Clozapine N-oxide dihydrochloride
Names
[ CAS No. ]:
2250025-93-3
[ Name ]:
Clozapine N-oxide dihydrochloride
Biological Activity
[Description]:
Clozapine N-oxide dihydrochloride is a major metabolite of Clozapine and a human muscarinic designer receptors (DREADDs) agonist. Clozapine N-oxide dihydrochloride specifically activates the DREADD receptor hM3Dq. Clozapine N-oxide dihydrochloride can cross the blood-brain barrier[1][2][3]. Clozapine is a potent dopamine antagonist and also a potent and selective muscarinic M4 receptor (EC50=11 nM) agonist[4][5].
[Related Catalog]:
[Target]
Human muscarinic designer receptors (DREADDs)[1]
[In Vitro]
Clozapine N-oxide (CNO) can bind to non-DREADD receptors at concentrations required for DREADD activation, and undergoes reverse-metabolism to its parent compound clozapine, an atypical antipsychotic that acts at a variety of pharmacological targets and produces numerous physiological and behavioral effects[2].
[In Vivo]
After a single intraperitoneal (i.p.) injection of Clozapine N-oxide (1 mg/kg) into mice, Clozapine N-oxide (CNO) plasma levels peak at 15 min and are very low after 2 h. Despite the short plasma half-life of CNO in mice, the biological effects that have been described after acute treatment of DREADD-expressing experimental animals are usually much longer (6-10 h)[1].
[References]
Chemical & Physical Properties
[ Molecular Formula ]:
C18H21Cl3N4O
[ Molecular Weight ]:
415.74