Loxapine hydrochloride

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Loxapine hydrochloride is an orally active dopamine inhibitor, 5-HT receptor antagonist and also a dibenzoxazepine anti-psychotic agent.

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

Loxapine hydrochloride Chemical Structure

CAS No. : 54810-23-0

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Other In-stock Forms of Loxapine hydrochloride:

Loxapine Loxapine succinate

Other Forms of Loxapine hydrochloride:

Loxapine In-stock
Loxapine succinate In-stock
Loxapine-d₈ hydrochloride Get quote
Loxapine-d₈ Get quote

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•Related Small Molecules:

•Related Proteins:

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Dopamine Receptor D₁ Receptor D₂ Receptor D₃ Receptor D₄ Receptor D₅ Receptor

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5-HT₁ Receptor 5-HT₂ Receptor 5-HT₃ Receptor 5-HT₄ Receptor 5-HT₅ Receptor 5-HT₆ Receptor 5-HT₇ Receptor 5-HT Receptor

Biological Activity
Purity & Documentation
References
Customer Review

Description

Loxapine hydrochloride is an orally active dopamine inhibitor, 5-HT receptor antagonist and also a dibenzoxazepine anti-psychotic agent^[1]^[4].

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 K_i 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].

MedChemExpress (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].

MedChemExpress (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

364.27

Formula

C₁₈H₁₉Cl₂N₃O

CAS No.

54810-23-0

SMILES

CN1CCN(C2=NC3=CC=CC=C3OC4=CC=C(Cl)C=C24)CC1.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Singh AN, et al. A neurochemical basis for the antipsychotic activity of loxapine: interactions with dopamine D1, D2, D4 and serotonin 5-HT2 receptor subtypes. J Psychiatry Neurosci. 1996 Jan;21(1):29-35. [Content Brief]

[2]. Labuzek K, et al. Chlorpromazine and loxapine reduce interleukin-1beta and interleukin-2 release by rat mixed glial and microglial cell cultures. Eur Neuropsychopharmacol. 2005 Jan;15(1):23-30. [Content Brief]

[3]. Lee T, et al. Loxapine and clozapine decrease serotonin (S2) but do not elevate dopamine (D2) receptor numbers in the rat brain. Psychiatry Res. 1984 Aug;12(4):277-85. [Content Brief]

[4]. Keating GM. Loxapine inhalation powder: a review of its use in the acute treatment of agitation in patients with bipolar disorder or schizophrenia. CNS Drugs. 2013 Jun;27(6):479-89. [Content Brief]