Journal of Medicinal Chemistry p. 1261 - 1263 (1981)
Update date:2022-07-29
Topics:
Taylor, Clinton A.
Smith, Howard E.
Goldberg, Michael R.
Robertson, David
The enantiomers of a number of catecholamines, including (αS)- and (αR)-erythro-α-methylepinephrine, were evaluated for their capacity to compete for binding sites in rat forebrain homogenates with <(3)H>prazosin, a ligand which selectively binds to adrenergic receptors of the α1 subtype. (αR)-erythro-α-Methylepinephrine is devoid of apparent biological activity, but the activity of the αS isomer is substantial.The latter is less active than the endogeneous catecholamines, (R)-norepinephrine and (R)-epinephrine, but the stereospecific competition for <(3)H>prazosin binding sites by the catecholamine isomers with the βR configuration is additional evidence that (αS)-erythro-α-methylepinephrine may be a biologically active metabolite of L-α-methyl-3,4-dihydroxyphenylalanine.
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