Characterization of a light-sensitive muscarinic agonist

Muscarinic acetylcholine receptors (mAChRs) are class A GPCRs characterized by a widespread tissue distribution and involved in the control of numerous central and peripheral physiological responses. We developed an M2 photoswitchable ligand, named PAI, for the optical control of (neuro)biological functions. This dataset contains the evaluation in vitro of the photopharmacological activity of PAI. We performed calcium imaging assay in genetically unmodified M2 mAChRs receptors overexpressed in mammalian HEK cells under 1P-illumination. Oregon Green BAPTA-1, AM was used as a fluorescent calcium probe. Cytosolic calcium oscillations are indicative of M2 receptor activation and are recorded as increments of the intracellular fluorescence (F/F0). The raw data are here available: PAI turned out to be a potent activator of M2 receptors in the dark or under illumination with blue light (460 nm) or white light (trans isomer), but inactive under UV illumination (cis isomer).