Pirlindole lactate
Pirlindole lactate is an orally active, selective and reversible MAO-A inhibitor with an IC50 value of 250 nM. Pirlindole lactate inhibits genomic replication of Enterovirus species B and D, and exhibits moderate activity against enterovirus species A. Pirlindole lactate 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 lactate shows no detectable mutagenic, clastogenic or carcinogenic properties. Pirlindole lactate can be used in research related to depression and enterovirus infections.
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- CAS No.: 292039-20-4
- Formule: C18H24N2O3
- Masse moléculaire:316.40
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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MAO-A 250 nM (IC50) |
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].
Pirlindole (0.1 nM-34 μM) lactate slightly increases electrically stimulated dopamine release at concentrations of 0.1-10 nM, and doubles electrically induced norepinephrine and serotonin release at concentrations of 4.5 μM and 34 μM, respectively, in rat cortical slices[3].
Pirlindole (3 μg/mL) lactate prolongs the refractory period of electrically stimulated rabbit atrial contractions[3].
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 (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 (0.3-30 μM; 8 h postinfection) lactate inhibits the replication of CV-B3 in BGM cells and EV-D68 in HeLa R19 cells, exhibits moderate activity against EV-A71, and shows no activity against EV-C, rhinoviruses or EMCV[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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 (10 mg/kg; intraperitoneal injection; once daily for 5 consecutive days) lactate enhances electrical self-stimulation behavior in rats with hypofunction of the reward system induced by internal capsule injury[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 (10-25 mg/kg; p.o.) lactate antagonizes the sedative effect induced by Diazepam[3].
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. 292039-20-4
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Masse moléculaire 316.40
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Formule C18H24N2O3
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SMILES
O=C(O)C(O)C.C1=CC2=C(C=C1C)C3=C4N2CCNC4CCC3
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pirlindole lactate Related Classifications
HY-167152 Related Classifications
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- Pirlindole
- 292039-20-4
- 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