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A guinea pig ileum preparation devoid of functional kappa receptors: a new in vitro pharmacologic assay for mu-opioid ligands.

Abstract：

:Guinea pig ileum longitudinal muscle/myenteric plexus preparations contain functional mu- and kappa-opioid receptors. A preparation with blocked kappa receptors was obtained by pretreating guinea pigs with 0.1-10.0 mg/kg intraperitoneal doses of a new kappa-selective affinity label, DIPPA (2-(3,4-dichlorophenyl)-N-methyl-N-[1S-1-(-3-isothiocyanatophenyl)-2-(-1 -pyrrolidinyl) ethyl] acetamide). Determination of IC50 values for the mu-selective agonist DAMGO ([D-Ala2,MePhe4,Gly(ol)5]-enkephalin) and the kappa-selective agonist U 69,593 ([5alpha,7alpha,8beta]-(+)-N-methyl-N-[7-(1-pyrrolidin yl)-1-oxaspiro-(4,5)-dec-8-yl]) showed that 0.5 mg/kg DIPPA at 48 h produced reliable, near-complete blockade of kappa-opioid activity but a minimal shift for kappa-opioid agonism. This new assay should be useful for studying mixed agonists/antagonists that produce strong kappa-opioid receptor agonism, which prevents determination of mu-opioid receptor antagonism.

journal_name

Life Sci

journal_title

Life sciences

authors

Schwartz RW,Chang AC,Portoghese PS,Berzetei-Gurske IP

doi

10.1016/s0024-3205(97)00076-3

subject

Has Abstract

pub_date

1997-01-01 00:00:00

pages

PL235-9

issue

15

eissn

0024-3205

issn

1879-0631

pii

S0024320597000763

journal_volume

60

pub_type

杂志文章

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