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编 号：F572720
分子式：C18H19Cl2N3O
分子量：364.27
分子式：C18H19Cl2N3O
分子量：364.27
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CAS No: 54810-23-0
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生物活性：
Loxapine hydrochloride is an orally active dopamine inhibitor, 5-HT receptor antagonist and also a dibenzoxazepine anti-psychotic agent.
体内研究：
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.
体外研究：
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 hydrochloride is an orally active dopamine inhibitor, 5-HT receptor antagonist and also a dibenzoxazepine anti-psychotic agent.
体内研究：
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.
体外研究：
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.
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