Absorption, Distribution and Excretion
Absorbed well, with a bioavailability of 90%. Primarily excreted via the kidneys, approximately 0.4-0.5% is excreted unchanged in the urine of healthy men. Renal excretion is the main route of elimination for metabolites in the human body. One study showed a high plasma clearance rate (450-1000 L/h). Metabolism/Metabolites This drug is primarily metabolized by the liver. Studies in dogs and mice have shown that the bioavailability of pyrazindole is between 20% and 30% due to the first-pass effect of the liver. Rats primarily eliminate the unbound drug, while dogs primarily eliminate the bound drug. Biological Half-Life A study in healthy volunteers showed a biological half-life of 0.7 ± 0.3 months.

Protein Binding
The binding rate to plasma proteins reached 97%.

[1]. Pirlindole: a selective reversible inhibitor of monoamine oxidase A. A review of its preclinical properties. Pharmacol Res. 1997 Jul;36(1):23-33.

[2]. Screening of a Library of FDA-Approved Drugs Identifies Several Enterovirus Replication Inhibitors That Target Viral Protein 2C. Antimicrob Agents Chemother. 2016 Apr 22;60(5):2627-38.

LSM-1636 belongs to the carbazole class of compounds. This drug is classified as a reversible monoamine oxidase A (MAO) inhibitor (also known as a RIMA drug). Developed in Russia, it is currently used as an antidepressant in Russia. Its chemical structure and pharmacological properties are similar to methimdole. Pirinindole is a selective, reversible monoamine oxidase (MAO) A subtype (MAO-A) inhibitor, approved in several European and non-European countries for the treatment of major depressive disorder. The antidepressant efficacy and safety of pirinindole have been confirmed in numerous studies and supported by years of clinical experience in treating depression. Pirinindole has also shown efficacy and safety in the treatment of fibromyalgia. Drug Indications: For the treatment of major depressive disorder. Its efficacy in the treatment of fibromyalgia pain syndrome is currently under investigation. One study showed that pirinindole's effects on sensorimotor function while driving have many similarities to placebo. This drug appears to stimulate the central nervous system rather than producing a sedative effect like many antidepressants. Due to its selective, reversible inhibition of monoamine oxidase A (MAO-A) and short half-life, it avoids the unpleasant "cheese effect." The "cheese effect" refers to the severe headache and high blood pressure that can result from consuming tyramine-rich foods (such as cheese) while taking a MAO-A inhibitor. Current evidence supports pirlinindole as a safe and effective option for treating depression and fibromyalgia syndrome. Mechanism of Action This drug is a selective, reversible inhibitor of monoamine oxidase A (also known as MAO-A). Its primary mechanism of action is the selective and reversible inhibition of MAO-A. A secondary mechanism of action is the inhibition of the reuptake of norepinephrine and serotonin. Pharmacodynamics Pirlinindole regulates the metabolism of norepinephrine and catecholamines, thereby alleviating depressive symptoms. Inhibiting the breakdown of these neuromodulators is thought to improve mood.

C15H18N2.CH4O3S

322.42248

322.135

60762-57-4

Pirlindole mesylate;207572-66-5;Pirlindole-d4;1801646-26-3

68802

Off-white to light yellow solid powder

1.29 g/cm3

422.6ºC at 760 mmHg

209.4ºC

3.843

1

1

0

17

303

0

IWVRVEIKCBFZNF-UHFFFAOYSA-N

InChI=1S/C15H18N2/c1-10-5-6-14-12(9-10)11-3-2-4-13-15(11)17(14)8-7-16-13/h5-6,9,13,16H,2-4,7-8H2,1H3

12-methyl-1,4-diazatetracyclo[7.6.1.05,16.010,15]hexadeca-9(16),10(15),11,13-tetraene

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Note: Please store this product in a sealed and protected environment, avoid exposure to moisture.

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.)