Opiate receptor binding profile in the rabbit cerebellum and brain membranes.

Article Details

Citation

Copy to clipboard

Ho CL, Hammonds RG Jr, Li CH

Opiate receptor binding profile in the rabbit cerebellum and brain membranes.

Biochem Pharmacol. 1985 Apr 1;34(7):925-31.

PubMed ID

2985086 [ View in PubMed

]

Abstract

The equilibrium dissociation constants (Kd) and maximal binding capacities of tritiated dihydromorphine (DHM), [D-Ala2,D-Leu5]enkephalin (DADLE), ethylketocyclazocine (EKC) and human beta-endorphin (beta-EP) in rabbit cerebellum and brain membranes have been investigated. Binding of tritiated DHM and DADLE was adequately described by a single affinity class of binding sites, while that of EKC required two affinity sites. Binding of tritiated beta-EP was also consistent with a single affinity class of binding sites by Scatchard analysis, but inhibition of the binding with type selective opiate receptor ligands revealed multiple sites. Sequential displacement of a broad spectrum opiate ligand, diprenorphine (DIP), by type selective ligands showed that cerebellum membranes are relatively rich in mu (40%) and deficient in K (12%) binding sites, while brain membranes are relatively rich in K (32%) and deficient in mu (12%) binding sites. beta-EP displaces 88 and 73% of tritiated DIP from cerebellum and brain membranes, respectively, suggesting multiple sites of beta-EP binding.

DrugBank Data that Cites this Article

Drug Targets

Drug	Target	Kind	Organism	Pharmacological Action	Actions
Dihydromorphine	E3 ubiquitin-protein ligase TRIM13	Protein	Humans	Unknown	Agonist	Details