β‐Endorphin: synthesis and properties of analogs modified in positions 8 and 31
1982; Wiley; Volume: 20; Issue: 1 Linguagem: Inglês
10.1111/j.1399-3011.1982.tb02650.x
ISSN0367-8377
AutoresDonald Yamashiro, Pierre Nicolas, Choh Hao Li,
Tópico(s)Receptor Mechanisms and Signaling
ResumoFour analogs of human β‐endorphin (β h ‐EP) were synthesized by the solid‐phase method: [Gln 8.31 ]‐β h ‐EP(I), [Arg 8 , Gln 31 ] ‐β h ‐EP(II), [Ala 8 , Gln 31 ] ‐β h ‐EP (III), and [Val 8 , Gln 31 ]‐β h ‐EP(IV). Radioreceptor binding assay with use of tritiated β h ‐EP as primary ligand gave relative potencies as follows: β h ‐EP, 100; I, 200; II, 150; III, 150; IV, 120. Relative potencies in an analgesic assay were: β h ‐EP, 100; 1,236; II, 254;III, 116; IV, 121. The side‐chain of Glu‐8 in β h ‐EP can be replaced by a variety of structures without diminishing biological activity.
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