The bovine peripheral-type benzodiazepine receptor: a receptor with low affinity for benzodiazepines.

Abstract:

:The density of bovine peripheral-type benzodiazepine receptors (PBR) in four tissues was highest in adrenal cortex. The adrenal cortex PBR cofractionated with a mitochondrial membrane marker enzyme and could be solubilized with intact ligand binding properties using digitonin. The membrane bound and soluble mitochondrial receptors were pharmacologically characterized and showed the rank order of potency to inhibit [3H]PK 11195 binding was PK 11195 greater than protoporphyrin IX greater than benzodiazepines (clonazepam, diazepam, or Ro5-4864). [3H]PK 11195 binding to bovine adrenal mitochondria was unaffected by diethylpyrocarbonate, a histidine residue modifying reagent that decreased binding to rat liver mitochondria by 70%. [3H]PK 14105 photolabeled the bovine PBR and the Mr was estimated under nondenaturing (200 kDa) and denaturing (17 kDa) conditions. These results demonstrate the bovine peripheral-type benzodiazepine receptor is pharmacologically and biochemically distinct from the rat receptor, but the receptor component photolabeled by an isoquinoline ligand has a similar molecular weight.

journal_name

Life Sci

journal_title

Life sciences

authors

Parola AL,Laird HE 2nd

doi

10.1016/0024-3205(91)90090-x

subject

Has Abstract

pub_date

1991-01-01 00:00:00

pages

757-64

issue

8

eissn

0024-3205

issn

1879-0631

pii

0024-3205(91)90090-X

journal_volume

48

pub_type

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