Schizophrenia and L-745,870, a novel dopamine D4 receptor antagonist

被引：38

作者：

Bristow, LJ

Kramer, MS

Kulagowski, J

Patel, S

Ragan, CI

Seabrook, GR

机构：

[1] Department of Pharmacology, Merck, Sharp Dohme, Neurosci. R., Harlow

[2] Merck Research Laboratories, West Point, Philadelphia, PA

[3] Department of Medicinal Chemistry, Merck, Sharp Dohme, Neurosci. R., Harlow

[4] Department of Biochemistry, Merck, Sharp Dohme, Neurosci. R., Harlow

来源：

TRENDS IN PHARMACOLOGICAL SCIENCES | 1997年 / 18卷 / 06期

关键词：

D O I：

10.1016/S0165-6147(97)01066-3

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

The discovery of a novel high-affinity and selective dopamine D4 receptor antagonist, L-745,870, and the results of clinical trials with this compound are reviewed. Despite several lines of evidence which suggest that a selective D4 receptor antagonist may be an effective antipsychotic agent with a lower propensity to induce extrapyramidal side-effects, L-745,870 was ineffective as an antipsychotic in humans.

引用

页码：186 / 188

页数：3

共 11 条

[1] COMPARISON BETWEEN THE PHARMACOLOGY OF DOPAMINE-RECEPTORS MEDIATING THE INHIBITION OF CELL FIRING IN RAT-BRAIN SLICES THROUGH THE SUBSTANTIA-NIGRA PARS COMPACTA AND VENTRAL TEGMENTAL AREA [J].

BOWERY, B ;

ROTHWELL, LA ;

SEABROOK, GR .

BRITISH JOURNAL OF PHARMACOLOGY, 1994, 112 (03) :873-880

[2]

Bristow LJ, 1996, BRIT J PHARMACOL, V119, pP210

[3]

KRAMER MS, IN PRESS ARCH GEN PS

[4] 3-[[4-(4-chlorophenyl)piperazin-1-yl]methyl]-1H-pyrrolo[2,3-b]pyridine: An antagonist with high affinity and selectivity for the human dopamine D-4 receptor [J].

Kulagowski, JJ ;

Broughton, HB ;

Curtis, NR ;

Mawer, IM ;

Ridgill, MP ;

Baker, R ;

Emms, F ;

Freedman, SB ;

Marwood, R ;

Patel, S ;

Ragan, CI ;

Leeson, PD .

JOURNAL OF MEDICINAL CHEMISTRY, 1996, 39 (10) :1941-1942

[5] FUNCTIONAL COUPLING OF HUMAN D-2, D-3, AND D-4 DOPAMINE-RECEPTORS IN HEK293 CELLS [J].

MCALLISTER, G ;

KNOWLES, MR ;

WARDBOOTH, SM ;

SINCLAIR, HA ;

PATEL, S ;

MARWOOD, R ;

EMMS, F ;

PATEL, S ;

SMITH, A ;

SEABROOK, GR ;

FREEDMAN, SB .

JOURNAL OF RECEPTOR AND SIGNAL TRANSDUCTION RESEARCH, 1995, 15 (1-4) :267-281

[6]

OMALLEY KL, 1992, NEW BIOL, V4, P137

[7]

Patel S, 1996, BRIT J PHARMACOL, V119, pP30

[8]

REYNOLDS GP, 1994, J NEUROCHEM, V63, P1576

[9] PHARMACOLOGY OF HIGH-THRESHOLD CALCIUM CURRENTS IN GH(4)C(1) PITUITARY-CELLS AND THEIR REGULATION BY ACTIVATION OF HUMAN D-2 AND D-4 DOPAMINE-RECEPTORS [J].

SEABROOK, GR ;

KNOWLES, M ;

BROWN, N ;

MYERS, J ;

SINCLAIR, H ;

PATEL, S ;

FREEDMAN, SB ;

MCALLISTER, G .

BRITISH JOURNAL OF PHARMACOLOGY, 1994, 112 (03) :728-734

[10] DOPAMINE D4 RECEPTORS ELEVATED IN SCHIZOPHRENIA [J].

SEEMAN, P ;

GUAN, HC ;

VANTOL, HHM .

NATURE, 1993, 365 (6445) :441-445

← 1 2 →