Absorption, Distribution and Excretion
Methoxypromethazine has incomplete oral bioavailability due to significant first-pass metabolism in the liver. Oral bioavailability is approximately 50% to 60%. Metabolism/Metabolites Hepatic Metabolism Methoxypromethazine is metabolized in the liver and degraded into sulfoxides, glucuronic acid, and a demethylated moiety. Hepatic Metabolism Methoxypromethazine is metabolized in the liver and degraded into sulfoxides, glucuronic acid, and a demethylated moiety. Half-life: Approximately 20 hours. Biological Half-life Approximately 20 hours.

Toxicity Summary
The antipsychotic effects of methoxypromethazine are primarily attributed to its antagonistic effect on dopamine receptors in the brain. Additionally, its binding to 5-HT2 receptors may also play a role. Methoxypromethazine exerts its effects by blocking central adrenergic, dopamine, serotonin, and anticholinergic pathways.

[1]. Levomepromazine for nausea and vomiting in palliative care. Cochrane Database Syst Rev. 2015 Nov 2;(11):CD009420.

[2]. Levomepromazine for schizophrenia. Cochrane Database Syst Rev. 2010 Oct 6;(10):CD007779.

Methotrimeprazine is a phenothiazine compound with the structure 10H-phenothiazine, substituted at positions 10 and 2 with (2R)-3-(dimethylamino)-2-methylpropyl and methoxy, respectively. It possesses a variety of pharmacological activities, including as a phenothiazine antipsychotic, dopaminergic antagonist, serotonergic antagonist, cholinergic antagonist, non-narcotic analgesic, EC 3.4.21.26 (prolyl oligopeptidase) inhibitor, and anticoronavirus drug. It belongs to the phenothiazine class of compounds and is also a tertiary amine. It is a 10H-phenothiazine hydride derivative. Methotrimeprazine is a phenothiazine compound with pharmacological activities similar to chlorpromazine and promethazine. It possesses the histamine antagonistic properties of antihistamines while also producing effects on the central nervous system similar to chlorpromazine. (Excerpt from Martindale Pharmacopoeia, 30th Edition, p. 604)
Levopromethazine is a phenothiazine drug and a typical antipsychotic with sedative/hypnotic, anti-anxiety, antiemetic, analgesic, and antipsychotic effects. Although the exact mechanism of action of levopromethazine is not fully understood, after administration, it appears to antagonize multiple receptors in the central nervous system (CNS), including adrenergic receptors, dopamine receptors, histamine receptors, cholinergic receptors, and serotonin (5-hydroxytryptamine; 5-HT) receptors. Blocking these receptors is what allows levopromethazine to exert its pharmacological effects.
Methoxypromethazine is only found in individuals who have used or taken this drug. It is a phenothiazine drug with pharmacological activity similar to chlorpromazine and promethazine. It has the histamine-antagonistic properties of an antihistamine and CNS effects similar to chlorpromazine. (Excerpt from Martindale Pharmacopoeia, 30th Edition, p. 604) The antipsychotic effect of methoxypromethazine is primarily attributed to its antagonistic effect on dopamine receptors in the brain. Additionally, its binding to 5-HT2 receptors may also play a role. It is a phenothiazine drug with pharmacological activity similar to chlorpromazine and promethazine. It possesses the histamine-antagonistic properties of antihistamines while having similar effects on the central nervous system as chlorpromazine. (From Martindale Pharmacopoeia, 30th edition, p. 604) See also: Phenothiazines (subclasses). Indications: Used for the treatment of psychosis, particularly the manic phase of schizophrenia and bipolar disorder. Mechanism of Action: The antipsychotic effect of methoxypromethazine is primarily attributed to its antagonistic effect on dopamine receptors in the brain. Additionally, its binding to 5-HT2 receptors may also play a role. Pharmacodynamics: Methoxypromethazine is a phenothiazine drug with pharmacological activity similar to chlorpromazine and promethazine. It possesses the histamine-antagonistic properties of antihistamines, while also producing effects on the central nervous system similar to chlorpromazine. (Excerpt from Martindale Pharmacopoeia, 30th edition, page 604)

C19H24N2OS

328.47

328.161

C, 69.47; H, 7.36; N, 8.53; O, 4.87; S, 9.76

60-99-1

7104-38-3; 1236-99-3 (HCl); 60-99-1

72287

White to off-white solid powder

1.125g/cm3

468ºC at 760 mmHg

117°C

236.8ºC

1.594

4.56

0

4

5

23

378

1

C[C@H](CN(C)C)CN1C2=CC=CC=C2SC3=C1C=C(C=C3)OC

VRQVVMDWGGWHTJ-CQSZACIVSA-N

InChI=1S/C19H24N2OS/c1-14(12-20(2)3)13-21-16-7-5-6-8-18(16)23-19-10-9-15(22-4)11-17(19)21/h5-11,14H,12-13H2,1-4H3/t14-/m1/s1

(2R)-3-(2-methoxyphenothiazin-10-yl)-N,N,2-trimethylpropan-1-amine

Nozinan; Nosinan; Levomepromazine; Methoxytrimeprazine; mepromazine; Methotrimeprazine; Milezin; Minozinan; Neozine

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

DMSO: ~41.7 mg/mL (~126.9 mM)

Solubility in Formulation 1: ≥ 1.43 mg/mL (4.35 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 14.3 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

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Solubility in Formulation 2: ≥ 1.43 mg/mL (4.35 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 14.3 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

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Solubility in Formulation 3: ≥ 1.43 mg/mL (4.35 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 14.3 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

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 (Please use freshly prepared in vivo formulations for optimal results.)