PT  - JOURNAL ARTICLE
AU  - Patil, P. N.
TI  - STERIC ASPECTS OF ADRENERGIC DRUGS. VIII. OPTICAL ISOMERS OF <em>BETA</em> ADRENERGIC RECEPTOR ANTAGONISTS
DP  - 1968 Apr 01
TA  - Journal of Pharmacology and Experimental Therapeutics
PG  - 308--314
VI  - 160
IP  - 2
4099  - http://jpet.aspetjournals.org/content/160/2/308.short
4100  - http://jpet.aspetjournals.org/content/160/2/308.full
SO  - J Pharmacol Exp Ther1968 Apr 01; 160
AB  - Beta adrenergic receptor blocking actions of D and L isomers of butoxamine, INPEA, MJ 1999, pronethalol and related agents were investigated in the isolated guinea-pig tracheal chain preparation. D(-)-Isoproterenol was used as the agonist and the tissue was exposed to the antagonists for 30 min. pA2 values for (±)-pronethalol, D(-)-butoxamine, D(-)-MJ 1999 and D(-)-INPEA were 7.26, 7.23, 6.79 and 6.50, respectively. The L(+)-isomers were less active. pA2 values for L(+)-pronethalol, L(+)-MJ 1999 and L(+)-INPEA were 5.18, 5.15 and 4.22, respectively. Desoxy MJ 1999 (pA2, 3.88) appeared to be less active than L(+)-MJ 1999. L(+)-Butoxamlne and (±)-pseudobutoxamine did not produce any beta adrenergic blockade. Only D(-)-ephedrine produced significant blockade of beta adrenergic receptors; other isomers of ephedrine were inactive. Steric structure-action relationship is discussed. © 1968 by The Williams & Wilkins Company