New PDF release: Annual reports in medicinal chemistry. / Volume 9

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I most of which a r e p a r t i a l s t r u c t u r e s , appeared. 52 An e f f i c i e n t p r o c e s s f o r t h e p r e p a r a t i o n of v a r i o u s secondary and t e r t i a 8 ly5ergamides and t h e corresponding d i - and t e t r a h y d r o d e r i v a Nu-Demethylation o f l y s e r g i c a c i d diethylamide (LSD) was t i v e s was d e s ribed. -'5 A convenient p r e p a r a t i o n o f t h e t 7 t g l y s e r g i c a c i d e s t e r 15 from t h e corresponding N-oxide 1L;was d i s c l o s e d .

Thus, he postulated t h a t a long-acting antagonist could "immunize" an addict from the subjective e f f e c t s of o p i a t e abuse. e_ Naloxone, although a "pure" antagonist, has a short duration and poor o r a l a c t i v i t y . Hence, a 24-hour o r a l blocking dose must be measured i n grams. Thus, considerations of cost and p a l a t a b i l i t y would tend t o r u l e out t h i s substance. Cyclazocine has a d e s i r a b l e duration of a c t i o n (about 24 hours) and good o r a l a c t i v i t y .

135. L. N e m n , M. Lutz, M. Could, and E. Domino, Science, & I 831 (1972). 136. P. Bailey and S. Pradhan, Neurophannacology, &I 137. I. Cavero, J. Buckley and B. Jandhyala, Eur. J. , 3 243 (1973). 138. C. Nahas, I. Schwartz, J. Adanec, and W. Manger, Proc. Soc. Exp. Biol. , && 58 (1973). 169 (1073). 139. I% Biwfngham, Brit. J. P h a m c o l . , 140. W. Roth, J. Tinklenberg, B. Kopell, and L. H o l l i s t e r , C l i n Pharmacol. , 533 (1973). 3 671 (1972). 141. J. Weiss, A. Watanabe, L. Lcmberger, N.

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