HTL9936 (HTL-9936) is a potent, selective M1-muscarinic acetylcholine (M1) receptor partial agonist with EC50 of 32 nM.
HTL9936 dispalys little to no activity against M2 (EC50>20 uM), M3 (EC50>20 uM), M4 (EC50=398 nM).
HTL9936 demonstrated agonist activity in pERK1/2 (EC50=32 nM), label-free dynamic mass redistribution (EC50=79 nM) and inositol phosphate (IP1) assay formats (EC5=631 nM) in CHO cells overexpressing human M1-receptor.
HTL9936 demonstrated no detectable agonism at human M2-, M3-, or M5-receptors, although partial agonist activity was observed at the human M4-receptor.
Co-administration of HTL9936 with scopolamine resulted in a dose-dependent restoration of learning and memory responses, reverses cognitive deficits in a mouse model of neurodegeneration.
