THRX160209

THRX160209 (0.01-100 μM; 60 min) inhibits [³H] NMS radioligand binding to membranes of CHO cells expressing human mAChR subtypes, with apparent pK_i = 9.51 for M₂ receptors, apparent pK_i = 8.02 for M₁ receptors, apparent pK_i = 7.81 for M₃ receptors, apparent pK_i = 8.78 for M₄ receptors, and apparent pK_i = 7.11 for M₅ receptors^[1].
THRX160209 (0.01-100 μM; 60 min) retards the dissociation of [³H] NMS from CHO-M₂ cell membranes, with a pEC_50,diss = 6.5 for slowing radioligand dissociation^[1].
THRX160209 (0.01-100 μM; 60 min) competes with Obidoxime at the allosteric site in the extracellular vestibule of the M₂ receptor^[1].
THRX160209’s radiolabeled form [3H]THRX‑160209 exhibits a biphasic dissociation profile under infinite‑dilution assay conditions in CHO‑M2 cell membranes; the addition of orthosteric ligand atropine or allosteric ligand obidoxime converts the dissociation curve into a monophasic fast‑dissociation pattern^[2].
THRX160209 exhibits a cooperativity factor α = 2547 and pK_A = 10.2 in nonequilibrium radioligand binding assays on CHO‑M₂ cell membranes^[1].
THRX-160209 is a bitopic muscarinic receptor antagonist that exhibits significantly enhanced affinity and selectivity for the M₂ receptor^[2].