PD 102807

PD 102807 is a M4 muscarinic receptor antagonist with an IC₅₀ of 90.7 nM. PD 102807 inhibits M1, M2, M3, M5 muscarinic receptor with IC₅₀s of 6558.7, 3440.7, 950.0, and 7411.7 nM, respectively^[1]. Antidyskinetic effect. 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^[1].
PD 102807, a novel M4 selective antagonist, counteracts the M4 receptor-induced stimulation of [³⁵S]-GTPγS binding to membrane G proteins with a pK_B of 7.40, a value which is 63-, 33- and 10-fold higher than those display at M1 (pK_B=5.60), M2 (pK_B=5.88) and M3 (pK_B=6.39) receptor subtypes, respectively^[2].
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^[3]. 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^[3].