Therapeutic implications of dopamine D4 vs. D2 receptor selectivity and occupancy

R. A. Lahti; G. S. Gill; C. A. Tamminga; D. L. Evans; N. C. Stratman; L. M. Figur

doi:10.1016/0924-977X(93)90046-O

Therapeutic implications of dopamine D₄ vs. D₂ receptor selectivity and occupancy

R. A. Lahti, G. S. Gill, C. A. Tamminga, D. L. Evans, N. C. Stratman, L. M. Figur

Research output: Contribution to journal › Article › peer-review

Abstract

Clozapine and melperone exhibit higher affinity for the dopamine D₄ receptor than the D₂ receptor. Raclopride and chlorpromazine exhibit high selectivity for the dopamine D₂ receptor. D₄ selective compounds have a low incidence of EPS and TD, whereas D₂ selective compounds have a higher incidence. It is postulated that a drug's affinity for the D₄ receptor may confer antipsychotic activity and its affinity for the D₂ receptor may confer EPS and/or TD activity.

Original language	English (US)
Pages (from-to)	234-236
Number of pages	3
Journal	European Neuropsychopharmacology
Volume	3
Issue number	3
DOIs	https://doi.org/10.1016/0924-977X(93)90046-O
State	Published - Sep 1993

Keywords

Antipsychotic
Dopamine D
Dopamine D
Dyskinesia
Extrapyramidal

ASJC Scopus subject areas

Pharmacology
Neurology
Clinical Neurology
Psychiatry and Mental health
Biological Psychiatry
Pharmacology (medical)

Access to Document

10.1016/0924-977X(93)90046-O

Cite this

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title = "Therapeutic implications of dopamine D4 vs. D2 receptor selectivity and occupancy",

abstract = "Clozapine and melperone exhibit higher affinity for the dopamine D4 receptor than the D2 receptor. Raclopride and chlorpromazine exhibit high selectivity for the dopamine D2 receptor. D4 selective compounds have a low incidence of EPS and TD, whereas D2 selective compounds have a higher incidence. It is postulated that a drug's affinity for the D4 receptor may confer antipsychotic activity and its affinity for the D2 receptor may confer EPS and/or TD activity.",

keywords = "Antipsychotic, Dopamine D, Dopamine D, Dyskinesia, Extrapyramidal",

author = "Lahti, {R. A.} and Gill, {G. S.} and Tamminga, {C. A.} and Evans, {D. L.} and Stratman, {N. C.} and Figur, {L. M.}",

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T1 - Therapeutic implications of dopamine D4 vs. D2 receptor selectivity and occupancy

AU - Lahti, R. A.

AU - Gill, G. S.

AU - Tamminga, C. A.

AU - Evans, D. L.

AU - Stratman, N. C.

AU - Figur, L. M.

PY - 1993/9

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AB - Clozapine and melperone exhibit higher affinity for the dopamine D4 receptor than the D2 receptor. Raclopride and chlorpromazine exhibit high selectivity for the dopamine D2 receptor. D4 selective compounds have a low incidence of EPS and TD, whereas D2 selective compounds have a higher incidence. It is postulated that a drug's affinity for the D4 receptor may confer antipsychotic activity and its affinity for the D2 receptor may confer EPS and/or TD activity.

KW - Antipsychotic

KW - Dopamine D

KW - Dyskinesia

KW - Extrapyramidal

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