Detail of "482-98-4"

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Inhibition of norepinephrine transport and reserpine binding by reserpine derivatives

Inhibition of norepinephrine transport and reserpine binding by reserpine derivatives. Parti, Rajesh; Ozkan, Eric D.; Harnadek, Gordon J.; Njus, David (Dep. Biol. Sci., Wayne State Univ., Detroit, MI 48202, USA). J. Neurochem., 48(3), 949-53 (English) 1987.There are some reagents with their cas registry numbers 118-41-2 and 51-41-2 are used in this study. CODEN: JONRA9. ISSN: 0022-3042. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) Section cross-reference(s): 2, 13 Reserpine [50-55-5], a competitive inhibitor of catecholamine transport into adrenal medullary chromaffin vesicles, consists of a trimethoxybenzoyl group esterified to an alkaloid ring system. Reserpine inhibits norepinephrine [51-41-2] transport with a Ki of ~1 nM and binds to chromaffin-vesicle membranes with a KD of about the same value. Methyl reserpate [2901-66-8] and reserpinediol [482-98-4], derivs. that incorporate the alkaloid ring system, also competitively inhibit norepinephrine transport into chromaffin vesicles with Ki values of 38 and 440 nM, resp. Similar concns. inhibit [3H]reserpine binding to chromaffin-vesicle membranes. 3,4,5-Trimethoxybenzyl alc. [3840-31-1] and 3,4,5-trimethoxybenzoic acid [118-41-2], derivs. of the other part of the reserpine mol., do not inhibit either norepinephrine transport or [3H]reserpine binding at concns. up to 100 mM. Moreover, trimethoxybenzyl alc. does not potentiate the inhibitory action of Me reserpate. Therefore, the amine binding site of the catecholamine transporter appears to bind the alkaloid ring system of reserpine rather than the trimethoxybenzoyl moiety. The more potent inhibitors are more hydrophobic compds., suggesting that the reserpine binding site is hydrophobic. .