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roxindole

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Origin: China

Cas No: 112192-04-8

Specification: 99%min

Min order Quantity: 1 /kg

Supply Ability: 100 mt/month

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  • Products Specification
  • Product Description

  • Property

    CAS No.: 112192-04-8 Formula: C23H26N2O Molecular Weight: 346.46500

    Description

    Roxindole (EMD-49,980) is a dopaminergic and serotonergic drug which was originally developed for the treatment of schizophrenia. In clinical trials its antipsychotic efficacy was only modest but it was unexpectedly found to produce potent and rapid antidepressant and anxiolytic effects. As a result, roxindole was further researched for the treatment of depression instead. It has also been investigated as a therapy for Parkinson's disease and prolactinoma.
    Roxindole acts as an agonist at the following receptors:
    D2 receptor (pKi = 8.55) D3 receptor (pKi = 8.93) D4 receptor (pKi = 8.23) 5-HT1A receptor (pKi = 9.42); At D2 and possibly D3 receptors roxindole is a partial agonist with preferential actions at autoreceptors and has been touted as a 'selective' autoreceptor agonist, hence the justification of its application as an antipsychotic. Weaker activity at the serotonin 1B and 1D receptors has been seen. It is also a serotonin reuptake inhibitor (IC50 = 1.4 nM) and has been reported to act as a 5-HT2A receptor antagonist as well.

    Basic Info

    Chemical Name roxindole
    Synonyms

    ROXINDOLE HYDROCHLORIDE;
    Roxindole;
    RoxindoleHCl;
    Roxindole hydrochloride,3-[4-(3,6-Dihydro-4-phenyl-1(2H)-pyridinyl)butyl]-1H-indol-5-olhydrochloride;

    CAS No. 112192-04-8
    Molecular Formula C23H26N2O
    Molecular Weight 346.46500
    PSA 39.26000
    LogP 4.92340

    Properties

    Density 1.173g/cm3
    Boiling Point 575.7ºC at 760mmHg
    Flash Point 302ºC
    Refractive Index 1.651
    Vapor Pressure 7.46E-14mmHg at 25°C

    Safety Info

    HS Code 2933990090

    Synthesis Route

    5-methoxy-3-[3-(1,2,3,6-tetrahydro-4-phenyl-1-pyridyl)butyl]indole→roxindole
    4-(5-methoxy-1H-indol-3-yl)butanoic acid→roxindole
    4-Phenyl-1,2,3,6-Tetrahydropyridine Hydrochloride→roxindole

    Precursor

    5-methoxy-3-[3-(1,2,3,6-tetrahydro-4-phenyl-1-pyridyl)butyl]indole
    4-(5-methoxy-1H-indol-3-yl)butanoic acid
    4-Phenyl-1,2,3,6-Tetrahydropyridine Hydrochloride
    4-(5-methoxy-1H-indol-3-yl)-1-(4-phenyl-3,6-dihydropyridin-1(2H)-yl)butan-1-one

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