1. GPCR/G Protein
    Neuronal Signaling
  2. 5-HT Receptor
  3. Loxapine

Loxapine 

Cat. No.: HY-17390 Purity: 99.86%
Handling Instructions

Loxapine Succinate is a D2DR and D4DR inhibitor, serotonergic receptor antagonist and also a dibenzoxazepine anti-psychotic agent.

For research use only. We do not sell to patients.

Loxapine Chemical Structure

Loxapine Chemical Structure

CAS No. : 1977-10-2

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10 mM * 1 mL in DMSO USD 92 In-stock
Estimated Time of Arrival: December 31
100 mg USD 84 In-stock
Estimated Time of Arrival: December 31
500 mg USD 288 In-stock
Estimated Time of Arrival: December 31
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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 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].

Clinical Trial
Molecular Weight

327.81

Formula

C₁₈H₁₈ClN₃O

CAS No.

1977-10-2

SMILES

CN1CCN(C2=NC3=CC=CC=C3OC4=CC=C(Cl)C=C24)CC1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 33.33 mg/mL (101.67 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.0505 mL 15.2527 mL 30.5055 mL
5 mM 0.6101 mL 3.0505 mL 6.1011 mL
10 mM 0.3051 mL 1.5253 mL 3.0505 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (7.63 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (7.63 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (7.63 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

Loxapine5-HT ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorInhibitorinhibitorinhibit

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Loxapine
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