Loxapine-d8 hydrochloride

Names

[ CAS No. ]:
1246820-19-8

[ Name ]:
Loxapine-d8 hydrochloride

[Synonym ]:
Oxilapine-d8 Hydrochloride
Loxapine-d8 Hydrochloride
2-Chloro-11-(4-methyl-1-piperazinyl)dibenz[b,f][1,4]oxazepine-d8 Hydrochloride
S-805-d8 Hydrochloride
SUM-3170-d8 Hydrochloride

Biological Activity

[Description]:

Loxapine-d8 hydrochloride is the deuterium labeled Loxapine. Loxapine Succinate is a D2DR and D4DR inhibitor, serotonergic receptor antagonist and also a dibenzoxazepine anti-psychotic agent[1][2].

[Related Catalog]:

Research Areas >> Neurological Disease
Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor
Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor

[In Vitro]

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].

[References]

[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.

[2]. Singh AN, et al. A neurochemical basis for the antipsychotic activity of loxapine: interactions with dopamine D1, D2, D4 and serotonin 5-HT2 receptor subtypes. J Psychiatry Neurosci. 1996 Jan;21(1):29-35.

[3]. Labuzek K, et al. Chlorpromazine and loxapine reduce interleukin-1beta and interleukin-2 release by rat mixed glial and microglial cell cultures. Eur Neuropsychopharmacol. 2005 Jan;15(1):23-30.

[4]. Lee T, et al. Loxapine and clozapine decrease serotonin (S2) but do not elevate dopamine (D2) receptor numbers in the rat brain. Psychiatry Res. 1984 Aug;12(4):277-85.

[5]. Kalkman HO, et al. Clozapine inhibits catalepsy induced by olanzapine and loxapine, but prolongs catalepsy induced by SCH 23390 in rats. Naunyn Schmiedebergs Arch Pharmacol. 1997 Mar;355(3):361-4.

Chemical & Physical Properties

[ Molecular Formula ]:
C18H11Cl2D8N3O

[ Molecular Weight ]:
372.31800

[ Exact Mass ]:
371.14100

[ PSA ]:
28.07000

[ LogP ]:
3.88480

Related Compounds