Binding characteristics of kappa opioids in rat brain. A comparison of in vitro binding paradigms.

Abstract:

:Putative kappa binding was investigated in homogenates of the brain of the rat using [3H]ethylketocylazocine and [3H]diprenorphine under conditions where mu and delta sites were blocked. Under blocked conditions, the binding of [3H]ethylketocyclazocine labelled a single site, as defined by kinetic and equilibrium analysis, which showed high affinity for dynorphin 1-17, U50,488H, and benzomorphan compounds. However, blocked binding of [3H]diprenorphine showed a biphasic dissociation curve, and did not show high affinity for the specific kappa agonists dynorphin 1-17 or U50,488H. It is proposed that blocked [3H]ethylketocyclazocine is the more appropriate paradigm to study putative kappa binding, while blocked [3H]diprenorphine may label additional non-mu/non-delta sites.

journal_name

Neuropharmacology

journal_title

Neuropharmacology

authors

Weyhenmeyer JA,Mack KJ

doi

10.1016/0028-3908(85)90169-8

subject

Has Abstract

pub_date

1985-02-01 00:00:00

pages

111-5

issue

2

eissn

0028-3908

issn

1873-7064

journal_volume

24

pub_type

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