1262495-12-4
Chemical Structure
NPY Y2 antagonist 2
- CAS No.: 1262495-12-4
- Formula:C27H33ClF3N5O
- Molecular Weight:536.04
IUPAC Name: N-(3-chloro-4-(2-(cyclopropylmethyl)-2,8-diazaspiro[4.5]decan-8-yl)phenyl)-2-methyl-2-(4-(trifluoromethyl)pyrimidin-2-yl)propanamide
InChIKey: PZAIVSQWZAHADG-UHFFFAOYSA-N
SMILES: O=C(NC1=CC=C(C(Cl)=C1)N2CCC3(CN(CC3)CC4CC4)CC2)C(C5=NC=CC(=N5)C(F)(F)F)(C)C
Biological Activity: NPY Y2 antagonist 2 is a modulator targeting the neuropeptide Y (NPY) receptor Y2, with pKi values of 6.8 nM and 7.2 nM in human and rat brains, respectively, and demonstrating blood-brain barrier penetration. NPY Y2 antagonist 2 shows selectivity for the Y1 and Y5 receptors. NPY Y2 antagonist 2 blocks the negative feedback regulation mediated by the NPY Y2 receptor, thereby increasing endogenous NPY release and enhancing Y1 receptor activation, resulting in the modulation of central neurotransmitter release. NPY Y2 antagonist 2 exhibits moderate in vivo clearance, high free fraction in rat brain, and a favorable brain/plasma ratio and brain exposure. NPY Y2 antagonist 2 is applicable for research in conditions such as mood disorders, anxiety induced by alcohol withdrawal, and social anxiety associated with nicotine withdrawal[1].
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NPY Y2 antagonist 2 | NPY Y2 antagonist 2 is a modulator targeting the neuropeptide Y (NPY) receptor Y2, with pKi values of 6.8 nM and 7.2 nM in human and rat brains, respectively, and demonstrating blood-brain barrier penetration. NPY Y2 antagonist 2 shows selectivity for the Y1 and Y5 receptors. NPY Y2 antagonist 2 blocks the negative feedback regulation mediated by the NPY Y2 receptor, thereby increasing endogenous NPY release and enhancing Y1 receptor activation, resulting in the modulation of central neurotransmitter release. NPY Y2 antagonist 2 exhibits moderate in vivo clearance, high free fraction in rat brain, and a favorable brain/plasma ratio and brain exposure. NPY Y2 antagonist 2 is applicable for research in conditions such as mood disorders, anxiety induced by alcohol withdrawal, and social anxiety associated with nicotine withdrawal. | |||||||||||||||||||||
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Keywords
