Roxindole: Psychopharmacological profile of a dopamine D2 autoreceptor agonist

Journal of Pharmacology and Experimental Therapeutics

Volumn 276, Issue 1, 1996, Pages 41-48

  Bartoszyk, G D ^a   Harting, J ^a   Minck, K O ^a  

^a MERCK KGAA   (Germany)

Author keywords

[No Author keywords available]

Indexed keywords

1,2,3,6 TETRAHYDRO 4 PHENYL 1 [(3 PHENYL 3 CYCLOHEXEN 1 YL)METHYL]PYRIDINE; 2 DIMETHYLAMINO 6,7 DIHYDROXYTETRALIN; 2,3,4,5 TETRAHYDRO 7,8 DIHYDROXY 1 PHENYL 1H 3 BENZAZEPINE; 3 [4 (1,2,3,6 TETRAHYDRO 4 PHENYL 1 PYRIDYL)BUTYL]INDOLE; APOMORPHINE; BUSPIRONE; CLOZAPINE; DOPAMINE 2 RECEPTOR STIMULATING AGENT; DOPAMINE AUTORECEPTOR; HALOPERIDOL; NEUROLEPTIC AGENT; PD 118717; ROXINDOLE; SEROTONIN 1A AGONIST; SEROTONIN UPTAKE INHIBITOR; TALIPEXOLE; U 86170F; UNCLASSIFIED DRUG;

ANIMAL BEHAVIOR; ANIMAL EXPERIMENT; ARTICLE; AVOIDANCE BEHAVIOR; CATALEPSY; CONTROLLED STUDY; DRUG ANTAGONISM; DRUG SELECTIVITY; MOUSE; NONHUMAN; PRIORITY JOURNAL; RAT; STEREOTYPY; SUBCUTANEOUS DRUG ADMINISTRATION;

2,3,4,5-TETRAHYDRO-7,8-DIHYDROXY-1-PHENYL-1H-3-BENZAZEPINE; ANIMALS; APOMORPHINE; AVOIDANCE LEARNING; AZEPINES; CATALEPSY; DOPAMINE AGONISTS; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG EVALUATION, PRECLINICAL; DRUG INTERACTIONS; INDOLES; MALE; MICE; MOTOR ACTIVITY; PYRIDINES; RATS; RATS, WISTAR; RECEPTORS, DOPAMINE D2; STEREOTYPED BEHAVIOR;

EID: 0029923485     PISSN: 00223565     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article

References (69)

1. ANDÉN, N.-E., GOLEMBIOWSKA-NIKITIN, K. AND THORNSTRÖM, U. Selective stimulation of dopamine and noradrenaline autoreceptors by B-HT 920 and B-HT 933, respectively. Naunyn-Schmiedeberg's Arch. Pharmacol. 321: 100-104, 1982.
2. ARNT, J. AND PERREGAARD, J.: Synergistic interaction between dopamine D-1 and D-2 receptor agonists: Circling behaviour of rats with hemitransection. Eur. J. Pharmacol. 143: 45-53, 1987.
3. BENKERT, O., GRÜNDER, G. AND WETZEL, H.: Dopamine autoreceptor agonists in the treatment of schizophrenia and major depression. Pharmacopsychiatry 25: 254-260, 1992.
4. BERENDSEN, H. H. G. AND BROEKKAMP, C. L. E.: Behavioural evidence for functional interactions between 5-HT-receptor subtypes in rats and mice Br. J. Pharmacol 101: 667-673, 1990.
5. BRAVI, D., DAVIS, T. L., MOURADIAN, M. M. AND CHASE, T N.: Treatment of Parkinson's disease with the partial dopamine agonist EMD 49980. Movement Disorders 8: 195-197, 1993.
6. CARLSSON, A.: Dopamine receptor agonists: Intrinsic activity vs state of the receptor. J. Neural Transm. 57: 309-315, 1983.
7. CARLSSON, A.: Dopamine autoreceptors and schizophrenia. In Receptors and Ligands in Psychiatry, ed. by A. K. Sen and T. Lee, pp. 1-10, Cambridge University Press, Cambridge, 1988.
8. CLARK, D., HJORTH, S. AND CARLSSON, A. Dopamine-receptor agonists: Mechanisms underlying autoreceptor selectivity. II. Theoretical considerations J. Neural Transm. 62: 171-207, 1985.
9. COSTALL, B., FORTUNE, D. H., NAYLOR, R. J., MARSDEN, C. D. AND PYCOCK, C.: Serotonergic involvement with neuroleptic catalepsy. Neuropharmacology 14: 869-868, 1975a.
10. COSTALL, B., KELLY, D. M. AND NAYLOR, R. J.: Nomifensine: A potent dopaminergic agonist of antiparkinson potential. Psychopharmacologia 41: 153-164, 1975b.
11. 2 receptor agonists in the treatment of schizophrenia. Psychopharm. Bull. 25: 393-397, 1989.
12. CUTLER, N. R., JESTE, D. V., KAROUM, F. AND WYATT, R. J.: Low-dose apomorphine reduces serum homovanillic acid concentrations in schizophrenic patients. Life Sci. 30: 753-756, 1982.
13. DEUTCH, A. Y., MOGHADDAM, B., INNIS, R. B., KRYSTAL, J. H., AGHAJANIAN, G. K., BUNNEY, B. S. AND CHARNEY, D. S.: Mechanisms of action of atypical antipsychotic drugs: Implications for novel therapeutic strategies for schizophrenia. Schizophrenia Res. 4: 121-156, 1991.
14. DI CHIARA, G., CORSINI, G. U , MEREU, G. P., TISSARI, A. AND GESSA, G. L.: Self-inhibitory dopamine receptors: Their role in the biochemical and behavioral effects of low doses of apomorphine. In Advances in Biochemical Psychopharmacology, Vol. 19, ed. by P. J. Roberts, G. N. Woodruff and L. L. Iversen, pp. 275-292, Raven Press, New York, 1978.
15. DIXON, W. J. AND MOOD, A. M.: A method for obtaining and analyzing sensitivity data. J. Am. Stat. Ass. 43: 109-126, 1948.
16. DOURISH, C. T., HUTSON, P. H. AND CURZON, G.: Low doses of the putative serotonin agonist 8-hydroxy-2-(di-n-propylamino) tetralin (8-OH-DPAT) elicit feeding in the rat. Psychopharmacology 86: 197-204, 1985.
17. DRUKARCH, B. AND STOOF, J. C.: D-2 dopamine autoreceptor selective drugs: Do they really exist? Life Sci. 47: 361-376, 1990.
18. DUNNETT, C. W.: New tables for comparisons with a control. Biometrics 20: 482-491, 1964.
19. ERNST, A. M : Mode of action of apomorphine and dexamphetamine on gnawing in rats. Psychopharmacologica 10: 316-323, 1967.
20. FERSTER, C. B. AND SKINNER, B. F.: Schedules of reinforcement. Appleton-Century-Crofts, New York, 1957.
21. GERLACH, J.: New antipsychotics: Classification, efficacy, and adverse effects. Schizophrenia Bull. 17: 289-309, 1991.
22. GOFF, D. C., MIDHA, K. K., BROTMAN, A. W., MCCORMICK, S., WAITES, M. AND AMICO, E. T.: An open trial of buspirone added to neuroleptics in schizophrenic patients. J. Clin. Psychopharmacol. 11: 193-197, 1991.
23. GOLEMBIOWSKA, K. AND WEDZONY, K.: Enhancement by ipsapirone of dopamine release in the striatum. Pol. J. Pharmacol. 45: 299-308, 1993.
24. GOODALE, D. B., RUSTERHOLZ, D. B., LONG, J. P., FLYNN, J. R., WALSH, B., CANNON, J. G. AND LEE, T.: Neurochemical and behavioral evidence for a selective presynaptic dopamine receptor agonist. Science (Wash. DC) 210: 1141-1143, 1980.
25. GRÜNDER, G., WETZEL, H., HAMMES, E. AND BENKERT, O.: Roxindole, a dopamine autoreceptor agonist, in the treatment of major depression. Psychopharmacology 111: 123-126, 1993.
26. 1A agonists with potential anxiolytic properties. J. Pharmacol. Exp. Ther. 246: 745-752, 1988.
27. HARTING, J. AND MINCK, K.-O.: Pharmacological characterization of the dopamine autoreceptor agonist roxindole. Naunyn-Schmiedeberg's Arch. Pharmacol 339: R104, 1989.
28. HICKS, P. B.: The effect of serotonergic agents on haloperidol-induced catalepsy. Life Sci. 47: 1609-1615, 1990.
29. HILLEGAART, V., WADENBERG, M.-L. AND AHLENIUS, S.: Effects of 8-OH-DPAT on motor activity in the rat. Pharmacol. Biochem. Behav. 32: 797-800, 1989.
30. HINZEN, D., HORNYKIEWICZ, O., KOBINGER, W., PICHLER, L., PIFL, C. AND SCHINGNITZ, G.: The dopamine autoreceptor agonist B-HT 920 stimulates denervated postsynaptic brain dopamine receptors in rodent and primate models of Parkinson's disease: A novel approach to treatment. Eur. J. Pharmacol. 131: 75-86, 1986.
31. 2 antagonistic actions. Japan. J. Pharmacol. 53: 321-329, 1990.
32. JASPERS, C., BENKER, G., REINHARDT, W., CISSEWSKI, K., LEDERBOGEN, S., SCHRÖDER, H -G. AND REINWEIN, D.: A new non-ergot dopamine agonist (roxindol) for treatment of prolactinoma: First results. Acta Endocrinol. 126: suppl. 4, 131 (#218), 1992.
33. JOHANSSON, C. E., MEYERSON, B. J. AND HOGLUND, A U.: The long-term effects of 8-hydroxy-2-(di-n-propyl-amino) tetralin (8-OH-DPAT) on copulatory and exploratory behaviour in male rats Eur. J. Pharmacol. 178: 1-9, 1990.
34. KALKMAN, H. O. AND SOAR, J.. Determination of the 5-HT receptor subtype involved in 8-OH-DPAT-induced hyperlocomotion: Potential difficulties arising from inadequate pharmacological tools. Eur. J. Pharmacol. 191: 383-390, 1990.
35. KLIMKE, A. AND KLIESER, E.: Antipsychotic efficacy of the dopaminergic autoreceptor agonist EMD 49980 (Roxindol). Pharmacopsychiatry 24: 107-112, 1991.
36. KOSTRZEWA, R. M.: Dopamine receptor supersensitivity. Neurosci. Biobehav. Rev. 19: 1-17, 1995.
37. KRAUTH, J.: A locally most powerful tied rank test in a Wilcoxon situation. Ann. Math Stat. 42: 1949-1956, 1971.
38. LAHTI, R. A., EVANS, D. L., FIGUR, L. M., HUFF, R. M AND MOON, M. W.: Pre- and postsynaptic dopaminergic activities of U-86170F. Naunyn-Schmiedeberg's Arch. Pharmacol. 344: 509-513, 1991.
39. LIEBERMAN, J. A.: Understanding the mechanism of action of atypical antipsychotic drugs. A review of compounds in use and development. Brit. J. Psychiatry 163: Suppl. 22, 7-18, 1993.
40. LONGONI, R., SPINA, L. AND DI CHIARA, G.: Permissive role of D-1 receptor stimulation by endogenous dopamine for the expression of postsynaptic D-2 mediated behavioural responses. Yawning in rats. Eur. J. Pharmacol. 134: 163-173, 1987.
41. MARTIN, G. E. AND BENDESKY, R. J.: Mouse locomotor activity. An in vivo test for dopamine autoreceptor activation. J. Pharmacol. Exp. Ther. 229: 706-711, 1984.
42. MCMILLEN, B. A., SCOTT, S. M. AND DAVANZO, E. A.: Reversal of neuroleptic-induced catalepsy by novel aryl-piperazine anxiolytic drugs. J. Pharm. Pharmacol. 40: 885-887, 1988.
43. MELLER, E., BOHMAKER, K., NAMBA, Y., FRIEDHOFF, A. J. AND GOLDSTEIN, M.: Relationship between receptor occupancy and response at striatal dopamine autoreceptors. Mol. Pharmacol. 31: 592-598, 1987.
44. MELLER, E., BORDI, F. AND BOHMAKER, K.: Enhancement by the D1 dopamine agonist SKF 38393 of specific components of stereotypy elicited by the D2 agonists LY 171555 and RU 24213. Life Sci. 42: 2561-2567, 1988.
45. MELTZER, L T., CHRISTOFFERSEN, C. L., CORBIN, A. E., NINTEMAN, F. W., SERPA, K. A., WILEY, J. N., WISE, L. D. AND HEFFNER, T. G.. CI-1007, a dopamine partial agonist and potential antipsychotic agent. II. Neurophysiological and behavioral effects. J. Pharmacol. Exp. Ther. 274: 912-920, 1995.
46. MOORE, N A. AND AXTON, M. S.: Production of climbing behavior in mice requires both D1 and D2 receptor activation. Psychopharmacology 94: 263-266, 1988.
47. PIFL, C. AND HORNYKIEWICZ, O.: Postsynaptic dopamine agonist properties of B-HT 920 as revealed by concomitant D-1 receptor stimulation. Eur. J. Pharmacol. 146: 189-191, 1988.
48. PROTAIS, P., COSTENTIN, J. AND SCHWARTZ, J. C.: Climbing behavior induced by apomorphine in mice: A simple test for the study of dopamine receptors in striatum. Psychopharmacology 50: 1-6, 1976.
49. PUECH, A. J., SIMON, P. AND BOISSIER, J. R.: Benzamides and classical neuroleptics: Comparison of their actions using 6 apomorphine-induced effects. Eur. J. Pharmacol. 50: 291-300, 1978.
50. PUGSLEY, T. A., CHRISTOFFERSON, C. L., CORBIN, A., DEWALD, H. A., DEMATTOS, S., MELTZER, L. T., MYERS, S. L., SHIH, Y.-H , WHETZEL, S. Z., WILEY, J. N., WISE, L D AND HEFFNER, T. G.: Pharmacological characterization of PD 118717, a putative piperazinyl benzopyranone dopamine autoreceptor agonist. J Pharmacol. Exp. Ther. 263: 1147-1158, 1992.
51. PUGSLEY, T. A., DAVIS, M. D., AKUNNE, H C., COOKE, L. W., WHETZEL, S. Z., MACKENZIE, R. G., SHIH, Y.-H., VAN LEEUWEN, D. H., DEMATTOS, S. B., GEORGIC, L. M , CAPRATHE, B. W., WRIGHT, J. C. JAEN, J. C., WISE, L D. AND HEFFNER, T. G.: CI-1007, a dopamine partial agonist and potential antipsychotic agent. I. Neurochemical effects. J. Pharmacol. Exp. Ther. 274: 898-911, 1995.
52. 1a agonist ±8-OH-DPAT modulates basal and stress-induced changes in medial prefrontal cortical dopamine. Synapse 18: 218-224, 1994.
53. SEYFRIED, C. A. AND BOETTCHER, H.: Central D2-autoreceptor agonists, with special reference to indolylbutylamines. Drugs Future 15: 819-832, 1990.
54. SEYFRIED, C. A , FUXE, K., WOLF, H.-P. AND AGNATI, L. F.: Demonstration of a new type of dopamine receptor agonist: An idolyl-3-butylamine. Actions at intact versus supersensitive dopamine receptors in the rat forebrain. Acta Physiol. Scand. 116: 465-468, 1982.
55. SEYFRIED, C. A., GREINER, H. E AND HAASE, A. F.: Biochemical and functional studies on EMD 49980: A potent, selectively presynaptic D-2 dopamine agonist with actions on serotonin systems. Eur. J. Pharmacol. 160: 31-41, 1989.
56. 2-receptor selectivity of roxindole (EMD 49980). Possible indirect effects on postsynaptic striatal cholinergic neurons. In Schizophrenia Research, ed. by C. A. Tamminga and S. C. Schulz, pp. 317-322, Raven Press, New York, 1991.
57. SMITH, R. C., TAMMINGA, C. AND DAVIS, J. M.: Effect of apomorphine on schizophrenic symptoms. J. Neural Transm. 40:171-176, 1977.
58. STȦHLE, L.: Do autoreceptors mediate dopamine agonist-induced yawning and suppression of exploration? A critical review. Psychopharmacology 106: 1-13, 1992.
59. STANLEY, M. E. AND GLICK, S. D.: Interaction of drug effects with testing procedures in the measurement of catalepsy. Neuropharmacology 15: 393-394, 1976.
60. STARR, M. S.: D-1/D-2 behavioural interactions in the rat involving striatal dopamine D-1 receptors. Eur. J. Pharmacol 151: 479-482, 1988.
61. TAMMINGA, C. A., SCHAFFER, M. H., SMITH, R. C. AND DAVIS, J. M.: Schizophrenic symptoms improve with apomorphine. Science (Wash. DC) 200: 567-568, 1978.
62. 1 receptor and of catecholaminergic systems in the behavioural response to 8-hydroxy-2-(di-n-propylamino)tetralin in the rat. Eur. J. Pharmacol. 106: 271-282, 1985.
63. VASSE, M., CHAGRAOUI, A. AND PROTAIS, P.: Climbing and stereotyped behaviours in mice require the stimulation of D-1 dopamine receptors. Eur. J. Pharmacol. 148: 221-229, 1988.
64. WACHTEL, H. AND DOROW, R.: Dual action of central dopamine function of transdihydrolisuride, a 9, 10-dihydrogenated analogue of the ergot dopamine agonist lisuride. Life Sci. 32: 421-432, 1983.
65. WADENBERG, M. L. AND AHLENIUS, S.: Antipsychotic-like profile of combined treatment with raclopride and 8-OH-DPAT in the rat: Enhancement of antipsychotic-like effects without catalepsy. J. Neural Transm. [GenSect] 83: 43-53, 1991.
66. WALTERS, J. R., BERGSTROM, D. A., CARLSON, J. H., CHASE, T. N. AND BRAUN, A. R.: D1 dopamine receptor activation required for postsynaptic expression of D2 agonist effects. Science (Wash. DC) 236: 719-722, 1987.
67. WIEDEMANN, K., KELLNER, M., KRIEG, J.-C. AND HOLSBOER, F.: Effects of the dopamine autoreceptor agonist roxindole in patients with depression. Clin. Neuropharmacol. 15: suppl. 1, 175B; 1992.
68. WISE, L. D. AND JAEN, J C.: Design of orally active dopamine autoreceptor agonists. In Drug Design for Neuroscience, ed. by A. P. Kozikowski, pp. 119-148, Raven Press, New York, 1993.
69. YASUDA, Y., KIKUCHI, T., SUZUKI, S., TSUTSUI, M., YAMADA, K. AND HIYAMA, T.: 7-[3-(4-[2,3-dimethylphenyl]piperazinyl)propoxy]-2(1H)-quinolinone (OPC-4392), a presynaptic dopamine autoreceptor agonist and postsynaptic D2 receptor antagonist. Life Sci. 42: 1941-1954, 1988.