By Leong E. Way
Read Online or Download Endogenous and Exogenous Opiate Agonists and Antagonists. Proceedings of the International Narcotic Research Club Conference, June 11–15, 1979, North Falmouth, Massachusetts, USA PDF
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Additional info for Endogenous and Exogenous Opiate Agonists and Antagonists. Proceedings of the International Narcotic Research Club Conference, June 11–15, 1979, North Falmouth, Massachusetts, USA
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Ia = C H 2C H 2C H M e 2; Dmae = - C H 2C H 2N M e 2; DMae(O) = - C H 2C F 2N ( 0 ) M e 2 r 3 TyrD-AlaGlyMePheN(Me)la 4 235 5 M c T y r D - A1 a G1 y Me P h "e NHI a g h 65 500 1000 800 520 940 500 GPI* 14 26 15 35 44 MVD* Structure No In vitro Biological Evaluation of Analogues a c t i v i t y may b e a p r o b l e m o f d e l i v e r y , t h e compound b e i n g u n a b l e t o r e a c h t h e s i t e o f a c t i o n w i t h i n the c e n t r a l nervous system. A comparison o f the isoamyl s e r i e s (b - i ) w i t h peptides b e l i e v e d t o penetrate the b l o o d - b r a i n b a r r i e r ( e .
The effect of adding a 3-CH3 group on conformation is shown in Table II. All the geometries and isomers have a single, well-defined low enerciy conformer. For the 8 isomers (trans 3CH 3/CH 3) a <>f equatorial, N-CH 3 equatorial form is definitely preferred. These results are consistent with a x-ray structure determination of the closely related 1,4-dimethyl-3-ethyl analogue (8). For the a isomer (cis 3CH 3/4CH 3) either a c>j equatorial [ a x] or
W i l k e s and M r . A . N . A . W i l s o n t o t h i s study. REFERENCES T. BOWER, K . P . METCALF and C . F . C . S M I T H , P e p t i d e s - P r o c e e d i n g s o f t h e F i f t h A m e r i c a n / P e p t i d e Symposium,Eds. M. Goodman a n d J . M e i e n h o f e r , p p 1 1 1 - 1 1 3 , J o h n W i l e y & S o n s , I n c . , New Y o r k ( 1 9 7 7 ) . 2. KOSTERLITZ and F . M . L E S L I E , 3. 4. KOSTERLITZ and A . J . W A T T , B r i t . J . P h a r m a c . C h e m o t h e r . 33~766-276 ( 1 9 6 8 ) .