Loxapine Succinate 27833-64-3

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Molecular Weight:


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





Biological Activity

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 0.2
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.


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.


Loxapine (0.3 mg/kg s.c.) induces marked catalepsy, the scores reaching
the cut-off level of 45 s two to 5 hours after injection in rats.
Loxapine-induced catalepsy is fully established then treated by
clozapine (10 mg/kg s.c.), the high catalepsy score is reduced to a
value not significantly different from vehicle-treated controls in rats.

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Product Categories : Neuronal Signaling > 5-HT Receptor Inhibitor