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Clozapine D8

Names

[ CAS No. ]:
1185053-50-2

[ Name ]:
Clozapine D8

[Synonym ]:
5H-Dibenzo[b,e][1,4]diazepine, 8-chloro-11-(4-methyl-1-piperazinyl-2,2,3,3,5,5,6,6-d8)-
8-Chloro-11-[4-methyl(2H8)-1-piperazinyl]-5H-dibenzo[b,e][1,4]diazepine

Biological Activity

[Description]:

Clozapine D8 (HF 1854 D8) is the deuterium labeled Clozapine. Clozapine, an antipsychotic, is a potent antagonist of dopamine and a number of other receptors, with a Ki of 9.5 nM for muscarinic M1 receptor. Clozapine is also a potent and selective agonist at the muscarinic M4 receptor (EC50=11 nM)[1][2][3][4].

[Related Catalog]:

Signaling Pathways >> Neuronal Signaling >> mAChR
Signaling Pathways >> GPCR/G Protein >> mAChR
Signaling Pathways >> GPCR/G Protein >> Dopamine Receptor
Signaling Pathways >> Neuronal Signaling >> Dopamine Receptor
Research Areas >> Neurological Disease

[References]

[1]. Seeman P, et al. Clozapine, a fast-off-D2 antipsychotic. ACS Chem Neurosci. 2014 Jan 15;5(1):24-9.

[2]. Zhukovskaya NL, et al. Clozapine downregulates 5-hydroxytryptamine6 (5-HT6) and upregulates 5-HT7 receptors in HeLa cells. Neurosci Lett. 2000 Jul 21;288(3):236-40.

[3]. Moreno JL, et al. Persistent effects of chronic clozapine on the cellular and behavioral responses to LSD in mice. Psychopharmacology (Berl). 2013 Jan;225(1):217-26.

[4]. Zorn SH, et al. Clozapine is a potent and selective muscarinic M4 receptor agonist. Eur J Pharmacol. 1994 Nov 15;269(3):R1-2.

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Boiling Point ]:
489.2±55.0 °C at 760 mmHg

[ Molecular Formula ]:
C18H11D8ClN4

[ Molecular Weight ]:
334.873

[ Flash Point ]:
249.6±31.5 °C

[ Exact Mass ]:
334.180023

[ LogP ]:
2.36

[ Vapour Pressure ]:
0.0±1.2 mmHg at 25°C

[ Index of Refraction ]:
1.681

[ Storage condition ]:
-20°C

Related Compounds