Dayang Chem (Hangzhou) Co., Ltd.
China
Product Name: Loxapine hydrochloride
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Purity: 98.0%
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54810-23-0

54810-23-0 structure

54810-23-0 structure

Name: LOXITANE C
Chemical Name: 8-chloro-6-(4-methylpiperazin-1-yl)benzo[b][1,4]benzoxazepine,hydrochloride
CAS Number: 54810-23-0
Molecular Formula: C₁₈H₁₉Cl₂N₃O
Molecular Weight: 364.269
Catalog: Signaling Pathways GPCR/G Protein 5-HT Receptor
Create Date: 2018-08-08 23:02:56
Modify Date: 2024-01-16 18:04:37
Loxapine hydrochloride is an orally active dopamine inhibitor, 5-HT receptor antagonist and also a dibenzoxazepine anti-psychotic agent[1][4].

Name	8-chloro-6-(4-methylpiperazin-1-yl)benzo[b][1,4]benzoxazepine,hydrochloride
Synonyms	2-Chloro-11-(4-methyl-1-piperazinyl)dibenz[b,f][1,4]oxazepine Monohydrochloride Desconex (TN) Dibenz[b,f][1,4]oxazepine, 2-chloro-11-(4-methyl-1-piperazinyl)-, hydrochloride (1:1) LOXITANE C 2-Chloro-11-(4-methyl-1-piperazinyl)dibenzo[b,f][1,4]oxazepine hydrochloride (1:1) Dibenz(b,f)(1,4)oxazepine,2-chloro-11-(4-methyl-1-piperazinyl)-,monohydrochloride Loxapine hydrochloride Loxapine monohydrochloride 2-Chloro-11-(4-methyl-1-piperazinyl)dibenz(b,f)(1,4)oxazepine monohydrochloride Loxapine HCl

Description	Loxapine hydrochloride is an orally active dopamine inhibitor, 5-HT receptor antagonist and also a dibenzoxazepine anti-psychotic agent[1][4].
Related Catalog	Signaling Pathways >> GPCR/G Protein >> Dopamine Receptor Signaling Pathways >> Neuronal Signaling >> Dopamine Receptor Research Areas >> Neurological Disease Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor
Target	human 5-HT2 Human D4 Receptor Human D1 Receptor Human D2 Receptor
In Vitro	In the presence of Loxapine, [3H]ketanserin binds to 5-HT2 receptor in Frontal cortex of brain in human and bovine with Ki value of 6.2 nM and 6.6 nM, respectively. Loxapine has the rank order of potency for the various receptors appears to be as follows: 5-HT2≥D4>>>D1>D2 in comparing competition experiments involving the human membranes[1]. Loxapine (0-20 μM, 24 h or 72 h) reduces IL-1β secretion by LPS-activated mixed glia cultures, reduces IL-2 secretion in mixed glia cultures, and decreases IL-1β and IL-2 secretion in LPS-induced microglia cultures[2].
In Vivo	Loxapine (5 mg/kg; i.p.; daily for 4 or 10 weeks) decreases serotonin (S2) but does not elevate dopamine (D2) receptor numbers in the rat brain[3]. Animal Model: Adult male Wistar rats (150-175 g)[3] Dosage: 5 mg/kg Administration: Intraperitoneal injection, daily for 4 or 10 weeks Result: Induced a very significant reduction (more than 50%) of serotonin (S2) receptor density after 4 weeks or 10 weeks of daily injection, but did not produce any significant increase in dopamine receptor density.
References	[1]. 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. [2]. 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. [3]. 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. [4]. Keating GM. Loxapine inhalation powder: a review of its use in the acute treatment of agitation in patients with bipolar disorder or schizophrenia. CNS Drugs. 2013 Jun;27(6):479-89.

Boiling Point	458.6ºC at 760 mmHg
Melting Point	109-110ºC
Molecular Formula	C₁₈H₁₉Cl₂N₃O
Molecular Weight	364.269
Flash Point	231.1ºC
Exact Mass	363.090515
PSA	28.07000
LogP	3.88480