PHAR 340 Lecture Notes - Lecture 4: Cough Medicine, Levorphanol, Angiotensin
23 Dec 2018
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Stereospecificity: i-norepinephrine is active but d-norepinephrine is not. Levorphanol is an active antitussive (no cough) and analgesic (pain relief) Dextromethorphan only an active antitussive, sterochem dn allow interaction w analgesic rs. Bulky groups: ach is less selective, methacholine more due to extra methyl group. Ne (no side chain)< e (methyl)< isoproterenol (isopropyl) most potent + active w b-adrenoceptor. Molecular rigidity: ach is flexible so can bind w 7 rs but muscarine can only act on muscarinic rs. Neostigmine more potent than phycostigmine due to charged n. Sub of key atoms: ester procaine is rapidly metabolized but procainamide metabol slowly= acts longer. Angiotensin i + ace " angiotensin ii (incr bp) Viper venom, pentapeptide (bpp5a), trp-ala-pro, phe-ala-pro inhibit ace, tripeptides mod to make commercial drug. If receptors are located everywhere is easier for drug to be less selective where as if r is only in one place in the body it is thus more selective.
