LY2119620 displays modest allosteric agonism and positively modulates the functional G protein–signaling ability of an agonist at the M2/M4 receptor subtypes by placing the M2 and M4 receptors into an active G protein–bound state. LY2119620 enhances the potency of three muscarinic acetylcholine receptor agonists, ACh, Oxo-M and iperoxo. [H]LY2119620 can be used as a probe for the human M(2) and M(4) muscarinic receptor allosteric binding sites.