Monoamine transporters (MATs) belong to the solute carrier 6 (SLC6) family of human transporters, which, in turn, is a subfamily of the broader neurotransmitter:sodium symporters (NSSs) that comprise transporters from prokaryotic to human. MATs comprise three main members-the dopamine (DA) transporter (DAT), serotonin transporter (SERT) and norepinephrine transporter (NET). MATs regulate neurotransmission via the reuptake of dopamine, serotonin and norepinephrine from extra-neuronal regions and thus maintain neurotransmitter homeostasis.
MATs are transmembrane proteins located in plasma membranes of monoaminergic neurons. These proteins use ion (Na+, Cl−) gradients as energy sources to move monoamines into or out of neurons. In the membrane of intracellular synaptic vesicles is the vesicular monoamine transporters 1 and 2 (VMAT1 and VMAT2), which use a proton gradient as the energy source to sequester cytosolic monoamines into the vesicles and then release the monoamines into synaptic cleft by exocytosis. Dysregulation of MATs has been linked to depression, anxiety disorder, attention-deficit-hyperactivity disorder, obsessive-compulsive disorder, substance-use disorders, epilepsy, Parkinson’s disease and autism-spectrum disorder. Thus, MATs serve as pharmacological targets for several neuropsychiatric and neurodegenerative disorders.
货号 | 产品名 | Cas | 产品描述 |
---|---|---|---|
PL07513 | (+)-Tetrabenazine | 1026016-83-0 | (+)-Tetrabenazine ((+)-TBZ; (3R,11bR)-TBZ; (3R,11bR)-Tetrabenazine) 是一个可逆转的VMAT-2的抑制剂。 |
PL07512 | FFN200 dihydrochloride | 2080306-27-8 | FFN200 dihydrochloride 是 VMAT2 的一个荧光第五,在神经元细胞和脑组织中选择性的微量单胺胞吐。测定FFN200 荧光和发射波长最大值分别为 352 nm 和 451 nm。 |
PL07510 | hENT4-IN-1 | 949467-71-4 | hENT4-IN-1 是一种有效且选择性的人源 ENT4 (平衡核苷转运体 4) 抑制剂,IC50 为 74.4 nM。 |
PC54512 | Lazabemide | 103878-84-8 | Lazabemide (Ro 19-6327) 是单胺氧化酶 B (MAO-B) 的选择性的可逆抑制剂 (IC50=0.03 μM),但对 MAO-A (IC50>100 μM) 活性较低。高浓度 Lazabemide 具有抑制单胺摄取的作用,抑制去甲肾上腺素、血清素和多巴胺摄取的 IC50 值分别为 86 μM、123 μM 和 >500 μM。Lazabemide 可用于帕金森和阿尔茨海默病的研究。 |
PL07515 | NBI-98782 | 85081-18-1 | NBI-98782(alpha-dihydrotetrabenazine)是囊泡单胺转运体(VMAT2)抑制剂,Ki为0.97nM。 |
PL07516 | Nisoxetine | 53179-07-0 | Nisoxetine 是一种有效的和选择性的去甲肾上腺素转运蛋白 (NET) 抑制剂,Kd 值为 0.76 nM。Nisoxetine 是一种抗抑郁试剂和局部麻药,它可以阻断电压门控性钠通道。 |
PL07517 | Radafaxine hydrochloride | 106083-71-0 | Radafaxine hydrochloride (GW-353162A) 是 bupropion 的代谢活化物,DAT/NET 转运体抑制剂,能选择性的抑制去甲肾上腺素的再吸收。 |
PC11915 | Reserpine hydrochloride | 16994-56-2 | 囊泡单胺转运蛋白(VMAT)的阻断剂,Reserpine (hydrochloride) 是囊泡单胺转运蛋白 2 (VMAT2) 的抑制剂。 |
PL07511 | Reserpine-d9 | 84759-11-5 | Reserpine-d9 是 Reserpine 的氘代物。Reserpine 是囊泡单胺转运蛋白 2 (VMAT2) 的抑制剂。 |
PL07514 | Tetrabenazine Racemate | 718635-93-9 | Tetrabenazine Racemate (Ro 1-9569 Racemate) 是一个有选择性和可逆转的VMAT-2抑制剂。 |
PL07519 | Tetrabenazine-d6 | 1392826-25-3 | Tetrabenazine-d6 是Tetrabenazine 的氘代物。 |
PL07518 | Valbenazine | 1025504-45-3 | Valbenazine (NBI-98854) 是一种囊泡单胺类转运 2 (VMAT2) 抑制剂,Ki 为 110-190 nM。 |