By Leong E. Way

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Extra 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

Example text

One of these two conformers could represent the resting state (or non-induced) form of the anionic receptor site which interacts only with the cationic site of the fused ring opiate without a major deformation of either the N-substituent or of the anionic site. Such an interaction could be responsible for agonist activity. In the 3-methylfuryl analogue which forms a pure antagonist in the benzomorphan series, low-energy N-substituent conformers bind best to another conformation of the phosphate with ii* = 117°, which could correspond to a change in receptor conformation preventing agonist activity.

1 ) have found that c e r e b r o s i d e s u l f a t e , another sphingosine l i p i d , is capable of stereospecific binding of opiates, our f i n d i n g suggested that opiate binding in premature lung c o u l d be due t o t h e p r e s e n c e o f c e r e b r o s i d e s u l f a t e , or other s i m i l a r sphingolipid. We t h e r e f o r e undertook a p a r a l l e l analysis of the lipid c o m p o s i t i o n i n e m b r y o n i c l u n g a n d i n b r a i n i n s e a r c h o f a common s p h i n g o l i p i d w i t h which o p i a t e b i n d i n g might be associated.

A . J . NIEMEGEERS a n d J . G . H . D O N Y , A r z n e i m T o r s c h . 13 502-507 ( 1 9 6 3 ) . ~ 5. 6. HENDERSHOT a n d J . F O R S A I T H . J . P h a i m a c . E x p . T h e r . 1 2 5 2 3 7 - 2 4 0 ( 1 9 5 9 ) . RANCE and C . F . C . S M I T H T T t e t u r e 262 782-783 (1976). JOHNSON and N . T . B O Y D E N , B i o c h e m . P h a r m a c o l . 27 8 4 3 - 8 4 8 (1978). MALFROY, J . P . SCHWARTZ, N a t u r e 276 523-526 ( 1 9 7 8 ) . A . S . V . ROBERTS and J . F E E N E Y , N a t u r e 253 753-755 ( 1 9 7 5 ) .

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