Interaction of AZA analogs of chlorpromazine with the dopamine D2 receptor

Tahira Farooqui, Kim Markovich, Lane Wallace, Duane Miller, Norman Uretsky

Research output: Contribution to journalArticle

5 Citations (Scopus)

Abstract

1. 1. Permanently charged AZA analogs of chlorpromazine inhibited the binding of [3H]spiperone and antagonized the apomorphine-induced inhibition of the potassium evoked release of [3H]acetylcholine. 2. 2. The AZA analogs were more potent in binding affinity and antagonist activity than the trimethylammonium analog of chlorpromazine but less potent than chlorpromazine. 3. 3. These results suggest that it is possible to enhance the binding of the permanently charged trimethylammonium analog of chlorpromazine by the addition of a functional group near the quaternary nitrogen which is capable of forming a hydrogen bond with the D2 dopamine receptor. 4. 4. However, it appears that for optimal binding, as achieved with chlorpromazine, the hydrogen-bonding proton should be on the charged nitrogen.

Original languageEnglish (US)
Pages (from-to)147-151
Number of pages5
JournalGeneral Pharmacology
Volume24
Issue number1
DOIs
StatePublished - Jan 1 1993
Externally publishedYes

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Dopamine D2 Receptors
Chlorpromazine
Nitrogen
Spiperone
Apomorphine
Hydrogen Bonding
Acetylcholine
Protons
Hydrogen
Potassium

All Science Journal Classification (ASJC) codes

  • Pharmacology

Cite this

Interaction of AZA analogs of chlorpromazine with the dopamine D2 receptor. / Farooqui, Tahira; Markovich, Kim; Wallace, Lane; Miller, Duane; Uretsky, Norman.

In: General Pharmacology, Vol. 24, No. 1, 01.01.1993, p. 147-151.

Research output: Contribution to journalArticle

Farooqui, Tahira ; Markovich, Kim ; Wallace, Lane ; Miller, Duane ; Uretsky, Norman. / Interaction of AZA analogs of chlorpromazine with the dopamine D2 receptor. In: General Pharmacology. 1993 ; Vol. 24, No. 1. pp. 147-151.
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