EPPTB (Synonyms: Ro 5212773) |
| Catalog No.GC50062 |
EPPTB(EPPTB)는 강력하고 선택적인 미량 아민 관련 수용체 1(TAAR1) 길항제(마우스 TAAR1의 경우 Ki=0.9nM)이며, 다른 TAAR에는 유의미한 영향이 없습니다.
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Cas No.: 1110781-88-8
Sample solution is provided at 25 µL, 10mM.
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Trace amine 1 (TA1) receptor antagonist/inverse agonist; exhibits a higher potency at the mouse TA1 receptor than the rat and human TA1 receptors (IC50 values are 27.5, 4539 and 7487 nM, respectively). Blocks the TA1 receptor-mediated activation of an inwardly rectifying K+ current, which increases the firing frequency of dopamine (DA) neurons in the ventral tegmental area. Increases DA potency at the D2 receptor. Also displays inverse agonism, reducing basal cAMP levels in vitro (IC50 = 19 nM).
Bradaia et al (2009) The selective antagonist EPPTB reveals TAAR1-mediated regulatory mechanisms in DArgic neurons of the mesolimbic system. Proc.Natl.Acad.Sci.U.S.A. 106 20081 PMID:19892733
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