Application of 39657-45-9, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.39657-45-9, Name is Isoxazolidine hydrochloride, molecular formula is C3H8ClNO. In a Article£¬once mentioned of 39657-45-9
Cocaine and 3beta-(4′-substituted phenyl)tropane-2beta-carboxylic acid ester and amide analogues. New high-affinity and selective compounds for the dopamine transporter
Several 2beta-carboxylic acid ester and amide analogues of cocaine and of 3beta-(4′-substituted phenyl)tropane-2beta-carboxylic acid were prepared. The binding affinities of these compounds, and of some previously prepared analogues, at the dopamine (DA), norepinephrine (NE), and serotonin (5-HT) transporters were determined. The phenyl esters of 3beta-(4′-methylphenyl)and 3beta-(4′-chlorophenyl)tropane-2beta-carboxylic acid are highly potent and highly selective for the DA transporter. The isopropyl esters of 3beta-(4′- chlorophenyl)- and 3beta-(4′-iodophenyl)tropane-2beta-carboxylic acid also possess high DA affinity and show significant DA transporter selectivity. Similarly, the phenyl and isopropyl ester analogues of cocaine are much more selective for the DA transporter than cocaine. Tertiary amide analogues of cocaine and of 3beta-(4′-substituted phenyl)tropane-2beta-carboxylic acids are more potent inhibitors of radioligand binding at the DA transporter than the primary and secondary amide analogues. In particular, 3beta-(4′- chlorophenyl)tropane-2beta-N-morpholinocarboxamide as well as the 3beta-(4′- chlorophenyl)- and 3beta-(4′-iodophenyl)tropane-2beta-N-pyrrolidinocarboxamides possess high affinity and selectivity for the DA transporter. The N,N- dimethylamide cocaine analogue is the most selective cocaine amide derivative for the DA transporter. High correlation between the inhibition of radioligand binding and inhibition of uptake at the DA, NE, and 5-HT transporter was found for a selected group of analogues. Within this group, one compound, the isopropyl ester of 3beta-(4′-iodophenyl)-tropane-2beta- carboxylic acid, was found to be more potent in the inhibition of radioligand binding than in the inhibition of DA uptake. Taken together with its high potency and selectivity at the DA transporter, this suggests that this compound may be a lead in the development of a cocaine antagonist.
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Reference£º
Oxazolidine – Wikipedia,
Oxazolidine | C3H1280NO – PubChem