N-Desmethyl xanomeline is a pharmacologically active metabolite of Xanomeline. N-Desmethyl xanomeline binds to muscarinic, serotonergic, histaminergic and dopaminergic receptors. N-Desmethyl xanomeline can be used for the research of schizophrenia [1].
In Vitro, N-Desmethyl xanomeline (0.1 nM-10 µM) exhibits a complex polypharmacological profile with potent binding to σ1, 5-HT2B, 5-HT1D, 5-HT7, and muscarinic receptors (Ki values range from 6.2 nM to 219 nM)[1]. N-Desmethyl xanomeline (10 µM) exhibits potential agonism at multiple muscarinic, serotonergic, and histaminergic GPCRs[1]. N-Desmethyl xanomeline acts as a full or partial agonist at 5-HT1D (potencies 17-130 nM) and 5-HT1A (EC50 = 2.20 µM) receptors, and weak partial agonist at 5-HT2A, 5-HT2C, H3, and H4 receptors[1].
References:
[1]. Kensuke Sakamoto, et al. The polypharmacological profiles of xanomeline and N-desmethylxanomeline. bioRxiv. November 21, 2025.
In Vitro, N-Desmethyl xanomeline (0.1 nM-10 µM) exhibits a complex polypharmacological profile with potent binding to σ1, 5-HT2B, 5-HT1D, 5-HT7, and muscarinic receptors (Ki values range from 6.2 nM to 219 nM)[1]. N-Desmethyl xanomeline (10 µM) exhibits potential agonism at multiple muscarinic, serotonergic, and histaminergic GPCRs[1]. N-Desmethyl xanomeline acts as a full or partial agonist at 5-HT1D (potencies 17-130 nM) and 5-HT1A (EC50 = 2.20 µM) receptors, and weak partial agonist at 5-HT2A, 5-HT2C, H3, and H4 receptors[1].
References:
[1]. Kensuke Sakamoto, et al. The polypharmacological profiles of xanomeline and N-desmethylxanomeline. bioRxiv. November 21, 2025.