LY2119620

LY2119620 is a high-affinity muscarinic M₂/M₄ receptor agonist. IC50 & Target: M₂/M₄ receptor^[1] In Vitro: LY2119620 shows a modest allosteric agonism of 23.2±2.18% and 16.8±5.01% at the M₂ and M₄ receptors, respectively. Minimal allosteric agonism (<20%) is observed for LY2119620 at the M₁, M₃, and M₅ receptors. The variable K_B of LY2119620 for the allosteric binding site on the unoccupied receptor is found to be consistently about 1.9 to 3.4 µM. Results show a B_max increase at the M₂ receptor from 793±1.95 fmol/mg to 2850±162 fmol/mg upon addition of 10 µM LY2119620, and about a 5-fold increase in B_max at the M₄ receptor, 284±18.3 fmol/mg to 1340±42.2 fmol/mg^[1].