Abstract：
:The chloromethyl ketone derivative of D-Ala2-Leu5-enkephalin was synthesized in a radioactive form, and the resulting compound (3H-DALECK) was used to label opioid receptors. 3H-DALECK binds with high affinity, specificity and saturability to rat brain membranes. The number of sites labeled is 130 fmoles/mg protein. Unlabeled opioids inhibited the binding of 3H-DALECK; etorphine and DAGO being most potent. A 10-fold preference for mu sites over delta was seen in site-specific competition experiments; while DALECK displayed low affinity for kappa sites of rat brain. DALECK irreversibly blocked a certain population of sites. Approximately 40% of 3H-DALECK binding at 15 min, and 60% at 60 min association time did not dissociate in the presence of a large excess of unlabeled DALECK and was resistant to washing. Autoradiography performed after SDS-PAGE revealed specific alkylation of proteins with molecular weight of 74, 65, 56, 43 and 34 kD. These results demonstrate the applicability of using 3H-DALECK to covalently label opioid receptors.
journal_name
Life Scijournal_title
Life sciencesauthors
Szücs M,Belcheva M,Simon J,Benyhe S,Tóth G,Hepp J,Wollemann M,Medzihradszky Kdoi
10.1016/0024-3205(87)90491-7subject
Has Abstractpub_date
1987-07-13 00:00:00pages
177-84issue
2eissn
0024-3205issn
1879-0631pii
0024-3205(87)90491-7journal_volume
41pub_type
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