CAS No. : 1977-10-2

Product Details
For research use only. Not Intended for Therapeutic Use!
Cat No:I000025
Molecular Formula:C18H18ClN3O
Molecular Weight:327.81
Target:5-HT Receptor
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Appearance:Solid powder
Purity: > 98%
Cat No:I000025
Cas No:1977-10-2

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 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 0.2 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].

1:Pharmacokinetics and Safety of Single-Dose Inhaled Loxapine in Children and Adolescents. Selim S, Riesenberg R, Cassella J, Kunta J, Hellriegel E, Smith MA, Vinks AA, Rabinovich-Guilatt L.J Clin Pharmacol. 2017 May 16. doi: 10.1002/jcph.932. [Epub ahead of print] PMID: 28510296
2:Rationale and design of the PLACID study: a randomised trial comparing the efficacy and safety of inhaled loxapine versus IM aripiprazole in acutely agitated patients with schizophrenia or bipolar disorder. San L, Estrada G, Oudovenko N, Vieta E.BMC Psychiatry. 2017 Apr 4;17(1):126. doi: 10.1186/s12888-017-1291-5. PMID: 28376877 Free PMC Article
3:Dopamine antagonists for treatment resistance in autism spectrum disorders: review and focus on BDNF stimulators loxapine and amitriptyline. Hellings JA, Arnold LE, Han JC.Expert Opin Pharmacother. 2017 Apr;18(6):581-588. doi: 10.1080/14656566.2017.1308483. Review. PMID: 28335658
4:The Role of Inhaled Loxapine in the Treatment of Acute Agitation in Patients with Psychiatric Disorders: A Clinical Review. de Berardis D, Fornaro M, Orsolini L, Iasevoli F, Tomasetti C, de Bartolomeis A, Serroni N, Valchera A, Carano A, Vellante F, Marini S, Piersanti M, Perna G, Martinotti G, Di Giannantonio M.Int J Mol Sci. 2017 Feb 8;18(2). pii: E349. doi: 10.3390/ijms18020349. Review. PMID: 28208695 Free PMC Article
5:Clinical Trial Simulations and Pharmacometric Analysis in Pediatrics: Application to Inhaled Loxapine in Children and Adolescents. Dong M, Fukuda T, Selim S, Smith MA, Rabinovich-Guilatt L, Cassella JV, Vinks AA.Clin Pharmacokinet. 2017 Feb 15. doi: 10.1007/s40262-017-0512-x. [Epub ahead of print] PMID: 28205038
6:ClinicalTrials.gov, Inhaled Loxapine, and Safety Issues. Shader RI.J Clin Psychopharmacol. 2017 Apr;37(2):119-121. doi: 10.1097/JCP.0000000000000679. No abstract available. PMID: 28187007
7:Simultaneous quantification of loxapine, loxapine N-oxide, amoxapine, 8-hydroxyloxapine and 7-hydroxyloxapine in human plasma using LC-MS/MS. Meng M, Zhao N, Pederson CC, Harrison E, Green C, Gorman SH, Reuschel S.J Chromatogr B Analyt Technol Biomed Life Sci. 2017 Mar 1;1046:87-97. doi: 10.1016/j.jchromb.2017.01.007. Epub 2017 Jan 9. PMID: 28152454
8:Loxapine and Cyproheptadine Combined Limit Clozapine Rebound Psychosis and May Also Predict Clozapine Response. Aboueid L, McCarthy RH.Case Rep Psychiatry. 2016;2016:6123913. doi: 10.1155/2016/6123913. Epub 2016 Jun 28. PMID: 27433365 Free PMC Article
9:Inhaled loxapine for the urgent treatment of acute agitation associated with schizophrenia or bipolar disorder. Pollack CV Jr.Curr Med Res Opin. 2016 Jul;32(7):1253-60. doi: 10.1185/03007995.2016.1170004. Epub 2016 Jun 1. PMID: 27121764
10:Inhaled loxapine and intramuscular lorazepam in healthy volunteers: a randomized placebo-controlled drug-drug interaction study. Spyker DA, Cassella JV, Stoltz RR, Yeung PP.Pharmacol Res Perspect. 2015 Dec 17;3(6):e00194. doi: 10.1002/prp2.194. eCollection 2015 Dec. PMID: 27022468 Free PMC Article
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