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A serotonin-dopamine reuptake inhibitor (SDRI) is a type of drug which acts as a reuptake inhibitor of the monoamine neurotransmitters serotonin and dopamine by blocking the actions of the serotonin transporter (SERT) and dopamine transporter (DAT), respectively. This in turn leads to increased extracellular concentrations of serotonin and dopamine, and, therefore, an increase in serotonergic and dopaminergic neurotransmission. Unlike the case of other combination monoamine reuptake inhibitors such as serotonin-norepinephrine reuptake inhibitors (SNRIs) and norepinephrine-dopamine reuptake inhibitors (NDRIs), on account of the very similar chemical structures of their substrates, it is extraordinarily difficult to tease apart affinity for the DAT from the norepinephrine transporter (NET) and inhibit the reuptake of dopamine alone. As a result, selective dopamine reuptake inhibitors (DRIs) are rare, and comparably, SDRIs are even more so. In fact, only two SDRIs are well established in research at present, which are RTI-83 and UWA-101, though other related compounds are known.〔Jin C, Navarro HA, Carroll FI. Development of 3-phenyltropane analogues with high affinity for the dopamine and serotonin transporters and low affinity for the norepinephrine transporter. ''Journal of Medicinal Chemistry''. 2008 Dec 25;51(24):8048-56. PMID 19053748〕〔Jin C, Navarro HA, Ivy Carroll F. Synthesis and structure-activity relationship of 3beta-(4-alkylthio, -methylsulfinyl, and -methylsulfonylphenyl)tropane and 3beta-(4-alkylthiophenyl)nortropane derivatives for monoamine transporters. ''Bioorganic and Medicinal Chemistry''. 2009 Jul 15;17(14):5126-32. PMID 19523837〕 However, UWA-101 may also possess some activity as a releasing agent, and if so, unlike RTI-83, it would not be an SDRI in the purest sense and would also be an SDRA or serotonin-dopamine releasing agent.〔 Since bromantane acts mainly by inhibiting the reuptake of both dopamine and serotonin, it could be considered a SDRI. Manning et al. presented two high-affinity MAT-ligands with good binding selectivity for SERT and DAT, namely the 4-indolyl and 1-naphthyl arylalkylamines ''ent''-16b (Ki 0.82, 3.8, 4840 nM for SERT, DAT, NET) and ''ent''-13b respectively.〔PMID 19038547〕 ==See also== * Monoamine reuptake inhibitor * Dopamine reuptake inhibitor * Serotonin reuptake inhibitor 抄文引用元・出典: フリー百科事典『 ウィキペディア(Wikipedia)』 ■ウィキペディアで「Serotonin-dopamine reuptake inhibitor」の詳細全文を読む スポンサード リンク
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