194038-94-3
194038-94-3
Chemical Structure
RBI257
- CAS No.: 194038-94-3
- Formula:C21H28IN3O
- Molecular Weight:465.38
IUPAC Name: N-(1-(4-iodobenzyl)piperidin-4-yl)-3-isopropoxy-N-methylpyridin-2-amine
InChIKey: ZJAXDNQQFMPNAV-UHFFFAOYSA-N
SMILES: IC1=CC=C(C=C1)CN2CCC(N(C3=NC=CC=C3OC(C)C)C)CC2
Biological Activity: RBI257 is a selective dopamine D4R antagonist with a pKi of 8.42 for the hD4.4 receptor. RBI257 acts as a competitive antagonist at the hD4.4 receptor, blocking dopamine-stimulated G protein activation and GIRK current activation. RBI257 can be used for research on hypertension and schizophrenia[1][2][3].
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RBI257 | RBI257 is a selective dopamine D4R antagonist with a pKi of 8.42 for the hD4.4 receptor. RBI257 acts as a competitive antagonist at the hD4.4 receptor, blocking dopamine-stimulated G protein activation and GIRK current activation. RBI257 can be used for research on hypertension and schizophrenia. | |||||||||||||||||||||
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References
- [1]. Pedrosa R, et al. Dopamine D3 receptor-mediated inhibition of Na+/H+ exchanger activity in normotensive and spontaneously hypertensive rat proximal tubular epithelial cells. British journal of pharmacology. 2004 Aug;142(8):1343-53.
- [2]. Moran-Gates T, et al. Repeated antipsychotic drug exposure in developing rats: dopamine receptor effects. Synapse (New York, N.Y.). 2006 Feb;59(2):92-100.
- [3]. Newman-Tancredi A, et al. Agonist and antagonist properties of antipsychotics at human dopamine D4.4 receptors: G-protein activation and K+ channel modulation in transfected cells. The international journal of neuropsychopharmacology. 2008 May;11(3):293-307.
