Loxapine succinate

SKU: orb1225446

Description

A typical antipsychotic agent that displays an extremely strong binding affinity for dopamine D4 and serotonin 5-HT2 receptors.Schizophrenia Approved(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.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.Loxapine (4 μM, 24 h) is active against multiple-antibiotic-resistant or Fluoroquinolone-resistant S. Typhimurium.Loxapine (1, 2, 4 and 8 μM) suppresses intracellular Methicillin-resistant S. aureus (MRSA), Y. enterocolitica and S. flexneri in RAW264.7.(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.

Images & Validation

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Key Properties

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CAS Number	27833-64-3
MW	445.8961
Purity	>98% (HPLC)
Formula	C₂₂H₂₄ClN₃O₅
SMILES	CN1CCN(CC1)C2=NC3=CC=CC=C3OC4=C2C=C(C=C4)Cl.C(CC(=O)O)C(=O)O
Target	5-HT Receptor
Solubility	10 mM in DMSO

Bioactivity

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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. Animal model: Adult male Wistar rats (150-175 g). 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.

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

Storage & Handling

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Storage	Storage temperature: -20°C. Stability: ≥ 2 years
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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CL 71,563

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Gene Symbol

5-HT Receptor

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