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27833-64-3

27833-64-3 structure

Name: Loxapine succinate
Chemical Name: loxapine succinate
CAS Number: 27833-64-3
Molecular Formula: C₂₂H₂₄ClN₃O₅
Molecular Weight: 445.896
Catalog: Biochemical Inhibitor Neuronal Signaling 5-HT Receptor Antagonist
Create Date: 2018-03-22 08:00:00
Modify Date: 2024-01-03 08:05:00
Loxapine Succinate is a D2DR and D4DR inhibitor, serotonergic receptor antagonist and also a dibenzoxazepine anti-psychotic agent.IC50 value: Target: D2DR/D4DR; 5-HT receptorin 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 0.2 μM, 2 μM and 20 μM reduces IL-1beta secretion by LPS-activated mixed glia cultures after 1 and 3 days of exposure. Loxapine in concentrations of 0.2 μM, 2 μM and 20 μM reduces IL-2 secretion in mixed glia cultures after 1 and 3 days of exposure, and additionally Loxapine decreases IL-1beta and IL-2 secretion in LPS-induced microglia cultures in concentrations of 2 μM, 10 μM and 20 μM [2].in vivo: Loxapine (5 mg/kg) induces a very significant reduction (more than 50%) of serotonin (S2) receptor density after 4 weeks or 10 weeks of daily injection in the rat. Loxapine (5 mg/kg) does not change dopamine receptor density but greatly reduces serotonin receptor density by 47% in the brain of rats [3].

Name	loxapine succinate
Synonyms	2-Chloro-11-(4-methylpiperazin-1-yl)dibenzo[b,f][1,4]oxazepine succinate (1:1) Succinic acid - 2-chloro-11-(4-methyl-1-piperazinyl)dibenzo[b,f][1,4]oxazepine (1:1) Daxolin Butandisäure--2-chlor-11-(4-methylpiperazin-1-yl)dibenzo[b,f][1,4]oxazepin(1:1) loxapine succinate salt acide butanedioïque - 2-chloro-11-(4-méthylpipérazin-1-yl)dibenzo[b,f][1,4]oxazépine (1:1) MFCD00069298 Loxitane Cloxazepin Dibenz[b,f][1,4]oxazepine, 2-chloro-11-(4-methyl-1-piperazinyl)-, butanedioate (1:1) Loxapac EINECS 248-682-0 butanedioic acid,8-chloro-6-(4-methylpiperazin-1-yl)benzo[b][1,4]benzoxazepine 2-chloro-11-(4-methylpiperazin-1-yl)dibenzo[b,f][1,4]oxazepine butanedioate Lederle 2-Chloro-11-(4-methyl-1-piperazinyl)dibenzo[b,f][1,4]oxazepine succinate Loxapine succinate Loxapine (succinate)

Description	Loxapine Succinate is a D2DR and D4DR inhibitor, serotonergic receptor antagonist and also a dibenzoxazepine anti-psychotic agent.IC50 value: Target: D2DR/D4DR; 5-HT receptorin 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 0.2 μM, 2 μM and 20 μM reduces IL-1beta secretion by LPS-activated mixed glia cultures after 1 and 3 days of exposure. Loxapine in concentrations of 0.2 μM, 2 μM and 20 μM reduces IL-2 secretion in mixed glia cultures after 1 and 3 days of exposure, and additionally Loxapine decreases IL-1beta and IL-2 secretion in LPS-induced microglia cultures in concentrations of 2 μM, 10 μM and 20 μM [2].in vivo: Loxapine (5 mg/kg) induces a very significant reduction (more than 50%) of serotonin (S2) receptor density after 4 weeks or 10 weeks of daily injection in the rat. Loxapine (5 mg/kg) does not change dopamine receptor density but greatly reduces serotonin receptor density by 47% in the brain of rats [3].
Related Catalog	Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor Research Areas >> Neurological Disease
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]. 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.

Boiling Point	458.6ºC at 760mmHg
Melting Point	150-152°C
Molecular Formula	C₂₂H₂₄ClN₃O₅
Molecular Weight	445.896
Flash Point	231.1ºC
Exact Mass	445.140442
PSA	102.67000
LogP	3.01860
Storage condition	-20°C Freezer
Water Solubility	H2O: soluble

CHEMICAL IDENTIFICATION

RTECS NUMBER :: WM5750000

CAS REGISTRY NUMBER :: 27833-64-3

LAST UPDATED :: 198910

DATA ITEMS CITED :: 3

MOLECULAR FORMULA :: C18-H18-Cl-N3-O.C4-H6-O4

MOLECULAR WEIGHT :: 445.94

WISWESSER LINE NOTATION :: T C676 BO INJ MG J- AT6N DNTJ D1 &QV2VQ

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 6 mg/kg/2D-I

TOXIC EFFECTS :: Behavioral - toxic psychosis

REFERENCE :: JCLPDE Journal of Clinical Psychiatry. (Physicians Postgraduate Press, Inc., POB 240008, Memphis, TN 38124) V.39- 1978- Volume(issue)/page/year: 44,37,1983

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 30 mg/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Behavioral - coma Lungs, Thorax, or Respiration - chronic pulmonary edema

REFERENCE :: CTOXAO Clinical Toxicology. (New York, NY) V.1-18, 1968-81. For publisher information, see JTCTDW. Volume(issue)/page/year: 14,181,1979

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 27 mg/kg/9D-I

TOXIC EFFECTS :: Endocrine - hyperglycemia

REFERENCE :: JCLPDE Journal of Clinical Psychiatry. (Physicians Postgraduate Press, Inc., POB 240008, Memphis, TN 38124) V.39- 1978- Volume(issue)/page/year: 44,347,1983

Personal Protective Equipment	Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter
Hazard Codes	Xi
RIDADR	UN 2811 6.1 / PGII
WGK Germany	3
RTECS	WM5750000

27833-64-3	247566-38-7
1246820-19-8	145823-23-0
25967-34-4	1977-10-2
5634-40-2	106635-81-8
106-65-0	13415-07-1