N-Desmethylclozapine-d8 (hydrochloride)

N-Desmethylclozapine-d8 (hydrochloride) is the deuterium labeled N-Desmethylclozapine hydrochloride. N-Desmethylclozapine hydrochloride is a major active metabolite of the atypical antipsychotic agent Clozapine. N-Desmethylclozapine hydrochloride is a potent, allosteric and partial M1 receptors agonist (EC50=115 nM) and is able to potentiate hippocampal N-methyl-d-aspartate (NMDA) receptor currents through M1 receptor activation. N-Desmethylclozapine hydrochloride is also a δ-opioid agonist[1][2][3].

Product Specifications

CAS Number

[2705402-91-9]

Product Name Alternative

Norclozapine-d8 (hydrochloride) ; Desmethylclozapine-d8 (hydrochloride) ; Normethylclozapine-d8 (hydrochloride)

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Drug Metabolite; mAChR; Opioid Receptor; Virus Protease

Type

Isotope-Labeled Compounds

Related Pathways

Anti-infection; GPCR/G Protein; Metabolic Enzyme/Protease; Neuronal Signaling

Applications

COVID-19-anti-virus

Field of Research

Infection

Purity

99.74

Solubility

10 mM in DMSO|DMSO : ≥ 50mg/mL

Smiles

ClC1=CC=C2NC3=CC=CC=C3C(N4C([2H])([2H])C([2H])([2H])NC([2H])([2H])C4([2H])[2H])=NC2=C1.[H]Cl

Molecular Formula

C17H10D8Cl2N4

Molecular Weight

357.31

Precautions

H302, H315, H319, H335

References & Citations

[1]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53 (2) :211-216.|[2]Li Z, et al. N-desmethylclozapine, a major metabolite of clozapine, increases cortical acetylcholine and dopamine release in vivo via stimulation of M1 muscarinic receptors. Neuropsychopharmacology. 2005 Nov;30 (11) :1986-95.|[3]Odagaki Y, et al. Comparative analysis of pharmacological properties of xanomeline and N-desmethylclozapine in rat brain membranes. J Psychopharmacol. 2016 Sep;30 (9) :896-912.