Pharmacological characterizations of recombinant human 5-HT(1Dα) and 5-HT(1Dβ) receptor-subtypes coupled to adenylate cyclase inhibition in clonal cell lines: Apparent differences in drug intrinsic efficacies between human 5-HT(1D) subtypes

Naunyn-Schmiedeberg's Archives of Pharmacology

Volumn 354, Issue 3, 1996, Pages 226-236

  Zgombick, John M ^a   Schechter, Lee E ^a,b   Adham, Nika ^a   Kucharewicz, Stefan A ^a   Weinshank, Richard L ^a   Branchek, Theresa A ^a  

^a H LUNDBECK A S   (Denmark)

^b Wyelh Ayerst Research   (United States)

Author keywords

Cyclic AMP inhibition; Intrinsic activity; Intrinsic efficacy; Receptor reserve; Recombinant human 5 HT(1D ) and 5 HT(1D ) subtypes; Serotonin receptors; Stable transfection; Sumatriptan

Indexed keywords

1 [2 (4 AMINOPHENYL)ETHYL] 4 (3 TRIFLUOROMETHYLPHENYL)PIPERAZINE; 1 NAPHTHYLPIPERAZINE; 2 DIPROPYLAMINO 8 HYDROXYTETRALIN; 4 IODO 2,5 DIMETHOXYAMPHETAMINE; 5 CARBAMOYLTRYPTAMINE; CYCLIC AMP; DIHYDROERGOTAMINE; FORSKOLIN; LYSERGIDE; METERGOLINE; METITEPINE; N [4 METHOXY 3 (4 METHYL 1 PIPERAZINYL)PHENYL] 2' METHYL 4' (5 METHYL 1,2,4 OXADIAZOL 3 YL)[1,1' BIPHENYL] 4 CARBOXAMIDE; OXYMETAZOLINE; QUIPAZINE; RAUWOLSCINE; RECEPTOR SUBTYPE; RIZATRIPTAN; SEROTONIN; SEROTONIN 1 RECEPTOR; SEROTONIN 1D ANTAGONIST; SEROTONIN 1D RECEPTOR; SEROTONIN AGONIST; SUMATRIPTAN; UNCLASSIFIED DRUG; YOHIMBINE;

ADRENAL CORTEX TUMOR; ANIMAL CELL; ARTICLE; CELL LINE; CONTROLLED STUDY; DISSOCIATION CONSTANT; DRUG RECEPTOR BINDING; FIBROBLAST; GENE EXPRESSION; GENETIC TRANSFECTION; HUMAN; MOUSE; NONHUMAN; RECEPTOR DENSITY; RECEPTOR OCCUPANCY;

ADENYLATE CYCLASE; BINDING, COMPETITIVE; CELL LINE; CYCLIC AMP; DOSE-RESPONSE RELATIONSHIP, DRUG; FORSKOLIN; GENE EXPRESSION REGULATION; HUMANS; RECEPTORS, SEROTONIN; RECOMBINANT PROTEINS; SEROTONIN AGONISTS; SUMATRIPTAN;

EID: 0029818982     PISSN: 00281298     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article

References (55)

1. 2-adrenergic receptor-mediated contraction of vascular smooth muscle. Circ Res 72:778 785
2. 1Dβ receptor. Mol Pharmacol 41:1-7
3. 1B receptor expression system. Mol Pharmacol 43:427-433
4. 1F receptor to multiple signal transduction pathways. Naunyn-Schmiedeberg's Arch Pharmacol 348:566-575
5. Arunlakshana O, Schild HO (1959) Some quantitative uses of drug antagonists. Br J Pharmacol 14:48-58
6. Bax WA, Renzenbrink GJ, Heuven-Nolsen DV. Thijssen EJM, Bos E, Saxena PR (1993) 5-HT receptors mediating contractions of the isolated human coronary artery. Eur J Pharmacol 239: 203-210
7. 1Dβ receptor subtype in human cortex. Eur J Pharmacol 242:195-198
8. 1D receptor agonist. Br J Pharmacol 110: 1196-1200
9. 1D receptor agonist MK-462 (abstract). Third IUPHAR Satellite Meeting on Serotonin, p.105
10. 1A receptors: variations in intrinsic activity studied in transfected HeLa cells. Naunyn-Schmiedebera's Arch Pharmacol 345:257-263
11. Bradford M (1976) A rapid and sensitive method for the quantification of microgram quantities of protein utilizing the principle of protein-dye binding. Anal Biochem 72:248-254
12. 2 receptor. Mol Pharmacol 38:604-609
13. 1D subtypes in heterologous expression systems (abstract). Second International Symposium on Serotonin: From Cell Biology to Pharmacology and Therapeutics, p 10
14. 1B binding sites in rat brain. Naunyn-Schmiedeberc's Arch Pharmacol 347:569-582
15. 1F receptor messenger RNA in rodent and primate brain. Neuropharmacology 33:367-382
16. 1B D receptor ligands. Pharmacol Ther 62: 385-405
17. α subunits that interact with Gβγ, receptors, and effectors. Cell 73:631-641
18. 1Dβ) encoded by an intronless gene on chromosome 6. Proc Natl Acad Sci USA 89:5522-5526
19. 1-like receptors linked to increases in intracellular calcium concentration and inhibition of cyclic AMP accumulation in cultured vascular smooth muscle cells derived from bovine basilar artery. J Pharmacol Exp Ther 266:692-699
20. Furchgott RF, Bursztyn P (1967) Comparison of dissociation constants and relative efficacies of selected agonists acting on parasympathetic receptors. Ann NY Acad Sci 144:882-899
21. 3H]hydroxytryptamine in slices of the human neocortex. J Neurochem 59:1293-1301
22. Göthert M, Fink K, Frölich D, Likungu J, Molderings G, Schlicker E, Zentner J (1996) Presynaptic 5-HT auto- and heteroreceptors in the human central and peripheral nervous system. Behav Brain Res 73:89-92
23. 1D-type scrotonin receptor. Mol Pharmcol 40:143-148
24. 1D binding sites. Br J Pharmacol 102:227-233
25. 1Dβ receptor subtype in human and bovine cerebral arteries. Mol Pharmacol 44:242-246
26. 1D receptor genes. Trends Pharmacol Sci 13:152-159
27. 1D receptors. Ann NY Acad Sci 600:168-181
28. Hoyer D, Boddeke HWGM (1993) Partial agonists, full agonists, antagonists: dilemmas of definition. Trends Pharmacol Sci 14: 270-275
29. Hoyer D, Clarke DE, Fozard JR, Hartig PR, Martin GR, Mylecharane EJ, Saxena PR, Humphrey PPA (1994) VII. International union of pharmacology classification of receptors for 5-hydroxytryptamine (scrotonin). Pharmacol Rev 46: 157-203
30. 1B receptor. J Biol Chem 267: 5735-5738
31. Kaumann AJ, Parsons AA, Brown AM (1993) Human arterial constrictor serotonin receptors. Cardiovasc Res 27:2094-2103
32. Kenakin T (1993a) Pharmacological analysis of drug-receptor interaction. Raven Press, New York, pp 46-49
33. Kenakin T (1993b) Pharmacological analysis of drug-receptor interaction. Raven Press, New York, pp 255-258
34. 1 receptors (abstract). Third IUPHAR Satellite Meeting on Serotonin. p.116
35. 1D subtype. J Biol Chem 267:7553-7562
36. Manuel NA, Wallis DI. Crick H (1995) Ketanserin-sensitive depressant actions of 5-HT receptor agonists in the neonatal rat spinal cord. Br J Pharmacol 116:2647-2654
37. 1D autoreceptors in human cerebral cortex. J Neurochem 60:1179-1182
38. 1D receptor in the action of sumatripian. Eur J Pharmacol Mol Pharmacol Sect 227:99-102
39. 1-like receptors mediates 5-hydroxytryptamine-induced contraction of human isolated basilar artery. Br J Pharmacol 96:434-449
40. 1B receptors. Eur J Pharmacol Mol Pharmacol Sect 290:95-103
41. 1B receptors. Naunyn-Schmiedeberg's Arch Pharmacol 353:144-156
42. 1D receptors regulate 5-HT release in rat raphe nuclei: in vivo voltammetry and in vitro superfusion studies. Neuropsychopharmacology 13:249-260
43. Ruffolo RR, Nichols AJ, Stadel JM, Hieble JP (1991) Structure and function of α-adrenoceptors. Pharmacol Rev 43:475-505
44. 1D receptor antagonist. Br J Pharmacol 110:9P
45. Southern PJ, Berg P (1982) Transformation of mammalian cells to antibiotic resistance with a bacterial gene under control of SV40 early region promoter. J Mol Appl Genet 1:327-354
46. 1D receptor subtypes. J Rec Sign Transduc Res 15:199-211
47. 1A receptors to adenylyl cyclase. Mol Pharmacol 41:999-1007
48. 1D receptor subtype. Mol Pharmacol 42:439-444
49. 1D receptor: a progress review. Neurochem Res 15:567-582
50. 1Dβ receptors. Eur J Pharmacol 287:79-84
51. 1Dβ receptors. Br J Pharmacol 114:362P
52. 1Dβ Proc Natl Acad Sci USA 89:3630-3634
53. 1D receptor subtype. Mol Pharmacol 40:1036-1042
54. 1Dβ receptors stably expressed in murine fibroblasts: inhibition of adenylate cyclase and elevation of intracellular calcium concentrations via pertussis-toxin sensitive G protein(s). Mol Pharmacol 44:575-582
55. 1Dβ receptor subtypes. Eur J Pharmacol Mol Pharmacol Sect 291:9-15