Characterization of 5-HT(1A) receptor functional coupling in cells expressing the human 5-HT(1A) receptor as assessed with the cytosensor microphysiometer

Journal of Pharmacological and Toxicological Methods

Volumn 40, Issue 1, 1998, Pages 47-55

  Dunlop, John ^a   Zhang, Yingxin ^a   Smith, Deborah L ^a   Schechter, Lee E ^a  

^a PFIZER INC   (United States)

Author keywords

Cyclic AMP; Human 5 HT(1A) receptor; Microphysiometer

Indexed keywords

2 DIPROPYLAMINO 8 HYDROXYTETRALIN; 8 [2 [4 (2 METHOXYPHENYL) 1 PIPERAZINYL]ETHYL] 8 AZASPIRO[4.5]DECANE 7,9 DIONE; ADENYLATE CYCLASE; BUSPIRONE; CYCLIC AMP; IPSAPIRONE; LIGAND; N TERT BUTYL 3 [4 (2 METHOXYPHENYL) 1 PIPERAZINYL] 2 PHENYLPROPIONAMIDE; PINDOLOL; SEROTONIN 1A RECEPTOR; FORSKOLIN; SEROTONIN 1 RECEPTOR; SEROTONIN AGONIST; SEROTONIN RECEPTOR;

ANIMAL CELL; ARTICLE; CHO CELL; CONTROLLED STUDY; DEVICE; MEASUREMENT; NONHUMAN; PROTEIN EXPRESSION; RECEPTOR BINDING; ANIMAL; BIOSYNTHESIS; CYTOLOGY; DRUG EFFECT; HAMSTER; HUMAN; INSTRUMENTATION; METABOLISM; MOLECULAR CLONING; POLYMERASE CHAIN REACTION; RADIOASSAY;

ANIMALS; CHO CELLS; CLONING, MOLECULAR; CRICETINAE; CYCLIC AMP; CYTOLOGICAL TECHNIQUES; FORSKOLIN; HUMANS; POLYMERASE CHAIN REACTION; RADIOLIGAND ASSAY; RECEPTORS, SEROTONIN; RECEPTORS, SEROTONIN, 5-HT1; SEROTONIN AGONISTS;

EID: 0032217303     PISSN: 10568719     EISSN: None     Source Type: Journal    
DOI: 10.1016/S1056-8719(98)00035-5     Document Type: Article

References (39)

1. 1A antagonists. Trends Neurosci 19:378-383.
2. 1A antagonists on hippocampal 5-hydroxytryptamine levels: (S)-WAY100135, but not WAY100635, has partial agonist properties. Eur J Pharmacol 304:15-21.
3. 1A receptor antagonist (S)-5-fluoro-8-hydroxy-2-(dipropylamino)tetralin: inhibition of (R)-8-hydroxy-2-(dipropylamino)tetralin-induced effects. J Pharmacol Exp Ther 258:58-65.
4. 1A receptors: variations in intrinsic activity studied in transfected HeLa cells. Naunyn Schmied Arch Pharmacol 345:257-263.
5. 1A serotonin receptor. Mol Pharmacol 45:516-520.
6. Chen J, De Vivo M, Dingus J, Harry A, Li J, Sui J, Carty DJ, Blank JL, Exton JH, Stoffel RH, Inglese J, Lefkowitz RJ, Logothetis DE, Hildebrandt JD, Iyengar R (1995) A region of adenylyl cyclase 2 critical for regulation by G protein βγ subunits. Science 268:1166-1169.
7. 50) of an enzymatic reaction. Biochem Pharmacol 22:3099-3108.
8. Clapham DE (1994) Direct G protein activation of ion channels? Annu Rev Neurosci 17:441-464.
9. Clapham DE, Neer EJ (1993) New roles for G-protein βγ-dimers in transmembrane signalling. Nature 365:403-406.
10. 1A receptor-mediated inhibition of forskolin-stimulated adenylate cyclase activity in guinea-pig and rat hippocampal membranes. J Pharmacol Exp Ther 238:248-253.
11. 1A agonists in anxiety and depression. J Psycopharmacol 7:283-289.
12. 1A receptors which inhibit cAMP production in hippocampal and cortical neurons in primary culture. Mol Pharmacol 33:178-186.
13. 1A receptor antagonist activity of WAY-100135 and spiperone. J Pharmacol Exp Ther 268:441-447.
14. 1A receptors. Eur J Pharmacol 237:283-291.
15. 1A receptor antagonist, WAY100635. Eur J Pharmacol 281:81-88.
16. 1A ligand with anxiolytic and antidepressant properties. Drugs Future 13:429-431.
17. Goa KL, Ward A (1986) Buspirone: a preliminary review of its pharmacological properties and therapeutic efficacy as an anxiolytic. Drugs 32:114-129.
18. 1A receptor antagonists NAN-190 and BMY7378 are partial agonists in the rat dorsal raphe nucleus in vitro. Eur J Pharmacol 211:211-219.
19. Hirst MA, Pitchford SJ (1993) Use of a single assay system to assess functional coupling of a variety of receptors. J NIH Research 5:69-73.
20. Hjorth S, Carlsson A (1986) Is pindolol a mixed agonist-antagonist at central serotonin receptors? Eur J Pharmacol 129:131-138.
21. 1A receptors: behavioural and in vivo brain microdialysis studies. Life Sci 46:955-963.
22. Hodgkiss JP, Dawson IM, Kelly JS (1992) An intracellular study of the action of NAN-190 on neurons in the dorsal raphe nucleus of the rat. Brain Res 576:157-161.
23. Hoyer D, Boddeke WGM (1993) Partial agonists, full agonists, antagonists: dilemmas of definition. Trends Pharmacol Sci 14:270-275.
24. 3H]WAY-100635. Life Sci 60:653-665.
25. 1A receptor ligands (+)-WAY100135 and SDZ 216-525. Eur J Pharmacol 249:25-35.
26. Logothetis DE, Kurachi Y, Galper J, Neer EJ, Clapham DE (1987) The βγ subunits of GTP-binding proteins activate the muscarinic K' channel in heart. Nature 325:321-326.
27. McConnell HM, Owicki JC, Parce JW, Miller DL, Baxter GT, Wada HG, Pitchford S (1992) The cytosensor microphysiometer: biological applications of silicon technology. Science 257:1906-1912.
28. Meltzer HY, Maes M (1994) Effect of pindolol on L-5-HTP-induced increase in plasma prolactin and cortisol concentrations in man. Psychopharmacology 114:635-643.
29. Meltzer HY, Maes M (1996) Effect of pindolol on hormone secretion and body temperature: partial agonist effects. J Neural Transm 103:77-88.
30. Mistry R, Challiss RA (1996) Differences in agonist and antagonist activities for two indices of metabotropic glutamate receptor-stimulated phosphoinositide turnover. Br J Pharmacol 117:1735-1743.
31. 1A 5-hydroxytryptamine receptors in Chinese hamster ovary cells. Biochem J 285:933-938.
32. 1A receptor-mediated activation of high-affinity GTP hydrolysis in rta hippocampal memnranes. J Pharmacol Exp Ther 274:337-344.
33. 1A receptors that are negatively coupled to adenylate cyclase in permanently transfected HeLa cells. Biochem Pharmacol 45:375-383.
34. Saxena PR (1995) Serotonin receptors: subtypes, functional responses and therapeutic relevance. Pharmacol Ther 66:339-368.
35. Seelig S, Sayers G (1973) Isolated adrenal cortex cells: ACTH agonists, partial agonists, antagonists; cyclic AMP and corticosterone production. Arch Biochem Biophys 154:230-239.
36. 1A antagonist BMY7378. Eur J Pharmacol 176:331-340.
37. Tang W-J, Gilman AG (1991) Type-specific regulation of adenylyl cyclase by G protein βγ subunits. Science 254:1500-1503.
38. 1A receptors to adenylyl cyclase. Mol Pharmacol 41:999-1007.
39. 1A receptor in rat and guinea pig hippocampal membranes. Eur J Pharmacol 137:293-294.