Abstract:
:The enkephalin analogs, [D-Pen2,L-Cys5]- and [D-Pen2,D-Cys5]-enkephalin are cyclic compounds, conformationally constrained by virtue of their 14-membered, disulfide containing rings and by the rigidizing effect of the beta, beta dimethyl substituents of the penicillamine side chain. The analogs exhibit profound delta receptor specificity as assessed by their relative potencies in the guinea pig ileum (GPI) and mouse vas deferens (MVD) assays, exhibiting, respectively, 666 and 215 times higher potency in the latter assay system. By contrast, the receptor selectivities measured in rat brain binding assays in the absence of sodium were much more modest, the cyclic analogs being, respectively, 15.2 and 6.0 times more effective at displacing [3H] [D-Ala2,D-Leu5]enkephalin than [3H]naloxone. However, for binding assays performed in the presence of a sodium concentration equivalent to that used in the GPI and MVD assays, these binding selectivities increased to 167 and 49, respectively.
journal_name
Life Scijournal_title
Life sciencesauthors
Mosberg HI,Hurst R,Hruby VJ,Galligan JJ,Burks TF,Gee K,Yamamura HIdoi
10.1016/0024-3205(83)90239-4subject
Has Abstractpub_date
1983-05-30 00:00:00pages
2565-9issue
22eissn
0024-3205issn
1879-0631pii
0024-3205(83)90239-4journal_volume
32pub_type
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