Cloning of rat histamine H3 receptor reveals distinct species pharmacological profiles

Journal of Pharmacology and Experimental Therapeutics

Volumn 293, Issue 3, 2000, Pages 771-778

  Lovenberg, Timothy W ^a   Pyati, Jayashree ^a   Chang, Hong ^a   Wilson, Sandy J ^a   Erlander, Mark G ^a  

^a JOHNSON AND JOHNSON PHARMACEUTICAL RESEARCH AND DEVELOPMENT   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

CLOBENPROPIT; HISTAMINE H3 RECEPTOR; THIOPERAMIDE;

ARTICLE; CENTRAL NERVOUS SYSTEM; DRUG EFFECT; DRUG SCREENING; MOLECULAR CLONING; NONHUMAN; PRIORITY JOURNAL; PROTEIN TRANSPORT; RAT;

ADENYLATE CYCLASE; AMINO ACID SEQUENCE; ANIMALS; CLONING, MOLECULAR; DOSE-RESPONSE RELATIONSHIP, DRUG; HUMANS; METHYLHISTAMINES; MOLECULAR SEQUENCE DATA; RATS; RECEPTORS, HISTAMINE H3; RECOMBINANT PROTEINS; RNA, MESSENGER;

EID: 0034047202     PISSN: 00223565     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article

References (31)

1. Arrang JM, Garbarg M and Schwartz JC (1983) Autoinhibition of brain histamine release mediated by a novel class (H3) of histamine receptor. Nature (Lond) 302:832-837.
2. Beck-Sickinger AG (1996) Structural characterization and binding sites of G-protein-coupled receptors. Drug Discov Today 1:502-513.
3. Boess FG, Monsma FJ Jr and Sleight AJ (1998) Identification of residues in transmembrane regions III and VI that contribute to the ligand binding site of the serotonin 5-HT6 receptor. J Neurochem 71:2169-2177.
4. Cardell LO and Edvinsson L (1994) Characterization of the histamine receptors in the guinea-pig lung: Evidence for relaxant histamine H3 receptors in the trachea. Br J Pharmacol 111:445-454.
5. Cheng Y-C and Prusoff WH (1973) Relation between the inhibition constant K1 and the concentration of inhibitor which causes fifty per cent inhibition (I50) of an enzymic reaction. Biochem Pharmacol 22:3099-3108.
6. Cherifi Y, Pigeon C, Le Romancer M, Bado A, Reyl-Desmars F and Lewin MJM (1992) Purification of a histamine H3 receptor negatively coupled to phosphoinositide turnover in the human gastric cell line HGT1. J Biol Chem 267:25315-25320.
7. Coruzzi G, Poli E, Giuseppina M and Bertaccini G (2000) The histamine H3 receptor: Pharmacotherapy targets in gastrointestinal disorders. Drug Dev 239-267.
8. Dimitriadou V, Rouleau A, Dam Trung Tuong M, Newlands GJF, Miller HRP, Luffau G, Schwartz J-C and Garbarg M (1994) Functional relationship between mast cells and C-sensitive nerve fibers evidenced by histamine H3-receptor modulation in the rat lung and spleen. Clin Sci 87:151-163.
9. Gros J, Manning BS, Pietri-Rouxel F, Guillaume J-L, Drumare M-F and Strosberg AD (1998) Site-directed mutagenesis of the human b3-adrenoceptor. Transmembrane residues involved in ligand binding and signal transduction. Eur J Biochem 251:590-596.
10. Harper EA, Shankley NP and Black JW (1999a) Characterization of the binding of [3H]-clobenpropit to histamine H3-receptors in guinea-pig cerebral cortex membranes. Br J Pharmacol 128:881-890,
11. Harper EA, Shankley NP and Black JW (1999b) Evidence that histamine homologues discriminate between H3-receptors in guinea-pig cerebral cortex and ileum longitudinal muscle myenteric plexus. Br J Pharmacol 128:751-759.
12. Hill SJ, Ganellin CR, Timmerman H, Schwartz JC, Shankley NP, Young JM, Schunack W, Levi R and Haas HL (1997) International Union of Pharmacology. XIII. Classification of histamine receptors. Pharmacol Rev 49:253-278.
13. Imamura M, Seyedi N, Lander HM and Levi R (1995) Functional identification of histamine H3-receptors in the human heart. Circ Res 77:206-210.
14. Jackson T (1991) Structure and function of G protein coupled receptors. Pharmacoi Ther 50:425-442.
15. Kathmann M, Schlicker E and Goethert M (1994) Intermediate affinity and potency of clozapine and low affinity of other neuroleptics and of antidepressants at H3 receptors. Psychopharmacology 116:464-468.
16. Langer SZ (1997) 25 Years since the discovery of the presynaptic receptors: Present knowledge and future perspectives. Trends Pharmacol Sci 18:95-99.
17. Lee NH, Pellegrino SM, Fraser CM and Dep M (1994) Site-directed mutagenesis of a-adrenergic receptors. NeuroProtocols 4:20-31.
18. Liggett SB (1999) Molecular and genetic basis of b2-adrenergic receptor function. J Allergy Clin Immunol 104:S42-S46.
19. 125I]Iodoproxyfan, a new antagonist to label and visualize cerebral histamine H3 receptors. J Pharmacol. Exp Ther 271:452-459.
20. Lipman DJ and Pearson WR (1985) Rapid and sensitive protein similarity searches. Science (Wash DC) 227:1435-1441.
21. Lovenberg TW, Roland BL, Wilson SJ, Jiang W, Pyati J, Huvar A, Jackson MR and Erlander MG (1999) Cloning and functional expression of the human histamine H3 receptor. Mol Pharmacol 55:1101-1107.
22. Oike M, Kitamura K and Kuriyama H (1992) Histamine H3-receptor activation augments voltage-dependent calcium current via GTP hydrolysis in rabbit saphenous artery. J Physiol (Lond) 448:133-152.
23. Rodrigues AA, Jansen FP, Leurs R, Timmerman H and Prell GD (1995) Interaction of clozapine with the histamine H3 receptor in rat brain. Br J Pharmacol 114:1523-1524.
24. Sasse A, Stark H, Reidemeister S, Huels A, Elz S, Ligneau X, Ganellin CR, Schwartz J-C and Schunack W (1999) Novel partial agonists for the histamine H3 receptor with high in vitro and in vivo activity. J Med Chem 42:4269-4274.
25. Schild HO (1949) pAx and competitive drug antagonism. Br J Pharmacol 4:277-280.
26. Schlicker E, Kathmann M, Bitschnau H, Marr I, Reidemeister S, Stark H and Schunack W (1996) Potencies of antagonists chemically related to iodoproxyfan at histamine H3 receptors in mouse brain cortex and guinea pig ileum: Evidence for H3 receptor heterogeneity? Naunyn-Sckmiedeberg's Arch Pharmacol 353:482-488.
27. 125I]Iodoproxyfan and related compounds: A reversible radioligand and novel classes of antagonists with high affinity and selectivity for the histamine H3 receptor. J Med Chem 39:1220-1226.
28. Watt GF, Sykes DA, Roberts SP, Shankley NP and Black JW (1997) Estimation of agonist affinity and efficacy parameters of histamine H3-receptor ligands in guinea pig ileum. Br J Pharmacol 122:435.
29. West RE Jr, Wu R-L, Billah MM, Egan RW and Anthes JC (1999) The profiles of human and primate [3H]Na-methylhistamine binding differ from that of rodents. Eur J Pharmacol 377:233-239.
30. West RE Jr, Zweig A, Shih NY, Siegel MI, Egan RW and Clark MA (1990) Identification of two H3-histamine receptor subtypes. Mol Pharmacol 38:610-613.
31. Wieland K, Laak AMT, Smit MJ, Kuhne R, Timmerman H and Leurs R (1999) Mutational analysis of the antagonist-binding site of the histamine H1 receptor. J Biol Chem 274:29994-30000.