Morphinomimetic activity of synthetic fragments of beta-lipotropin and analogs. | Zendy

Nicholas Ling | Zendy; Roger Guillemin | Zendy

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Morphinomimetic activity of synthetic fragments of beta-lipotropin and analogs.

Author(s) -

Nicholas Ling,

Roger Guillemin

Publication year - 1976

Publication title -

proceedings of the national academy of sciences

Language(s) - English

Resource type - Journals

eISSN - 1091-6490

pISSN - 0027-8424

DOI - 10.1073/pnas.73.9.3308

Subject(s) - potency , beta (programming language) , enkephalin , chemistry , bioassay , endocrinology , alpha (finance) , beta endorphin , medicine , pharmacology , biochemistry , biology , in vitro , opioid , construct validity , receptor , nursing , computer science , patient satisfaction , genetics , programming language

In the myenteric plexus-longitudinal muscle bioassay, beta-endorphin, i.e., beta-lipotropin (beta-LPH)-[61-91], has a potency of 450 with confidence limits of 281-966 when Met5-enkephalin is used as a reference standard with a potency of 100. The primary amide and the ethylamide of Met5-enkephalin have potencies statistically overlapping with that of beta-endorphin. The primary amide of alpha-endorphin has twice the potency of the free acid form of alpha-endorphin. An intact NH2-terminal tyrosine is not necessary for full intrinsic activity. The shortest fragment of beta-LPH with morphinomimetic activity is beta-LPH-[61-64].

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