Detail of "6970-83-8"

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Carbamate prodrugs of phenylethylamines: a neurochemical investigation

Carbamate prodrugs of phenylethylamines: a neurochemical investigation. Baker, G. B.; Coutts, R.Several substances are used for example 93528-35-9 which is its cas registry number. T.; Nazarali, A. J.; Danielson, T. J.; Rubens, M. (Dep. Psychiatry, Univ. Alberta, Edmonton, AB T6G 2G3, Can.). Proc. West. Pharmacol. Soc., 27, 523-5 (English) 1984. CODEN: PWPSA8. ISSN: 0083-8969. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) Following i.p. administration of the carbamate prodrugs N-ethoxycarbonylamphetamine (I) [93528-35-9] and N-ethoxycarbonyltranylcypromine (II) [91640-64-1], both at 0.1 mmole/kg to rats, the brain levels of the free drugs amphetamine [300-62-9] and tranylcypromine [155-09-9] were 9.95 and 8.95 nmole/g, resp., 1 h after the drug administration; the resp. levels of I and II in the brain were 4.15 and 4.83 nmole/g. One h after i.p. injection of 0.5 mmole N-ethoxycarbonylphenylethylamine (III) [6970-83-8] to rats, the resp. brain levels of III and phenylethylamine [64-04-0] were 15.6 nmoles/g and 190 pmoles/g; when PEA-HCl (0.5 mmole) was injected, 835 pmoles PEA/g was found in the brain. II injection inhibited brain MAO [9001-66-5]-A and -B by 79.1 and 93.4%, resp. In vitro, II at concns. equiv. to the levels of tranylcypromine found in vivo, caused 11.7% inhibition of MAO-A and no inhibition of MAO-B; tranylcypromine caused 83.9 and 99.0% inhibition, resp. Thus, it appears that the MAO inhibiting activity of II in vivo is due to the tranylcypromine formed from the prodrug. Apparently, carbamate analogs are useful prodrugs of bioactive amines. .