Norbinaltorphimine: antagonist profile at kappa opioid receptors.

Abstract:

:The pharmacological profile of the opioid antagonist norbinaltorphimine has been characterised in vitro and in vivo. In vitro, norbinaltorphimine reversibly antagonised the effects of kappa agonists with pA2 values of 10.2-10.4. Norbinaltorphimine was much less potent as an antagonist at mu and delta receptors, pA2 values were 7.4-7.6 and 7.6-7.8, respectively. In all cases Schild slopes were unity. In vivo, norbinaltorphimine was an effective antagonist only at high dose levels and was not very selective between mu and kappa. The results indicate that in vitro norbinaltorphimine is a potent selective kappa antagonist; however, this antagonist profile is not maintained in vivo.

journal_name

Eur J Pharmacol

authors

Birch PJ,Hayes AG,Sheehan MJ,Tyers MB

doi

10.1016/0014-2999(87)90397-9

subject

Has Abstract

pub_date

1987-12-15 00:00:00

pages

405-8

issue

3

eissn

0014-2999

issn

1879-0712

pii

0014-2999(87)90397-9

journal_volume

144

pub_type

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