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[3H]-(+)-pentazocine binding to sigma recognition sites in human cerebellum.

Abstract：

:The binding characteristics of the sigma-1 selective benzomorphan [3H]-(+)-pentazocine were determined in human cerebellar membranes. Saturation binding analysis revealed two affinity sites with a KDH of 1.4 +/- 0.7 nM and a KDL of 33.6 +/- 11.9 nM. Kinetic studies performed at 25 degrees C demonstrated reversible binding with association and dissociation rate constants determined for two classes of sites. In saturation binding studies, the addition of (+)-SKF 10,047 occluded binding of [3H]-(+)-pentazocine to high affinity sigma binding sites. The affinity profile of ligands displacing [3H]-(+)-pentazocine was consistent with the labeling of sigma-1 recognition sites with haloperidol > (+)-pentazocine > (+)-SKF 10,047 > (+)-3-PPP > DTG > (-)-pentazocine > (-)-SKF 10,047. The potency of the putative D3 receptor-selective ligand (+)-7-OH-DPAT was close to that measured for (+)-pentazocine in displacement experiments. These data suggest that [3H]-(+)-pentazocine labels sigma-1 sites in human cerebellum under appropriate assay conditions.

journal_name

Life Sci

journal_title

Life sciences

authors

Zabetian CP,Staley JK,Flynn DD,Mash DC

doi

10.1016/0024-3205(94)00322-x

subject

Has Abstract

pub_date

1994-01-01 00:00:00

pages

PL389-95

issue

20

eissn

0024-3205

issn

1879-0631

pii

0024-3205(94)00322-X

journal_volume

55

pub_type

杂志文章

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