Coupling of multiple opioid receptors to GTPase following selective receptor alkylation in brain membranes

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Coupling of multiple opioid receptors to GTPase following selective receptor alkylation in brain membranes.

Opioid agonists of the mu, kappa and delta types stimulated low-Km guanosine triphosphatase (GTPase) in membranes, from the brain of the rat by up to 34%, with potencies the rank order of which corresponded to the respective binding affinities to opioid receptor. In general, kappa ligands stimulated GTPase to a lesser degree than mu or delta opiates. The coupling of a given type of opioid recep...

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EVIDENCE FOR COUPLING OF THE K OPIOID RECEPTOR TO BRAIN GTPase

In membranes from guinea pig cerebellum, a tissue which predominantly contains < opioid receptors, exogenous and endogenous K-selective opioid agonists stimulated low-Km GTPase activity by 11-20% with concentrations for halfmaximal stimulation of 3-23 ~M. Opioid ligands of the and ~ type had no effect on GTPase in these membranes. Similar stimulation of GTPase by K opiates was obtained in rat a...

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Relationship between opioid-receptor occupancy and stimulation of low-Km GTPase in brain membranes.

Treatment of rat brain membranes with the irreversible opioid ligand cis-3-methylfentanylisothiocyanate (Superfit) was used to reduce gradually the number of available binding sites for the delta-selective agonist [3H][D-Ser2,Leu5]enkephalin-Thr6 ([ 3H]DSLET). Subsequently, the correlation between ligand binding and low-Km GTPase was investigated. Alkylation with 10 microM and 25 microM Superfi...

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Mu opioid receptor coupling to Gi/o proteins increases during postnatal development in rat brain.

Mu opioid receptors are densely expressed within rat striatum and are concentrated in anatomically discrete patches called striosomes. The density of striosomal mu receptors remains relatively constant during postnatal development, but little is known about their functional maturation. We examined the extent of G protein coupling by mu opioid receptors in rat brain during development, focusing ...

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Cloning and characterization of multiple opioid receptors.

Over the course of 1 to 2 years, the field has moved swiftly to investigate the functional and structural properties of the newly cloned opioid receptors. Achieving a better understanding of these macromolecules is likely to have profound implications for drug design aimed at the production of better analgesic drugs, for a more fundamental understanding of mechanisms of action of drugs of abuse...

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ژورنال

عنوان ژورنال: Neuropharmacology

سال: 1987

ISSN: 0028-3908

DOI: 10.1016/0028-3908(87)90129-8