Affinity labels for opioid receptors

A. E. Takemori, P. S. Portoghese

Research output: Contribution to journalArticlepeer-review

128 Scopus citations


A variety of affinity labels have been synthesized as pharmacologic and biochemical probes for opioid receptors. Their usefulness as affinity labels is related to their receptor selectivity and pharmacologic characteristics. High selectivity or, better still, specificity for a single receptor type or subtype is an important feature. The potential for obtaining specific electrophilic affinity labels is greater than for other classes of affinity labels because two consecutive recognition steps lead to the amplification of selectivity. Indeed, of the presently available affinity labels, the electrophilic antagonist affinity labels have proved to be the most useful opioid receptor probes for pharmacologic studies. The fact that electrophilic affinity labels can be employed in studies both in vitro and in vivo represents a distinct advantage over photoaffinity labels, which can be activated only in vitro.

Original languageEnglish (US)
Pages (from-to)193-223
Number of pages31
JournalAnnual review of pharmacology and toxicology
VolumeVOL. 25
StatePublished - 1985


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