[3H]2-nitroimipramine: A selective "slowly-dissociating" probe of the imipramine binding site ("serotonin transporter") in platelets and brain

Moshe Rehavi, Howard Tracer, Kenner Rice, Phil Skolnick, Steven M. Paul

Research output: Contribution to journalArticle

15 Scopus citations

Abstract

Previous studies have demonstrated a close functional and structural relationship between the "high affinity" binding site for [3H]imipramine and the presynaptic and platelet uptake site(s) for serotonin. Recently we have synthesized several nitro derivatives of imipramine which have a very high affinity for the imipramine binding site and which dissociate very slowly when incubations are performed at 0-4°C. In this report, we describe the characteristics of [3H]2-nitroimipramine binding to platelet and brain membranes. Our results support the relative utility of this ligand for studying the impramine binding site (serotonin transporter) since this analogue has both a higher affinity and specific activity than [3H]imipramine. [3H]2-Nitroimipramine by virtue of its extremely slow dissociation rate should be a valuable tool in subsequent characterization and purification of the serotonin uptake or transport site.

Original languageEnglish
Pages (from-to)645-653
Number of pages9
JournalLife Sciences
Volume32
Issue number6
DOIs
StatePublished - Feb 7 1983
Externally publishedYes

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