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Tertiary 3- and 4-haloalkylamine analogues of oxotremorine as prodrugs of potent muscarinic agonists.
J Med Chem
January 1988
Department of Pharmacology, School of Medicine, University of California, Los Angeles 90024-1735.
A series of tertiary 3- and 4-haloalkylamines related to the muscarinic agent oxotremorine was synthesized. The compounds cyclized in neutral aqueous solution to quaternary ammonium salts, which, in contrast to the parent haloalkylamines, were potent muscarinic agonists in vitro. When administered systemically to mice, the haloalkylamines produced central (tremor and analgesia) and peripheral (salivation) muscarinic effects.
View Article and Find Full Text PDFPharmacokinetics of haloalkylamines: cyclization and distribution in blood in vitro and in vivo.
J Pharm Pharmacol
May 1975
The cyclization of N-(5-chloropentyl)-N-methylaminoaceto-2,6-xylidide hydrochloride (RAD 150) and N-(5-bromopentyl)-N-methylamino-aceto-2,6-xylide hydrobromide (RAD 154) in red blood cells of rats and rabbits was examined under in vitro and in vivo conditions. The rate of cyclization was much slower in plasma and blood than in a buffer solution, probably due to influence of protein binding of the compounds. The tertiary amines disappeared rapidly from the blood cells in vitro and in vivo and the piperidinium derivative (RAD 179) formed from the haloalkylamines disappeared almost as rapidly as the tertiary amines from the plasma in vivo.
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