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CAS No. : 23062-91-1
MCE 国际站:PD 102807
产品活性:PD 102807 是一种 M4 毒蕈碱受体拮抗剂,IC50 为 90.7 nM。PD 102807 抑制 M1、M2、M3、M5 毒蕈碱受体,IC50 分别为 6558.7、3440.7、950.0 和 7411.7 nM。具有抗运动障碍作用。
研究领域:GPCR/G Protein | Neuronal Signaling
作用靶点:mAChR
In Vitro: PD 102807 (example 1) shows selectivity for M4 muscarinic receptor with 72-fold (M1), 38-fold (M2), 10-fold (M3), and 82-fold (M5) more selective compared to the other receptors.
PD 102807, a novel M4 selective antagonist, counteracts the M4 receptor-induced stimulation of [35S]-GTPγS binding to membrane G proteins with a pKB of 7.40, a value which is 63-, 33- and 10-fold higher than those display at M1 (pKB=5.60), M2 (pKB=5.88) and M3 (pKB=6.39) receptor subtypes, respectively.
PD-102807 is an M4 mAChR preferring antagonist, with 7-28 nM affinity for M4 mAChRs, a 14-36-fold selectivity for M4 over M3 mAChRs, and 76-2600-fold selectivity for M4 over M1, M2 and M5 mAChRs.
In Vivo: Striatal perfusion of PD-102807 (3 μM) alleviates levodopa-induced dyskinesia (LID) and inhibits nigral GABA and Glu along with striatal Glu release.
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