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

Loxapine succinate 

Cat. No.: HY-17390A Purity: 99.81%
COA Handling Instructions

Loxapine succinate is an orally active dopamine inhibitor, 5-HT receptor antagonist and also a dibenzoxazepine anti-psychotic agent. Loxapine can also suppresses bacterial efflux pump activity and inhibit intracellular multiple-antibiotic-resistant Salmonella enterica serovar Typhimurium in macrophages.

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

Loxapine succinate Chemical Structure

Loxapine succinate Chemical Structure

CAS No. : 27833-64-3

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Solution
10 mM * 1 mL in DMSO USD 66 In-stock
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
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Solid
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500 mg USD 204 In-stock
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Description

Loxapine succinate is an orally active dopamine inhibitor, 5-HT receptor antagonist and also a dibenzoxazepine anti-psychotic agent. Loxapine can also suppresses bacterial efflux pump activity and inhibit intracellular multiple-antibiotic-resistant Salmonella enterica serovar Typhimurium in macrophages[1][4][6].

IC50 & 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].
Loxapine (4 μM, 24 h) is active against multiple-antibiotic-resistant or Fluoroquinolone-resistant S. Typhimurium[6].
Loxapine (1, 2, 4 and 8 μM) suppresses intracellular Methicillin-resistant S. aureus (MRSA), Y. enterocolitica and S. flexneri in RAW264.7[6].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Clinical Trial
Molecular Weight

445.90

Appearance

Solid

Formula

C22H24ClN3O5

CAS No.
SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (224.27 mM; Need ultrasonic)

H2O : 2.5 mg/mL (5.61 mM; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2427 mL 11.2133 mL 22.4266 mL
5 mM 0.4485 mL 2.2427 mL 4.4853 mL
10 mM 0.2243 mL 1.1213 mL 2.2427 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 (5.61 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.5 mg/mL (5.61 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.5 mg/mL (5.61 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation
References
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Loxapine succinate Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Loxapine succinate
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HY-17390A
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