2002495-17-0
Chemical Structure
VU6001221
- CAS No.: 2002495-17-0
- Formula:C20H26ClN3O3
- Molecular Weight:391.89
IUPAC Name: 4-chloro-N-((3-isopropylisoxazol-5-yl)methyl)-3-((1-methylpiperidin-4-yl)oxy)benzamide
InChIKey: IMOCLELOJXGLLE-UHFFFAOYSA-N
SMILES: O=C(NCC1=CC(C(C)C)=NO1)C2=CC=C(Cl)C(OC3CCN(C)CC3)=C2
Biological Activity: VU6001221 is a blood-brain barrier permeable Choline Transporter (CHT) inhibitor (IC50 = 270 nM). VU6001221 increases the likelihood of extracellular choline elevation activating synaptic α7 nicotine ACh receptors. VU6001221 attenuates potassium-induced ACh levels in the prefrontal cortex[1][2].
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VU6001221 | VU6001221 is a blood-brain barrier permeable Choline Transporter (CHT) inhibitor (IC50 = 270 nM). VU6001221 increases the likelihood of extracellular choline elevation activating synaptic α7 nicotine ACh receptors. VU6001221 attenuates potassium-induced ACh levels in the prefrontal cortex. | |||||||||||||||||||||
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- [1]. Bertron JL, et al. Optimization of the choline transporter (CHT) inhibitor ML352: Development of VU6001221, an improved in vivo tool compound. Bioorg Med Chem Lett. 2016 Oct 1;26(19):4637-4640. [Content Brief]
- [2]. Koshy Cherian A, et al. Unresponsive Choline Transporter as a Trait Neuromarker and a Causal Mediator of Bottom-Up Attentional Biases. J Neurosci. 2017 Mar 15;37(11):2947-2959. [Content Brief]
Keywords
