Absorption, Distribution and Excretion
Morinda is rapidly absorbed from the gastrointestinal tract after oral administration. Human metabolic studies have shown that morinda is rapidly absorbed and metabolized after oral administration. Currently, 36 metabolites are known, and less than 2-3% of unmetabolized morinda is excreted in urine and feces. Peak plasma concentration is reached within 1 hour after oral administration. Metabolism/Metabolites Primarily metabolized in the liver. 36 metabolites have been identified, some of which may be active.

Hepatotoxicity

A small number of patients taking morinda for a long period have reported liver function abnormalities, but elevations exceeding three times the upper limit of normal are uncommon. Transaminase abnormalities are usually mild, asymptomatic, and transient, returning to normal with continued use. While there have been reports of clinically significant acute liver injury caused by morinda, this is extremely rare. Injury usually appears within 4 to 8 weeks of use, with serum enzyme elevations typically exhibiting a hepatocellular pattern. Jaundice is uncommon, and most cases resolve spontaneously with mild symptoms. Immune hypersensitivity and autoantibody formation are atypical.
Probability Score: D (Possible, but rare, cause of clinically significant liver injury).

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Effects During Pregnancy and Lactation
◉ Overview of Use During Lactation
Since there is no published experience regarding the use of morinda during lactation, alternative antipsychotic medications are recommended as a priority.
◉ Effects on Breastfed Infants
As of the revision date, no relevant published information was found.
◉ Effects on Lactation and Breast Milk
There have been reports of morinda causing galactorrhea. Hyperprolactinemia appears to be the cause. Hyperprolactinemia is caused by the drug blocking the action of dopamine in the tuberous-infundibular pathway. For mothers who have already established lactation, their prolactin levels may not affect their ability to breastfeed.

Morinone belongs to the indole class of drugs. It is an indole derivative effective against schizophrenia and other psychoses, and may also be effective against aggressive social disorder. Morinone has a much lower affinity for D2 receptors than most antipsychotics, and a relatively low affinity for D1 receptors. Its affinity for cholinergic and alpha-adrenergic receptors is only low to moderate. Some animal electrophysiological data suggest that morinone possesses certain properties similar to clozapine. (From JAMA Drug Evaluation Yearbook, 1994, p. 283) Morinone is a typical antipsychotic. Morinone is a traditional antipsychotic used to treat schizophrenia. Morinone treatment usually results in a slight increase in serum transaminases, but is rarely associated with clinically significant cases of acute liver injury. Morinone is an indole derivative effective against schizophrenia and other psychoses, and may also be effective against aggressive social disorder. Compared to most antipsychotics, morinone has a much lower affinity for D2 receptors and a relatively lower affinity for D1 receptors. Its affinity for cholinergic and alpha-adrenergic receptors is only low to moderate. Some animal electrophysiological data suggest that morinone possesses certain properties similar to clozapine. (From JAMA Drug Evaluation Yearbook, 1994, p. 283)
See also: morinone hydrochloride (salt form).
Drug Indications

Morinone is used to treat symptoms of psychotic disorders.
Mechanism of Action

The exact mechanism of action is not fully understood, but based on electroencephalogram (EEG) studies, morinone is thought to exert its effects by occupying (antagonizing) dopamine (D2) receptor sites in the reticular limbic system of the brain, thereby reducing dopamine activity. Reduced dopamine activity leads to a diminished physiological effect that would normally result from excessive dopamine stimulation, such as the typical manifestations of psychotic disorders.
Current information is insufficient to determine the specific effects of morinone…
This antipsychotic drug is a dihydroindole derivative. It is chemically unrelated to phenothiazines, butyrophenones, or thioxanthates, but its pharmacological effects are similar to those of piperazine and phenothiazine drugs.

276.37396

276.184

7416-34-4

Molindone hydrochloride;15622-65-8;Molindone-d8;1189805-13-7

23897

CRYSTALS

1.14 g/cm3

462.9ºC at 760 mmHg

180 - 181ºC

233.7ºC

1.559

1.9

1

3

3

20

354

0

O=C1C(CN2CCOCC2)CCc2c1c(CC)c(C)[nH]2

KLPWJLBORRMFGK-UHFFFAOYSA-N

InChI=1S/C16H24N2O2/c1-3-13-11(2)17-14-5-4-12(16(19)15(13)14)10-18-6-8-20-9-7-18/h12,17H,3-10H2,1-2H3

3-ethyl-2-methyl-5-(morpholin-4-ylmethyl)-1,5,6,7-tetrahydroindol-4-one

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)

May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples

Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.

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Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)
*Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution.
Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)
Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil)
Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals).

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Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)]
*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.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)

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Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium)
Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose
Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals).

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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders

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Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

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