SYNTHESIS OF NEW HALOPERIDOL ANALOGUES AND CHARACTERIZATION OF THEIR INTERACTIONS WITH α‐ADRENOCEPTORS IN RAT PAROTID SLICES AND HUMAN PLATELET MEMBRANES

DAPHNE ATLAS*, ZEEV FRIEDMAN, YAIR LITVIN, MICHAEL L. STEER

*Corresponding author for this work

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Abstract

The synthesis of several butyrophenone analogues of haloperidol is described. The effects of these compounds on α‐adrenoceptors were evaluated by examining their ability to reduce α1‐stimulated K+ release from rat parotid slices and to displace [3H]‐phentolamine from human platelet membrane α2‐adrenoceptors. The affinity of haloperidol and its analogues for α1‐receptors was found to be 1 to 2 orders of magnitude greater than that for α2‐adrenoceptors. These observations suggest that most of the α‐adrenoceptor activity of butyrophenones results from their interaction with α1‐adrenoceptors. The relatively high affinity of the butyrophenones for α1‐adrenoceptors suggests that they may be useful as probes in studies of α1‐adrenoceptors in these and other tissues. 1982 British Pharmacological Society

Original languageEnglish
Pages (from-to)213-217
Number of pages5
JournalBritish Journal of Pharmacology
Volume75
Issue number1
DOIs
StatePublished - Jan 1982
Externally publishedYes

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