LOXITANE C

Modify Date: 2024-01-16 18:04:37

LOXITANE C Structure
LOXITANE C structure
Common Name LOXITANE C
CAS Number 54810-23-0 Molecular Weight 364.269
Density N/A Boiling Point 458.6ºC at 760 mmHg
Molecular Formula C18H19Cl2N3O Melting Point 109-110ºC
MSDS N/A Flash Point 231.1ºC

 Use of LOXITANE C


Loxapine hydrochloride is an orally active dopamine inhibitor, 5-HT receptor antagonist and also a dibenzoxazepine anti-psychotic agent[1][4].

 Names

Name 8-chloro-6-(4-methylpiperazin-1-yl)benzo[b][1,4]benzoxazepine,hydrochloride
Synonym More Synonyms

 LOXITANE C Biological Activity

Description Loxapine hydrochloride is an orally active dopamine inhibitor, 5-HT receptor antagonist and also a dibenzoxazepine anti-psychotic agent[1][4].
Related Catalog
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.

 Chemical & Physical Properties

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

 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