Inhibition of plasma membrane monoamine transporters by β-ketoamphetamines
作者： Nicholas V Cozzi , Michael K Sievert , Alexander T Shulgin , Peyton Jacob , Arnold E Ruoho
DOI: 10.1016/S0014-2999(99)00538-5
关键词:
摘要: Methcathinone and methylone, the beta-ketone analogues of methamphetamine 3,4-methylenedioxymethamphetamine (MDMA), respectively, were tested for neurotransmitter uptake inhibition in vitro. The beta-ketones threefold less potent than nonketo drugs at inhibiting platelet serotonin accumulation, with IC(50)'s 34.6+/-4.8 microM 5.8+/-0.7 microM, respectively. methylone similar potency to MDMA catecholamine transporters individually expressed transfected glial cells. For dopamine uptake, 0.36+/-0.06 0.82+/-0.17 respectively; noradrenaline IC(50) values 0.51+/-0.10 1. 2+/-0.1 In chromaffin granules, accumulation 112+/-8.0 methcathinone 166+/-12 10-fold higher respective MDMA. Our results indicate that potently inhibit plasma membrane but only weakly vesicle transporter.
maps.org
elsevier.com参考文章(22)
D. Marona-Lewicka, Xuemei Huang, D. E. Nichols, M. P. Johnson, Novel serotonergic agents Drug Design and Discovery. ,vol. 9, pp. 299- 312 ,(1993)
Mildred C Rebstock, Yvon J L'italien, Methylaminopropiophenone compounds and methods for producing the same ,(1954)
Gary Rudnick, Stephen C. Wall, Non-neurotoxic amphetamine derivatives release serotonin through serotonin transporters Molecular Pharmacology. ,vol. 43, pp. 271- 276 ,(1993)
Annette E. Fleckenstein, Glen R. Hanson, James W. Gibb, Melanie P. Gygi, Role of Endogenous Dopamine in the Neurochemical Deficits Induced by Methcathinone Journal of Pharmacology and Experimental Therapeutics. ,vol. 283, pp. 1350- 1355 ,(1997)
Michael P. Johnson, Paul F. Conarty, David E. Nichols, [3H]Monoamine releasing and uptake inhibition properties of 3,4-methylenedioxymethamphetaimne and p-chloroamphetamine analogues European Journal of Pharmacology. ,vol. 200, pp. 9- 16 ,(1991) , 10.1016/0014-2999(91)90659-E
G. Rudnick, S. C. Wall, The molecular mechanism of "ecstasy" [3,4-methylenedioxy-methamphetamine (MDMA)]: serotonin transporters are targets for MDMA-induced serotonin release. Proceedings of the National Academy of Sciences of the United States of America. ,vol. 89, pp. 1817- 1821 ,(1992) , 10.1073/PNAS.89.5.1817
Michael P. Johnson, Andrew J. Hoffman, David E. Nichols, Effects of enantiomers of MDA, MDMA and related analogues on [3H]serotonin and [3H]dopamine release from superfused rat brain slices European Journal of Pharmacology. ,vol. 132, pp. 269- 276 ,(1986) , 10.1016/0014-2999(86)90615-1
D. M. PATON, Mechanism of efflux of noradrenaline from adrenergic nerves in rabbit atria. British Journal of Pharmacology. ,vol. 49, pp. 614- 627 ,(1973) , 10.1111/J.1476-5381.1973.TB08537.X
David Sulzer, Stephen Rayport, Amphetamine and other psychostimulants reduce pH gradients in midbrain dopaminergic neurons and chromaffin granules: a mechanism of action. Neuron. ,vol. 5, pp. 797- 808 ,(1990) , 10.1016/0896-6273(90)90339-H
Dennis J. McKenna, X.-M. Guan, A.T. Shulgin, 3,4-Methylenedioxyamphetamine (MDA) analogues exhibit differential effects on synaptosomal release of 3H-dopamine and 3H-5-hydroxytryptamine. Pharmacology, Biochemistry and Behavior. ,vol. 38, pp. 505- 512 ,(1991) , 10.1016/0091-3057(91)90005-M