved	[7]
Levocabastine	DMMZPWT	Allergic conjunctivitis	9A60.02	Approved	[31]
Levocetirizine dihydrochloride	DMW6ZJI	Allergic rhinitis	CA08.0	Approved	[29]
Loratadine	DMF3AN7	Allergy	4A80-4A85	Approved	[32]
Mepyramine	DMB4SFH	Allergic rhinitis	CA08.0	Approved	[33]
Mepyramine maleate	DM7F5OW	Allergy	4A80-4A85	Approved	[33]
Mequitazine	DMAFBCY	Allergic rhinitis	CA08.0	Approved	[34]
Methdilazine	DMAUHQX	Allergic rhinitis	CA08.0	Approved	[35]
Mizolastine	DM1FDN8	Allergic rhinitis	CA08.0	Approved	[36]
Olopatadine	DMKMWQG	Allergic conjunctivitis	9A60.02	Approved	[37]
Oxatomide	DM1F42Z	Hay fever	CA08.00	Approved	[7]
Pemirolast	DML97WV	Allergic conjunctivitis	9A60.02	Approved	[38]
Phenindamine	DMDTC7R	Allergic rhinitis	CA08.0	Approved	[39]
Pheniramine	DMCH7RU	Allergic rhinitis	CA08.0	Approved	[40]
Promethazine	DM6I5GR	Hyperemesis gravidarum		Approved	[7]
Propiomazine	DMKY8V1	Insomnia	7A00-7A0Z	Approved	[41]
Tranilast	DME5Y64	Allergic rhinitis	CA08.0	Approved	[37]
Trimeprazine	DMEMV9D	Allergic rhinitis	CA08.0	Approved	[42]
Tripelennamine	DMZBU15	Allergic rhinitis	CA08.0	Approved	[43]
Triprolidine	DM7SWIA	Allergic rhinitis	CA08.0	Approved	[44]
RUPATADINE	DMBPN7T	N. A.	N. A.	Phase 4	[45]

9 Clinical Trial Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
AC-170	DMXZ9T3	Allergic conjunctivitis	9A60.02	Phase 3	[46]
Carebastine	DMUVMWZ	Ocular allergy	4A81	Phase 3	[37]
E-4716	DMC5PB2	Respiratory disease	CB40	Phase 2	[47]
LY-2624803	DMTPQUA	Insomnia	7A00-7A0Z	Phase 2	[48]
Noberastine	DME8IFQ	Asthma	CA23	Phase 2	[49]
OBE-101	DMJIBSG	Obesity	5B81	Phase 2	[50]
RP5063	DMKUE8O	Schizophrenia	6A20	Phase 2	[51]
UCB-35440	DM5Z34K	Rhinitis	FA20	Phase 2	[52]
Vapitadine	DMNFVKC	Allergic skin disorder	4A82	Phase 2	[53]

3 Patented Agent(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Citalopram derivative 1	DMITX1G	N. A.	N. A.	Patented	[54]
Piperidine derivative 1	DMHN5KW	N. A.	N. A.	Patented	[54]
PMID29334795-Compound-61	DM9H3LI	N. A.	N. A.	Patented	[54]

12 Discontinued Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Astemizole	DM2HN6Q	Allergic rhinitis	CA08.0	Withdrawn from market	[55]
Terfenadine	DM4KLPT	Allergy	4A80-4A85	Withdrawn from market	[56]
Norastemizole	DMXF0NS	N. A.	N. A.	Discontinued in Preregistration	[57]
GSK835726	DMRNJPY	Allergic rhinitis	CA08.0	Discontinued in Phase 2	[58]
HSR-609	DM1PJ0V	Rhinitis	FA20	Discontinued in Phase 2	[59]
Mequitamium iodide	DM2DK4A	Asthma	CA23	Discontinued in Phase 2	[60]
ReN-1869	DMHCBQS	Pain	MG30-MG3Z	Discontinued in Phase 2	[61]
SUN-1334H	DMWTLQ4	Allergic rhinitis	CA08.0	Discontinued in Phase 2	[62]
AZD-1744	DMCOMG5	Asthma	CA23	Discontinued in Phase 1	[63]
GSK1004723	DMEC6RD	Allergic rhinitis	CA08.0	Discontinued in Phase 1	[58]
KA-398	DM0MXWC	Asthma	CA23	Terminated	[64]
Selenotifen	DM4ESAP	Asthma	CA23	Terminated	[65]

47 Investigative Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
(+)-cis-H2-PAT	DMDFR59	Discovery agent	N.A.	Investigative	[66]
(+)-trans-H2-PAT	DMAN63P	Discovery agent	N.A.	Investigative	[66]
(+/-)-cis-H2-PAT	DMAHO9M	Discovery agent	N.A.	Investigative	[66]
(-)-trans-H2-PAT	DMITWZ7	Discovery agent	N.A.	Investigative	[66]
(S)-cetirizine	DMJN659	Discovery agent	N.A.	Investigative	[67]
1-(4-p-Tolyl-butyl)-piperidine	DMFYK6T	Discovery agent	N.A.	Investigative	[68]
1-[(Furan-2(5H)-one)-4-methyl]-desloratadine	DMQPFT3	Discovery agent	N.A.	Investigative	[69]
2-(2-thiazolyl)ethanamine	DMRL65E	Discovery agent	N.A.	Investigative	[70]
2-(3-bromophenyl)histamine	DM260RG	Discovery agent	N.A.	Investigative	[70]
2-(3-chlorophenyl)histamine	DMO0Y79	Discovery agent	N.A.	Investigative	[70]
2-(3-iodophenyl)histamine	DMML0VP	Discovery agent	N.A.	Investigative	[70]
2-(9,10-dihydroanthracen-9-yl)-N-methylethanamine	DMRW475	Discovery agent	N.A.	Investigative	[71]
2-pyridylethylamine	DMN516S	Discovery agent	N.A.	Investigative	[67]
3,3-diphenylpropan-1-amine	DMNOUSV	Discovery agent	N.A.	Investigative	[71]
4,4-Diphenylbutan-1-amine	DMQ0TBX	Discovery agent	N.A.	Investigative	[71]
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one	DMM9X0G	Discovery agent	N.A.	Investigative	[72]
8R-Lisuride	DMLK4WO	Discovery agent	N.A.	Investigative	[73]
9-(2-aminoethyl)-9,10-dihydroanthracene	DM4Y9U3	Discovery agent	N.A.	Investigative	[71]
9-(2-aminopropyl)-9,10-dihydroanthracene	DMND39P	Discovery agent	N.A.	Investigative	[71]
9-(Aminomethyl)-9,10-dihydroanthracene	DM6QDNH	Discovery agent	N.A.	Investigative	[71]
9-OH-risperidone	DMGORXQ	Discovery agent	N.A.	Investigative	[74]
9-Phenyl-2,3-dihydro-1H-indeno[2,1-c]pyridine	DMRCM7Q	Discovery agent	N.A.	Investigative	[75]
arpromidine	DMB9PDA	Discovery agent	N.A.	Investigative	[70]
BU-E 47	DM1D47I	Discovery agent	N.A.	Investigative	[70]
DIMEBOLIN	DMV8ZQG	Discovery agent	N.A.	Investigative	[76]
dimethylhistaprodifen	DMY0FVU	Discovery agent	N.A.	Investigative	[70]
Diphenyl(piperidin-4-yl)methanol	DMO4XUC	Discovery agent	N.A.	Investigative	[68]
histaprodifen	DMA9YIB	Discovery agent	N.A.	Investigative	[77]
Hydroxyclemastine	DM5DOEC	Discovery agent	N.A.	Investigative	[16]
impromidine	DMTDRPM	Discovery agent	N.A.	Investigative	[78]
KF-A6	DMQJ3T5	Discovery agent	N.A.	Investigative	[79]
MDL-28163	DMUHJ2C	Discovery agent	N.A.	Investigative	[45]
methylhistaprodifen	DM7PRDY	Discovery agent	N.A.	Investigative	[70]
N,N-dimethyl-2,2-diphenylethanamine	DMJDQGR	Discovery agent	N.A.	Investigative	[71]
N,N-Dimethyl-3,3-diphenylpropan-1-amine	DMIP5K7	Discovery agent	N.A.	Investigative	[71]
N,N-dimethyl-4,4-diphenylbutan-1-amine	DMX9U7S	Discovery agent	N.A.	Investigative	[71]
N-methyl-3,3-diphenylpropan-1-amine	DM8IHQP	Discovery agent	N.A.	Investigative	[71]
N-methyl-4,4-diphenylbutan-1-amine	DMO3PNF	Discovery agent	N.A.	Investigative	[71]
OCTOCLOTHEPIN	DM0UADK	Discovery agent	N.A.	Investigative	[80]
oxo-arpromidine	DMV0KTW	Discovery agent	N.A.	Investigative	[78]
R-226161	DM4BP7S	Discovery agent	N.A.	Investigative	[81]
R-dimethindene	DM6FVZW	Discovery agent	N.A.	Investigative	[82]
UR-PG131A	DM2C6GB	Discovery agent	N.A.	Investigative	[78]
UR-PG146	DMQCL6Y	Discovery agent	N.A.	Investigative	[78]
UR-PG153	DM3VTLG	Discovery agent	N.A.	Investigative	[78]
UR-PG55B	DM6SM4N	Discovery agent	N.A.	Investigative	[78]
VUF-10148	DM89PMC	Discovery agent	N.A.	Investigative	[83]

References

• [1] Analytical 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.
• [2] Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34.
• [3] Clinical pharmacology of new histamine H1 receptor antagonists. Clin Pharmacokinet. 1999 May;36(5):329-52.
• [4] Mullard A: 2010 FDA drug approvals. Nat Rev Drug Discov. 2011 Feb;10(2):82-5.
• [5] Histamine and the convulsive threshold or effectiveness of antiepileptic drugs. Przegl Lek. 2008;65(11):803-6.
• [6] Comparative effects of loratadine and azatadine in the treatment of seasonal allergic rhinitis. Asian Pac J Allergy Immunol. 1990 Dec;8(2):103-7.
• [7] Intact 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.
• [8] Mast cells play a critical role in the pathogenesis of viral myocarditis. Circulation. 2008 Jul 22;118(4):363-72.
• [9] Studies on synergism between penicillins and ambodryl (bromodiphenhydramine HCl), an antihistamine with antimicrobial property. Indian J Exp Biol. 1990 Mar;28(3):253-8.
• [10] Histamine-induced venodilation in human beings involves both H1 and H2 receptor subtypes. J Allergy Clin Immunol. 1994 Mar;93(3):606-14.
• [11] Toxicologic and clinical appraisal of buclizine, a new antihistaminic compound. J Allergy. 1956 Jan;27(1):63-7.
• [12] Comparison 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.
• [13] Design, 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.
• [14] Identification 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.
• [15] Central effects of cinnarizine: restricted use in aircrew. Aviat Space Environ Med. 2002 Jun;73(6):570-4.
• [16] Histamine upregulates keratinocyte MMP-9 production via the histamine H1 receptor. J Invest Dermatol. 2008 Dec;128(12):2783-91.
• [17] Histamine 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.
• [18] Cyproheptadine displays preclinical activity in myeloma and leukemia. Blood. 2008 Aug 1;112(3):760-9.
• [19] Examining the tolerability of the non-sedating antihistamine desloratadine: a prescription-event monitoring study in England. Drug Saf. 2009;32(2):169-79.
• [20] H2 histaminergic control of inhibition of eating induced by intragastric NaCl in rats. Physiol Behav. 1998 Aug;65(1):105-13.
• [21] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
• [22] Histamine 1 receptor antagonist in symptomatic treatment of renal colic accompanied by nausea: two birds with one stone Urology. 2009 Jan;73(1):32-6.
• [23] Transport 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.
• [24] Novel therapeutic usage of low-dose doxepin hydrochloride. Expert Opin Investig Drugs. 2007 Aug;16(8):1295-305.
• [25] First-generation H1 antihistamines found in pilot fatalities of civil aviation accidents, 1990-2005. Aviat Space Environ Med. 2007 May;78(5):514-22.
• [26] Emedastine difumarate: a review of its potential ameliorating effect for tissue remodeling in allergic diseases. Expert Opin Pharmacother. 2009 Aug;10(11):1859-67.
• [27] Influence of epinastine hydrochloride, an H1-receptor antagonist, on the function of mite allergen-pulsed murine bone marrow-derived dendritic cell... Mediators Inflamm. 2009;2009:738038.
• [28] Cloning and pharmacological characterization of a fourth histamine receptor (H(4)) expressed in bone marrow. Mol Pharmacol. 2001 Mar;59(3):420-6.
• [29] Update on prescription and over-the-counter histamine inverse agonists in rhinitis therapy. Curr Allergy Asthma Rep. 2009 Mar;9(2):140-8.
• [30] Hydroxyzine, a first generation H(1)-receptor antagonist, inhibits human ether-a-go-go-related gene (HERG) current and causes syncope in a patient ... J Pharmacol Sci. 2008 Dec;108(4):462-71.
• [31] Contribution of alpha4beta1 integrin to the antiallergic effect of levocabastine. Biochem Pharmacol. 2008 Sep 15;76(6):751-62.
• [32] Clinical 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.
• [33] Antinociception induced by central administration of histamine in the formalin test in rats. Indian J Physiol Pharmacol. 2008 Jul-Sep;52(3):249-54.
• [34] Efficiency 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.
• [35] Effect of H1 blockers alone and in combination with morphine to produce antinociception in mice. Neuropharmacology. 1985 Jan;24(1):1-4.
• [36] Histamine 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.
• [37] Emerging drugs for ocular allergy. Expert Opin Emerg Drugs. 2005 Aug;10(3):505-20.
• [38] The 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.
• [39] The 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.
• [40] Role of central histaminergic system in lorazepam withdrawal syndrome in rats. Pharmacol Biochem Behav. 2001 Apr;68(4):777-82.
• [41] How many drug targets are there Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
• [42] Effectiveness of alimemazine in controlling retching after Nissen fundoplication. J Pediatr Surg. 2005 Nov;40(11):1737-40.
• [43] Involvement 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.
• [44] Histamine excites rat lateral vestibular nuclear neurons through activation of post-synaptic H2 receptors. Neurosci Lett. 2008 Dec 19;448(1):15-9.
• [45] Designed multiple ligands. An emerging drug discovery paradigm. J Med Chem. 2005 Oct 20;48(21):6523-43.
• [46] Clinical pipeline report, company report or official report of NicOx SA.
• [47] Population pharmacokinetics of epinastine, a histamine H1 receptor antagonist, in adults and children. Br J Clin Pharmacol. 2005 Jan;59(1):43-53.
• [48] Current Phase II investigational therapies for insomnia. Expert Opin Investig Drugs. 2015 Mar;24(3):401-11.
• [49] A double-blind placebo controlled dose response study of noberastine on histamine induced weal and flare. Eur J Clin Pharmacol. 1991;40(1):83-5.
• [50] Betahistine in the treatment of M ni re's disease. Neuropsychiatr Dis Treat. 2007 August; 3(4): 429-440.
• [51] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [52] The effect of a novel, dual function histamine H1 receptor antagonist/5-lipoxygenase enzyme inhibitor on in vivo dermal inflammation and extravasat... Eur J Pharmacol. 2005 Jan 4;506(3):265-71.
• [53] Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800020866)
• [54] Progress in the development of histamine H3 receptor antagonists/inverse agonists: a patent review (2013-2017).Expert Opin Ther Pat. 2018 Mar;28(3):175-196.
• [55] Histamine H1 receptor induces cytosolic calcium increase and aquaporin translocation in human salivary gland cells. J Pharmacol Exp Ther. 2009 Aug;330(2):403-12.
• [56] Small 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.
• [57] Effect of tecastemizole on pulmonary and cutaneous allergic inflammatory responses. Clin Exp Allergy. 2007 Jun;37(6):909-17.
• [58] Clinical pipeline report, company report or official report of GlaxoSmithKline (2009).
• [59] Studies 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.
• [60] High-affinity binding of mequitamium iodide (LG 30435) to muscarinic and histamine H1 receptors. Eur J Pharmacol. 1990 Jul 17;182(3):413-20.
• [61] ReN 1869, a novel tricyclic antihistamine, is active against neurogenic pain and inflammation. Eur J Pharmacol. 2002 Jan 18;435(1):43-57.
• [62] Preclinical efficacy and safety pharmacology of SUN-1334H, a potent orally active antihistamine agent. Drugs R D. 2008;9(2):93-112.
• [63] Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.
• [64] URL: 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).
• [65] Effect 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.
• [66] A novel phenylaminotetralin radioligand reveals a subpopulation of histamine H(1) receptors. J Pharmacol Exp Ther. 2002 Jul;302(1):328-36.
• [67] Large-scale overproduction, functional purification and ligand affinities of the His-tagged human histamine H1 receptor. Eur J Biochem. 2004 Jul;271(13):2636-46.
• [68] Structural determinants for histamine H(1) affinity, hERG affinity and QTc prolongation in a series of terfenadine analogs. Bioorg Med Chem Lett. 2009 Sep 1;19(17):5043-7.
• [69] Stereoselective synthesis of desloratadine derivatives as antagonist of histamine. Bioorg Med Chem. 2010 Feb 15;18(4):1626-32.
• [70] Multiple differences in agonist and antagonist pharmacology between human and guinea pig histamine H1-receptor. J Pharmacol Exp Ther. 2003 Jun;305(3):1104-15.
• [71] Synthesis, structure-affinity relationships, and modeling of AMDA analogs at 5-HT2A and H1 receptors: structural factors contributing to selectivity. Bioorg Med Chem. 2009 Sep 15;17(18):6496-504.
• [72] 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 rec... J Med Chem. 2010 Sep 9;53(17):6386-97.
• [73] 8R-lisuride is a potent stereospecific histamine H1-receptor partial agonist. Mol Pharmacol. 2004 Mar;65(3):538-49.
• [74] Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding. Psychopharmacology (Berl). 1996 Mar;124(1-2):57-73.
• [75] Conformationally-restricted ligands for the histamine H1 receptor. Bioorg Med Chem Lett. 2000 Jun 5;10(11):1277-9.
• [76] Synthesis and biological activity of 5-styryl and 5-phenethyl-substituted 2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indoles. Bioorg Med Chem Lett. 2010 Jan 1;20(1):78-82.
• [77] Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first pote... J Pharmacol Exp Ther. 2005 Sep;314(3):1310-21.
• [78] Probing ligand-specific histamine H1- and H2-receptor conformations with NG-acylated Imidazolylpropylguanidines. J Pharmacol Exp Ther. 2006 Apr;317(1):139-46.
• [79] Design, synthesis, and evaluation of 10-N-substituted acridones as novel chemosensitizers in Plasmodium falciparum. Antimicrob Agents Chemother. 2007 Nov;51(11):4133-40.
• [80] Exploring the neuroleptic substituent in octoclothepin: potential ligands for positron emission tomography with subnanomolar affinity for (1)-adre... J Med Chem. 2010 Oct 14;53(19):7021-34.
• [81] Tricyclic isoxazolines: identification of R226161 as a potential new antidepressant that combines potent serotonin reuptake inhibition and alpha2-a... Bioorg Med Chem. 2007 Jun 1;15(11):3649-60.
• [82] Characterization of novel selective H1-antihistamines for clinical evaluation in the treatment of insomnia. J Med Chem. 2009 Sep 10;52(17):5307-10.
• [83] Fragment based design of new H4 receptor-ligands with anti-inflammatory properties in vivo. J Med Chem. 2008 Apr 24;51(8):2457-67.