Contribution of active and inactive states of the human 5-HT4d receptor to the functional activities of 5-HT4-receptor agonists

Journal of Pharmacological Sciences

Volumn 107, Issue 3, 2008, Pages 251-259

  Mikami, Tadayoshi ^a   Sugimoto, Hiromi ^a   Naganeo, Rie ^a   Ohmi, Takashi ^a   Saito, Toshiyuki ^a   Eda, Hiroyuki ^a  

^a PFIZER INC   (United States)

Author keywords

5 hydroxytryptamine 4 (5 HT4) receptor; Agonist; Antagonist; GR113808; Serotonin

Indexed keywords

1 (4 AMINO 5 CHLORO 2 METHOXYPHENYL) 3 (1 BUTYL 4 PIPERIDINYL) 1 PROPANONE; 1 (4 AMINO 5 CHLORO 2 METHOXYPHENYL) 3 [1 [2 (METHANESULFONAMIDO)ETHYL] 4 PIPERIDINYL] 1 PROPANONE; 1 METHYL 3 INDOLECARBOXYLIC ACID [1 [2 (METHYLSULFONYLAMINO)ETHYL] 4 PIPERIDINYLMETHYL] ESTER; 5 FLUORO 2 METHOXY 1H INDOLE 3 CARBOXYLIC ACID 1 [2 (METHYLSULFONAMIDO)ETHYL] 4 PIPERIDINYLMETHYL ESTER; 5 METHOXYTRYPTAMINE; 8 AMINO 7 CHLORO 1,4 BENZODIOXAN 5 CARBOXYLIC ACID 1 BUTYL 4 PIPERIDINYLMETHYL ESTER; CISAPRIDE; GUANOSINE 5' O (3 THIOTRIPHOSPHATE); MOSAPRIDE CITRATE; SEROTONIN 4 AGONIST; SEROTONIN 4 RECEPTOR; SEROTONIN 4D RECEPTOR; TEGASEROD; TRITIUM;

ARTICLE; BINDING AFFINITY; BINDING SITE; DRUG EFFICACY; DRUG MECHANISM; DRUG RECEPTOR BINDING; HUMAN; HUMAN CELL; RADIOASSAY;

EID: 47749097152     PISSN: 13478613     EISSN: 13478648     Source Type: Journal    
DOI: 10.1254/jphs.FP0072230     Document Type: Article

References (26)

1. 4 receptors. FASEB J. 1996;10:1398-1407.
2. 4 receptor: molecular cloning and pharmaco logical characterization of two splice variants. EMBO J. 1995; 14:2806-2815.
3. 4 receptor. Eur J Pharmacol. 1996;304:231-235.
4. 4 receptors. Current Drug Targets CNS & Neurological Disorders. 2004;3: 39-51.
5. 4 receptor isoforms produced by alternative splicing in the carboxyl terminus. J Neurochem. 1998;70:2252-2261.
6. 4 receptors in the human and guinea-pig brain. Neuroreport. 1993;4:1239-1242.
7. 2A receptor with an agonist, a partial agonist and an antagonist: effects on apparent agonist affinities. Biochem Pharmacol. 1996;51:71-76.
8. Kearn CS, Greenberg MJ, DiCamelli R, Kurzawa K, Hillard CJ. Relationships between ligand affinities for the cerebellar cannabinoid receptor CB1 and the induction of GDP/GTP exchange. J Neurochem. 1999;72:2379-2387.
9. 2 dopamine receptors. Biochem Pharmacol. 2004;67:1657-1665.
10. De Lean A, Stadel JM, Lefkowitz RJ. A ternary complex model explains the agonist-specific binding properties of the adenylate cyclase-coupled β-adrenergic receptor. J Biol Chem. 1980;255: 7108-7117.
11. 4 splice variant. J Neurochem. 2000;74:478-489.
12. 4 receptor splice variants: compound specificity and dual coupling with Gαs- and Gαi/o-proteins. Mol Pharmacol. 2002;61:85-96.
13. Christopoulos A, Kenakin T. G protein-coupled receptor allosterism and complexing. Pharmacol Rev. 2002;54:323-374.
14. 4 receptor splice variants show marked constitutive activity: role of the C-terminal intracellular domain. Mol Pharmacol. 1999;55:910-920.
15. 4(d) receptor splice variant stably expressed in Chinese hamster ovary cells. Br J Pharmacol. 2000;131:827-835.
16. 4 receptor: a structural basis for drug efficacy. J Biol Chem. 2005;280:20253-20260.
17. Leff P. The two-state model of receptor activation. Trends Pharmacol Sci. 1995;16:89-97.
18. 4(e) receptor from human heart and comparative analysis of its pharmacological profile in C6-glial and CHO cell lines. Br J Pharmacol. 2000;129:771-781.
19. 4(d) receptors have nearly identical pharmacology and are both expressed in human atrium and ventricle. Naunyn Schmiedebergs Arch Pharmacol. 2001; 363:146-160.
20. 4(i). Naunyn Schmiedebergs Arch Pharmacol. 2004;369: 616-628.
21. 4 receptor antagonists on constitutively active wild-type and mutated receptors. Mol Pharmacol. 2000;58:136-144.
22. 4(c) receptor. Br J Pharmacol. 1998;125: 595-597.
23. 2C receptors: evidence favoring the ternary complex and two-state models of agonist action. J Neurochem. 1999; 72:2127-2134.
24. 1A receptor agonist-antagonist binding affinity difference as a measure of intrinsic activity in recombinant and native tissue systems. Br J Pharmacol. 2000;130:1108-1114.
25. 2C receptors. Synapse. 2000;35:144-150.
26. 2 receptor. Eur J Pharmacol. 1998;346:299-307.