Inhibitory effects of NaCl and guanyl-5'yl-imidodiphosphate (GppNHp) on [3H]naloxone binding to kappa-opioid receptors in guinea pig cerebellum.

Abstract:

:Studies were performed to characterize the opioid receptors in guinea pig brain using the radiolabeled opioid antagonists, [3H]naloxone and [3H]diprenorphine and the kappa-agonist [3H]U-69593. The binding of [3H]U-69593 to guinea pig cerebellar membranes was reduced by NaCl, guanyl-5'yl-imidodiphosphate (GppNHp) and NaCl+GppNHp, and [3H]naloxone binding to cerebellar membranes was also reduced by NaCl and GppNHp. In the guinea pig cerebral cortex and striatum and the rat cerebellum, [3H]naloxone binding was not affected significantly by GppNHp in the presence or absence of 100 nM [D-Ala2,N-Me-Phe4,Gly5-ol]enkephalin (DAMGO) and [D-Ala2, D-Leu5]enkephalin (DADLE). Guinea pig cerebellar [3H]diprenorphine binding was not affected by NaCl, GppNHp or NaCl+GppNHp. Furthermore, [3H]naloxone binding was reduced after pretreating cerebellar membranes with N-ethylmaleimide (NEM), which also attenuated GppNHp-induced inhibition of cerebellar [3H]naloxone binding. These results suggest that the properties of [3H]naloxone binding in guinea pig cerebellum differ from those in other brain regions and rat cerebellum, and that the interaction of [3H]naloxone and [3H]U-69593, but not [3H]diprenorphine, with guinea pig cerebellar opioid receptors is associated with a G-protein.

journal_name

Biol Pharm Bull

authors

Ishige K,Makimura M,Ito Y,Murakoshi Y

doi

10.1248/bpb.16.921

subject

Has Abstract

pub_date

1993-09-01 00:00:00

pages

921-5

issue

9

eissn

0918-6158

issn

1347-5215

journal_volume

16

pub_type

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