Potential probe for isolation of the β-adrenoceptor, chloropractolol

Mordechai Erez, Marta Weinstock, Sasson Cohen, Gad Shtacher

Research output: Contribution to journalArticlepeer-review

Abstract

A TECHNIQUE which has proved highly successful in the isolation and identification of pharmacological receptors, is the use of a high affinity, selective label which binds irreversibly to the receptor1. We report here our findings with a new irreversible, potent and cardioselective (β-1) β adrenoceptor antagonist, chloropractolol (I). This new compound is a modification (Fig. 1) of practolol (II), and represents the first known selective, irreversible β antagonist. Chloropractolol (I) was prepared with the intention of incorporating an alkylating function into the parent compound, while maintaining β-1 selectivity. An additional advantage of using practolol (II) rather than propranolol as the parent molecule, is that the resultant compound should, like practolol, lack nonspecific membrane stabilising effect2 and any interaction with 5-hydroxytryptamine receptors 3.

Original languageEnglish
Pages (from-to)635-636
Number of pages2
JournalNature
Volume255
Issue number5510
DOIs
StatePublished - 1975

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