Chemical Name: 5-Amino-N-[(3-fluoro-4-methoxyphenyl)methyl]-3,4-dimethylthieno[2,3-c]pyridazine-6-carboxamide
Biological ActivityPotent and selective positive allosteric modulator of M4 receptor; potentiates activity of ACh at M4 (EC50 values are 26.6 and 78.8 nM at rat and human M4 receptors, respectively). Exhibits selectivity for M4 over human and rat M1-3, 5, and a panel of 200 other pharmacological targets. Displays efficacy in a rat model of antipsychotic activity. Orally bioavailable and brain penetrant.
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Discovery of VU0467485/AZ13713945: an M4 PAM evaluated as a preclinical candidate for the treatment of schizophrenia.
Wood et al.
ACS Med.Chem.Lett., 2016;8:233
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