SB-649915, a novel, potent 5-HT1A and 5-HT1B autoreceptor antagonist and 5-HT re-uptake inhibitor in native tissue

European Journal of Pharmacology

Volumn 536, Issue 1-2, 2006, Pages 54-61

  Scott, Claire ^a   Soffin, Ellen M ^a   Hill, Matthew ^a   Atkinson, Peter J ^a   Langmead, Christopher J ^a   Wren, Paul B ^a   Faedo, Stefania ^a   Gordon, Laurie J ^a   Price, Gary W ^a   Bromidge, Steve ^a   Johnson, Christopher N ^a   Hagan, James J ^a   Watson, Jeannette ^a  

^a GLAXOSMITHKLINE   (United Kingdom)

Author keywords

5 HT re uptake; 5 HT1A receptor; 5 HT1B receptor; Antagonist; Autoreceptor

Indexed keywords

2 DIPROPYLAMINO 8 HYDROXYTETRALIN; 6 [[1 [2 [(2 METHYLQUINOLIN 5 YL)OXY]ETHYL]PIPERIDIN 4 YL]METHYL] 2H 1,4 BENZOXAZIN 3(4H) ONE; GUANOSINE 5' O (3 THIOTRIPHOSPHATE); SB 649915; SEROTONIN; SEROTONIN 1A ANTAGONIST; SEROTONIN 1A RECEPTOR; SEROTONIN 1B ANTAGONIST; SEROTONIN 1B RECEPTOR; SEROTONIN 1D RECEPTOR; SEROTONIN TRANSPORTER; SEROTONIN UPTAKE INHIBITOR; TRITIUM; UNCLASSIFIED DRUG;

ANIMAL CELL; ANIMAL TISSUE; ARTICLE; BRAIN CORTEX; CELL STRAIN HEK293; CONCENTRATION RESPONSE; DORSAL RAPHE NUCLEUS; DRUG ACTIVITY; ELECTROPHYSIOLOGY; GUINEA PIG; IC 50; IN VITRO STUDY; MARMOSET; MOUSE; NONHUMAN; PRIORITY JOURNAL; PROTEIN EXPRESSION; RAT; SEROTONIN RELEASE; STIMULATION; SYNAPTOSOME;

ANIMALS; AUTORECEPTORS; BINDING, COMPETITIVE; CALLITHRIX; CEREBRAL CORTEX; DOSE-RESPONSE RELATIONSHIP, DRUG; GUANOSINE 5'-O-(3-THIOTRIPHOSPHATE); GUINEA PIGS; HUMANS; MICE; PIPERIDINES; QUINOLINES; RADIOLIGAND ASSAY; RAPHE NUCLEI; RATS; RATS, SPRAGUE-DAWLEY; RECEPTOR, SEROTONIN, 5-HT1A; RECEPTOR, SEROTONIN, 5-HT1B; RECEPTOR, SEROTONIN, 5-HT1D; RECOMBINANT PROTEINS; SEROTONIN; SEROTONIN AGONISTS; SEROTONIN ANTAGONISTS; SEROTONIN UPTAKE INHIBITORS;

EID: 33645881352     PISSN: 00142999     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.ejphar.2006.02.042     Document Type: Article

References (43)

1. 1Dβ receptor. Mol. Pharmacol. 41 (1992) 1-7
2. Agnel M., Esnaud H., Langer S.Z., and Graham D. Pharmacological characterization of the cloned human 5-hydroxytryptamine transporter. Biochem. Pharmacol. 51 (1996) 1145-1151
3. Artigas F., Celada P., Laruelle M., and Adell A. How does pindolol improve antidepressant action?. TIPS 22 (2001) 224-228
4. 1A receptor antagonists with potent 5-HT reuptake inhibitory activity. Bioorg. Med. Chem. Lett. 15 (2005) 737-741
5. Benedetti R., Faedo S., Negri M., Zumerle A., Cavallini P., Cavanni P., Corsi M., and Wren P.B. The effect of cell density on 5-HT transporter function. Fundam. Clin. Pharmacol. 18 suppl. 1 (2004) (P01.30)
6. Blier P., and Bouchard C. Modulation of 5-HT release in the guinea-pig brain following long term administration of antidepressant drugs. Br. J. Pharmacol. 113 (1994) 485-495
7. Blier P., and DeMontigny C. Electrophysiological investigations on the effect of repeated zimelidine administration on serotonergic neurotransmission in the rat. J. Neurosci. 3 (1983) 1270-1278
8. Blier P., Chaput Y., and DeMontigny C. Long-term 5-HT uptake blockade, but not monoamine oxidase inhibition, decreases the function of terminal 5-HT autoreceptors: an electrophysiologic study in the rat brain. Arch. Pharmacol. 337 (1988) 246-254
9. Bowen W.P., and Jerman J.C. Nonlinear regression using spreadsheets. Trends Pharmacol. Sci. 16 (1995) 413-417
10. 50) of an enzymatic reaction. Biochem. Pharmacol. 92 (1973) 881-894
11. 1A receptors in the rat brain. Br. J. Pharmacol. 123 (1998) 449-462
12. 1D autoreceptors. Br. J. Pharmacol. 114 (1995) 1107-1109
13. 1B/1D receptors on the modulation of acute fluoxetine-induced changes in extracellular 5-HT: the mechanism of action of (±)pindolol. Neuropharmacology 39 (2000) 1044-1052
14. 1A receptor-G protein interactions in brain following chronic antidepressant administration. Neuropsychopharmacology 26 (2002) 565-573
15. 2C/2B receptor antagonist with anxiolytic-like properties. Br. J. Pharmacol. 117 (1996) 427-434
16. Kreiss D.S., and Lucki I. Effects of acute and repeated administration of antidepressant drugs on extracellular levels of 5-hydroxytryptamine measured in vivo. JPET 274 (1995) 866-876
17. Manuel N.A., Wallis D.I., and Crick H. Ketanserin-sensitive depressant actions of 5-HT receptor agonists in the neonatal rat spinal cord. Br. J. Pharmacol. 116 (1995) 2647-2654
18. 1 sites in the rat brain. Brain Res. 291 (1984) 159-163
19. 1D receptors sited on different neurons and involved in different functions. Br. J. Pharmacol. 126 (1999) 607-612
20. McAskill R., and Taylor D. Pindolol augmentation of antidepressant therapy. Br. J. Psychiatry 173 (1998) 203-208
21. 1B receptor inverse agonist, blocks the 5-HT human terminal autoreceptor. Eur. J. Pharmacol. 375 (1999) 359-365
22. 1B autoreceptors: regional differences and effects of WAY-100635. Eur. J. Pharmacol. 486 (2004) 25-30
23. 1B receptors. Nature 360 (1992) 161-163
24. 1D receptor as a presynaptic autoreceptor in the guinea pig. Eur. J. Pharmacol. 493 (2004) 85-93
25. 1A receptors: reductions in neuroendocrine responses to 8-OH-DPAT and in levels of Gz and Gi proteins. JPET 288 (1999) 98-106
26. Rabiner E.A., Bhagwagar Z., Gunn R.N., Sargent P.A., Bench C.J., Cowen P.J., and Grasby P.M. Pindolol augmentation of selective serotonin reuptake inhibitors: PET evidence that the dose used in clinical trials is too low. Am. J. Psychiatry 158 (2001) 2080-2082
27. Roberts C., and Price G.W. Interaction of serotonin autoreceptor antagonists in the rat dorsal raphe nucleus: an in vitro fast cyclic voltammetry study. Neurosci. Lett. 300 (2001) 45-48
28. Roberts C., Watson J., Burton M., Price G.W., and Jones B.J. Functional characterization of the 5-HT terminal autoreceptor in the guinea pig brain cortex. Br. J. Pharmacol. 117 (1996) 384-388
29. 1A or 5-HT re-uptake site blockade. Neuropharmacology 38 (1999) 1409-1419
30. 1B receptor inverse agonist, on in vivo extracellular levels of 5-HT in the freely-moving guinea-pig. Naunyn-Schmiedeberg's Arch. Pharmacol. 362 (2000) 177-183
31. 1D (BRL-15572) receptor ligands on guinea-pig and human 5-HT auto- and heteroreceptors. Naunyn-Schmiedeberg's Arch. Pharmacol. 356 (1997) 321-327
32. Scott C., Watson J., Middlemiss D.N., and Price G.W. 5-HT1B receptor agonist: antagonist binding affinity differences as a measure of intrinsic activity. B. J. Pharmacol. 129 (2000) (159 pp.)
33. Segrave R., and Nathan P.J. Pindolol augmentation of selective serotonin reuptake inhibitors: accounting for the variability of results of placebo-controlled double-blind studies in patients with major depression. Hum. Psychopharmacol. 20 (2005) 163-174
34. 1B receptor antagonist with negative intrinsic activity. Br. J. Pharmacol. 125 (1998) 202-208
35. Shalom G., Gur E., Van de Kar L.D., and Newman M.E. Repeated administration of the 5-HT1B receptor antagonist SB-224289 blocks the desensitisation of 5-HT1B autoreceptors induced by fluoxetine. Naun. Schmied. Arch. Pharmacol. 370 (2004) 84-90
36. 1B receptor antagonists on extracellular 5-HT in rat frontal cortex in vivo. Br. J. Pharmacol. 121 (1997) 941-946
37. 35S]GTPγS binding in rat brain regions. Neuropharmacology 42 (2002) 1031-1038
38. Shopsin B. Enhancement of the antidepressant response to l-tryptophan by a liver pyrrolase inhibitor: a rational treatment. Neuropsychobiology 4 (1978) 188-192
39. 1D receptor antagonist. Behav. Brain Res. 73 (1996) 157-161
40. Thomas D.R., Nelson D.R., and Johnson A.M. Biochemical effects of the antidepressant paroxetine, a specific 5-hydroxytryptamine uptake inhibitor. Psychopharmacology 93 (1987) 193-200
41. 1Dβ receptors. Eur. J. Pharmacol. 314 (1996) 365-372
42. 1A receptor agonist-antagonist binding affinity difference as a measure of intrinsic activity in recombinant and native tissue systems. Br. J. Pharmacol. 130 (2000) 1108-1114
43. Young S.N., Smith S.E., Pihl R.O., and Ervin F.R. Tryptophan depletion causes a rapid lowering of mood in normal males. Psychopharmacology 87 (1985) 173-177