EMD 68843, a serotonin reuptake inhibitor with selective presynaptic 5-HT(1A) receptor agonistic properties

European Journal of Pharmacology

Volumn 322, Issue 2-3, 1997, Pages 147-153

  Bartoszyk, Gerd D ^a   Hegenbart, Rainer ^a   Ziegler, Herbert ^a  

^a MERCK KGAA   (Germany)

Author keywords

5 HT(1A) autoreceptor; 8 OH DPAT (8 hydroxy 2 (di n propylamino)tetralin); EMD 68843; Fluoxetine; Hypothermic; Rat; Ultrasonic vocalization; WAY 100635

Indexed keywords

2 DIPROPYLAMINO 8 HYDROXYTETRALIN; AUTORECEPTOR; FLUOXETINE; N [2 [4 (2 METHOXYPHENYL) 1 PIPERAZINYL]ETHYL] N (2 PYRIDYL)CYCLOHEXANECARBOXAMIDE; SEROTONIN 1A AGONIST; SEROTONIN 1A ANTAGONIST; SEROTONIN 1A RECEPTOR; SEROTONIN UPTAKE INHIBITOR; UNCLASSIFIED DRUG; VILAZODONE;

ANIMAL EXPERIMENT; ARTICLE; BODY TEMPERATURE; CORE TEMPERATURE; DESENSITIZATION; DRUG EFFECT; HYPOTHERMIA; MALE; NONHUMAN; ORAL DRUG ADMINISTRATION; PRIORITY JOURNAL; RAT; SUBCUTANEOUS DRUG ADMINISTRATION; VOCALIZATION;

ANIMALS; BEHAVIOR, ANIMAL; BENZOFURANS; BODY TEMPERATURE; FLUOXETINE; INDOLES; MALE; PIPERAZINES; PRESYNAPTIC TERMINALS; PYRIDINES; RATS; RATS, SPRAGUE-DAWLEY; RATS, WISTAR; RECEPTORS, SEROTONIN; RECEPTORS, SEROTONIN, 5-HT1; SEROTONIN AGONISTS; SEROTONIN UPTAKE INHIBITORS;

EID: 0030957585     PISSN: 00142999     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0014-2999(96)00999-5     Document Type: Article

References (49)

1. 1A receptor: signalling, desensitization, and gene transcription, Neuropsychopharmacology 14, 19.
2. Artigas, F., V. Perez and E. Alvarez, 1994, Pindolol induces a rapid improvement of patients with depression treated with serotonin reuptake inhibitors, Arch. Gen. Psychiatry 51, 248.
3. Auerbach, S.B., J.F. Lundberg and S. Hjorth, 1995, Differential inhibition of serotonin release by 5-HT and NA blockers after systemic administration, Neuropharmacology 34, 89.
4. 1A-agonist EMD 68843, Soc. Neurosci. Abstr. 22, 613.
5. 1A receptors may induce a rapid antidepressant response, Psychopharmacol. Bull. 31, 523.
6. Blier, P. and R. Bergeron, 1995, Effectiveness of pindolol with selected antidepressant drugs in the treatment of major depression, J. Clin. Psychopharmacol. 15, 217.
7. 1A agonist geprione: electrophysiological studies in the rat brain, Synapse 1, 470.
8. Blier, P. and C. De Montigny, 1990, Differential effects of gepirone on presynaptic and postsynaptic serotonin receptors: single-cell recording studies, J. Clin. Psychopharmacol. 10, 13S.
9. Blier, P., C. De Montigny and Y. Chaput, 1987, Modifications of the serotonin system by antidepressant treatments: implications for the therapeutic response in major depression, J. Clin. Psychopharmacol. 7, 24S.
10. Blier, P., C. De Montigny and Y. Chaput, 1990, A role for the serotonin system in the mechanism of action of antidepressant treatments: preclinical evidence, J. Clin. Psychiatry 51 (Suppl.), 14.
11. Bonvento, G., B. Scatton, Y. Claustre and L. Rouquier, 1992, Effect of local injection of 8-OH-DPAT into the dorsal and median raphe nuclei on extracellular levels of serotonin in serotonergic projection areas in the rat brain, Neurosci. Lett. 137, 101.
12. Craven, R., D. Grahame-Smith and N. Newberry, 1994, WAY-100635 and GR127935: effects on 5-hydroxytryptamine-containing neurones, Eur. J. Pharmacol. 271, R1.
13. 1D autoreceptors, Br. J. Pharmacol. 114, 1107.
14. 1A receptor agonists: recent developments and controversial issues, Psychopharmacology 121, 1.
15. De Vry, J., U. Benz, R. Schreiber and J. Traber, 1993, Shock-induced ultrasonic vocalization in young adult rats: a model for testing putative anti-anxiety drugs, Eur. J. Pharmacol. 249, 331.
16. 1A receptors, Neurochem. Res. 21, 557.
17. 1A receptor antagonist, Br. J. Pharmacol. 112, 91P.
18. Godbout, R., Y. Chaput, P. Blier and C. De Montigny, 1991, Tandopsirone and its metabolite 1-(2-pyrimidinyl)-piperazine - I. Effects of acute and long-term administration of tandospirone on serotonin neurotransmission, Neuropharmacology 30, 679.
19. Goodwin, G.M., R.J. De Souza and A.R. Green, 1985, Presynaptic serotonin receptor-mediated response in mice attenuated by antidepressant drugs and electroconvulsive shock, Nature 317, 531.
20. Griebel, G., 1995, 5-Hydroxytryptamine-interacting drugs in animal models of anxiety disorders: more than 30 years of research, Pharmacol. Ther. 65, 319.
21. 1A properties of flesinoxan: in vivo electrophysiology and hypothermia study, Neuropharmacology 34, 1311.
22. Hjorth, S., 1985, Hypothermia in the rat induced by the potent serotoninergic agent 8-OH-DPAT, J. Neural Transm. 61, 131.
23. Hjorth, S., 1996, (-)-Pindolol, but not buspirone, potentiates the citalopram-induced rise in extracellular 5-hydroxytryptamine, Eur. J. Pharmacol. 303, 183.
24. 1A autoreceptors in the action of selective serotonin reuptake inhibitors, Eur. J. Pharmacol. 260, 251.
25. 1A agonist LY165163 and 8-OH-DPAT is not prevented by 5-HT depletion, Eur. J. Pharmacol. 143, 221.
26. Jackson, D.M., A. Bengtsson, C. Johansson, L. Cortizo and S.B. Ross, 1994, Development of tolerance to 8-OH-DPAT induced blockade of aquisition of a passive avoidance response, Neuropharmacology 33, 1003.
27. 1A receptor agonists and in their inhibitory effects on the firing of serotonergic neurons in the rat dorsal raphe nucleus?, J. Pharmacol. Exp. Ther. 272, 920.
28. 1A autoreceptors by chronic administration of 8-OH-DPAT, Neuropharmacology 31, 1073.
29. 1A autoreceptors of the dorsal and median raphe nuclei, J. Pharmacol. Exp. Ther. 269, 1268.
30. Kreiss, D.S. and I. Lucki, 1995, Effects of acute and repeated administration of antidepressant drugs on extracellular levels of 5-hydroxytryptamine measured in vivo, J. Pharmacol. Exp. Ther. 274, 866.
31. 1A receptor ligands (+)-WAY 100135 and SDZ 216-525, Eur. J. Pharmacol. 249, 25.
32. 1A receptor agonist 8-OH-DPAT, Neuropharmacology 29, 85.
33. Lucki, I., 1991, Behavioral studies of serotonin receptor agonists as antidepressant drugs, J. Clin. Psychiatry 52 (Suppl.), 24.
34. 1A receptor-mediated activity in the rat: a pharmacological characterization of the actions of novel agonists and antagonists, J. Pharmacol. Exp. Ther. 264, 1364.
35. Molewijk, H.E., A.M. Van der Poel, J. Mos, J.A.M. Van der Heyden and B. Olivier, 1995, Conditioned ultrasonic distress vocalizations in adult male rats as a behavioral paradigm for screening anti-panic drugs, Psychopharmacology 117, 32.
36. 1A antagonists WAY100135 and WAY100635, on guinea-pig behaviour and dorsal raphe 5-HT neurone firing, Br. J. Pharmacol. 117, 750.
37. O'Connell, M.T. and G. Curzon, 1996, A comparison of the effects of 8-OH-DPAT pretreatment on different behavioural responses to 8-OH-DAPT, Eur. J. Pharmacol. 312, 137.
38. 1A receptor activation, Br. J. Pharmacol. 106, 603.
39. Pawlowski, L., J. Ruczynska and J. Maj, 1980, Zimelidine and clomipramine: different influence on fenfluramine but not p-chloroamphetamine-induced pharmacological effects, Neurosci. Lett. 16, 203.
40. Pazos, A. and J.M. Palacios, 1985, Quantitative autoradiographic mapping of serotonin receptors in the rat brain. I. Serotonin-1 receptors, Brain Res. 346, 205.
41. Pazos, A., D. Hoyer, M.M. Dietl and J.M. Palacios, 1988, Autoradiography of serotonin receptors, in: Neuronal Serotonin, eds. N.N. Osborne and M. Hamon (Wiley&Sons, London) p. 507.
42. 1A receptors in a series of N4-substituted arylpiperazines, J. Med. Chem. 38, 4044.
43. Rényi, L, K. Ängeby Möller, K. Ensler and J. Evenden, 1992, The non-competitive NMDA receptor antagonist (+)MK801 conteracts the long-lasting attenuation of the hypothermic response induced by acute doses of 8-OH-DPAT in the rat, Neuropharmacology 31, 1265.
44. Sánchez, C., 1993, Effect of serotonergic drugs on foot-shock-induced ultrasonic vocalization in adult male rats, Behav. Pharmacol. 4, 269.
45. 1A receptor agonist 8-OH-DPAT, ipsapirone and buspirone in the rat, Eur. J. Pharmacol. 249, 341.
46. 1A receptor agonist ipsapirone in the rat: neurobiological correlates, Eur. J. Pharmacol. 240, 29.
47. Sugrue, M.F., 1980, Antagonism of fenfluramine-induced hypothermia in rats by some, but not all, selective inhibitors of 5-hydroxytryptamine uptake, Br. J. Pharmacol. 73, 307P.
48. 1A receptor activation in vivo, Life Sci. 56, PL-163.
49. 1A receptor mediated hypothermic response induced by 8-OH-DPAT in the rat, Prog. Neuro-Psychopharmacol. Biol. Psychiatry 18, 409.