VU0152100

VU0152100

CAT N°: 32968
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From 142.00 120.70

VU0152100 is a positive allosteric modulator of M4 muscarinic acetylcholine receptors.{61171} It potentiates calcium mobilization induced by acetylcholine (ACh) in CHO-K1 cells expressing the rat M4 receptor with an EC50 value of 380 nM. VU0152100 is selective for M4 over M1, M2, M3 and M5 receptors, as well as a panel of 68 additional GPCRs, ion channels, transporters, and enzymes, but does bind to the benzodiazepine binding site of the GABAA receptor at 10 µM. It reduces cocaine-induced increases in locomotor activity and cocaine self-administration in mice when administered at a dose of 1 mg/kg.{61172}

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