Pirlindole hydrochloride
Based on 1 Customer Validation
Pirlindole hydrochloride is an orally active, selective and reversible MAO-A inhibitor with an IC50 value of 250 nM. Pirlindole hydrochloride inhibits genomic replication of Enterovirus species B and D, and exhibits moderate activity against enterovirus species A. Pirlindole hydrochloride inhibits MAO-A-mediated monoamine metabolism, promotes adult hippocampal neurogenesis, rescues stress-induced dendritic atrophy of hippocampal granule neurons, reverses behavioral effects associated with chronic mild stress, and also possesses anticonvulsant, analgesic, local anesthetic, hypotensive, antiplatelet aggregation and antispasmodic activities. Pirlindole hydrochloride shows no detectable mutagenic, clastogenic or carcinogenic properties. Pirlindole hydrochloride can be used in research related to depression and enterovirus infections.
For research use only. We do not sell to patients.
- CAS No.: 16154-78-2
- Formula: C15H19ClN2
- Molecular Weight:262.78
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
MAO-A 250 nM (IC50) |
In Vitro
Pirlindole (10 μM) lactate potently inhibits CV-B3 replication in HeLa R19 cells, as evidenced by a significant reduction in GFP fluorescence intensity and extremely low cytotoxicity[4].
Pirlindole (Up to 0.5 mg per plate) lactate shows no mutagenic activity in the Ames test using Salmonella typhimurium strains TA 98, TA 1537, TA 100, and TA 1535, with or without metabolic activation[3].
Pirlindole lactate selectively inhibits MAO-A in rat brain with an IC50 value of 250 nM, and its inhibitory potency against MAO-B in rat brain and heart is more than 200-fold lower[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Pirlindole (10-25 mg/kg; p.o.) lactate antagonizes the sedative effect induced by Diazepam[3].
Pirlindole (5-25 mg/kg; i.p.; single acute administration or twice daily for 14 consecutive days) lactate significantly reduces the immobility time of mice in the forced swimming test, with efficacy comparable to that of standard antidepressants[3].
Pirlindole (administered via i.p. or p.o. at 1-50 mg/kg) lactate antagonizes reserpine (HY-N0480)-induced ptosis and hypothermia, as well as tetrabenazine (HY-B0590)-induced ptosis in mice[3].
Pirlindole (i.p.; administered daily for 21 consecutive days at doses of 5-30 mg/kg) lactate reverses chronic mild stress-induced depressive-like behaviors (with the strongest effects observed at doses of 5 mg/kg and 15 mg/kg) and restores hippocampal neuroplasticity by enhancing adult neurogenesis at all tested doses and reversing dendritic atrophy at the dose of 30 mg/kg[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Wistar (male, 2 months old, 300-400 g, chronic mild stress model)[1]
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Dosage:5 mg/kg; 15 mg/kg; 30 mg/kg
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Administration:i.p.; daily; 21 days
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Result:Significantly reversed stress-induced anhedonia at 5 mg/kg (P=0.001 vs vehicle-treated stressed rats).
Significantly decreased immobility time at 5 mg/kg and 15 mg/kg (P<0.001 for both doses vs vehicle-treated stressed rats).
Increased latency to immobility at 5 mg/kg (P=0.043 vs vehicle-treated stressed rats) and 15 mg/kg (P<0.001 vs vehicle-treated stressed rats).
Significantly increased adult neurogenesis (percentage of BrdU-positive cells co-labeled with PSA-NCAM) in the hippocampal subgranular zone at 5 mg/kg (P=0.035), 15 mg/kg (P=0.005), and 30 mg/kg (P=0.005) compared to vehicle-treated stressed rats.
Significantly reversed stress-induced reduction in total dendritic length of hippocampal granule neurons at 30 mg/kg (P=0.040 vs vehicle-treated stressed rats).
Chemical Information
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CAS No. 16154-78-2
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Appearance Solid
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Molecular Weight 262.78
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Formula C15H19ClN2
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SMILES
CC1=CC(C2=C3N4CCNC3CCC2)=C4C=C1.Cl
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Synonyms
Pyrazidole hydrochloride; Pirazidole hydrochloride
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
In Vitro:
DMSO : 7 mg/mL (26.64 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
References
[1]. Morais M, et al. The effects of chronic stress on hippocampal adult neurogenesis and dendritic plasticity are reversed by selective MAO-A inhibition. Journal of psychopharmacology (Oxford, England). 2014 Dec;28(12):1178-83. [Content Brief]
[2]. Macedo A, et al. Pirlindole in the treatment of depression: a meta-analysis. Clinical drug investigation. 2011;31(1):61-71. [Content Brief]
[3]. Bruhwyler J, et al. Pirlindole: a selective reversible inhibitor of monoamine oxidase A. A review of its preclinical properties. Pharmacological research. 1997 Jul;36(1):23-33. [Content Brief]
[4]. Ulferts R, et al. Screening of a Library of FDA-Approved Drugs Identifies Several Enterovirus Replication Inhibitors That Target Viral Protein 2C. Antimicrobial agents and chemotherapy. 2016 May;60(5):2627-38. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.8055 mL | 19.0273 mL | 38.0546 mL | 95.1366 mL |
| 5 mM | 0.7611 mL | 3.8055 mL | 7.6109 mL | 19.0273 mL | |
| 10 mM | 0.3805 mL | 1.9027 mL | 3.8055 mL | 9.5137 mL | |
| 15 mM | 0.2537 mL | 1.2685 mL | 2.5370 mL | 6.3424 mL | |
| 20 mM | 0.1903 mL | 0.9514 mL | 1.9027 mL | 4.7568 mL | |
| 25 mM | 0.1522 mL | 0.7611 mL | 1.5222 mL | 3.8055 mL |
Pirlindole hydrochloride Related Classifications
HY-W279140 Related Classifications
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Keywords
- Pirlindole
- 16154-78-2
- Pyrazidole
- Pirazidole
- Monoamine Oxidase
- Enterovirus
- monoamine oxidase subtype A
- Coxsackievirus B3 viral protein 2C
- BGM cells
- hippocampal adult neurogenesis
- noradrenaline reuptake transporters
- HeLa R19 cells
- enterovirus species B
- Salmonella typhimurium
- serotonin reuptake transporters
- enterovirus species D
- Inhibitor
- inhibitor
- inhibit