A series of N-aryl-N'-(1-methyl-2-pyrrolidinylidene)ureas was prepared and screened for pharmacological activity. Congeners possessing either phenyl or phenyl substituted with 4-nitro, 3-bromo, 3-chloro, 3-fluoro, and 3-methyl groups were found to demonstrate anxiolytic activity. 2,6-Disubstitution of the phenyl ring with methyl, chloro, and bromo imparted potent muscle-relaxant properties which appear to be centrally mediated. A significant separation of the anxiolytic and muscle-relaxant properties from other CNS activities, e.g., anticonvulsant, sedative, and hypnotic, was achieved.
By using a structured development process, the authors were able to create valid evaluation items for determining resident acquisition of the ACGME GCs.
A series of (imidazolylmethyl)oxazoles and -thiazoles were prepared and evaluated as alpha(2) adrenoceptor agonists. These compounds were also tested in in vivo paradigms that are predictive of analgesic activity. Variations in both the imidazole and thiazole portions of the molecule were investigated. Some of the more potent compounds such as 22, 26, 45, and 53 displayed alpha(2) receptor binding in the 10-20 nM range and also had significant antinociceptive activity in the mouse abdominal irritant test (MAIT).
EM residents from several residency programs showed statistically significant progressive acquisition of the ACGME GCs using a global assessment device. This suggests that the GCs may be an intrinsic component in the training of EM residents.
In an e f f o r t t o p r o t e c t xilobam from t h e e f f e c t s of h i g h temperatures and h i g h h u m i d i t i e s w i t h o u t a d v e r s e l y a f f e c t i n g i t s d i s s o l u t i o n from t a b l e t s , t h r e e a r y l s u l f o n i c a c i d s a l t s and t h e s a c c h a r i n s a l t were p r e p a r e d . A l l o f t h e s a l t s were determined t o be more s t a b l e a t 74% r e l a t i v e humidity and 70' t h a n t h e f r e e b a s e .I n s p i t e of t h e l a r g e d i f f e r e n c e s between t h e e f f e c t of h i g h humidity a t a h i g h temperature on t h e s a l t s v e r s u s t h e f r e e b a s e , t h e
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