OPIOID RECEPTOR LABELING WITH THE CHLOROMETHYL KETONE DERIVATIVE OF [H-3] TYR-D-ALA-GLY-(ME)PHE-GLY-OL (DAMGO) .2. COVALENT LABELING OF MU-OPIOID BINDING-SITE BY H-3 TYR-D-ALA-GLY-(ME)PHE CHLOROMETHYL KETONE

OKTEM, HÜSEYİN; MOITRA, J; BENYHE, S; TOTH, G; LAJTHA, A; BORSODI, A

doi:10.1016/0024-3205(91)90214-v

OPIOID RECEPTOR LABELING WITH THE CHLOROMETHYL KETONE DERIVATIVE OF [H-3] TYR-D-ALA-GLY-(ME)PHE-GLY-OL (DAMGO) .2. COVALENT LABELING OF MU-OPIOID BINDING-SITE BY H-3 TYR-D-ALA-GLY-(ME)PHE CHLOROMETHYL KETONE

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OKTEM H. A., MOITRA J., BENYHE S., TOTH G., LAJTHA A., BORSODI A.

LIFE SCIENCES, vol.48, no.18, pp.1763-1768, 1991 (SCI-Expanded)

Publication Type: Article / Article
Volume: 48 Issue: 18
Publication Date: 1991
Doi Number: 10.1016/0024-3205(91)90214-v
Journal Name: LIFE SCIENCES
Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus
Page Numbers: pp.1763-1768
Middle East Technical University Affiliated: Yes

Abstract

Opioid receptors of rat brain membranes were prelabeled with H-3-Tyr-D-Ala2-(Phe4)-Gly-CH2Cl, a chloromethyl ketone derivative of enkephalin, and solubilized in 1% digitonin. Hydrodynamic parameters of the receptor detergent complex derived from gel filtration and sucrose density gradient ultra-centrifugation were found to be 51 A and 8.7 S, respectively, and the size was estimated to be about 200 kDa. Sodium dodecyl sulfate gel electrophoresis followed by fluorography revealed specific alkylation of a major protein at 58 kDa.