A potent and selective 5-HT1A receptor agonist (Kis = 4.8

Eptapirone – 1 mg

Brand:
Cayman
CAS:
179756-58-2
Storage:
-20
UN-No:
Non-Hazardous - /

Eptapirone is a potent agonist of the serotonin (5-HT) receptor subtype 5-HT1A (Ki = 4.8 nM in a radioligand binding assay).{41165} It is selective for 5-HT1A over other 5-HT receptor subtypes, dopamine D2 receptors, α1-adrenergic receptors, and histamine H1 receptors (Kis = 11018) in HA7 cells transfected with human 5-HT1A receptors (EC50 = 158 nM). In vivo, eptapirone increases extracellular 5-HT (Item No. 14332) in the ventral hippocampus of rats (ED50 = 0.049 mg/kg) and serum corticosterone (Item No. 16063) levels when administered p.o. or i.p. (ED50s = 0.16 and 0.057 mg/kg, respectively). It decreases immobility in rats in a forced swim test and increases punished responding in a pigeon conflict procedure, demonstrating antidepressant-like and anxiolytic activity. Eptapirone (2.5 mg/kg, p.o.) also attenuates hypertension and tachycardia induced by sibutramine (Item No. 14476) in rats with no effect on sibutramine-induced hypophagia.{41166}  

 

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Description

A potent and selective 5-HT1A receptor agonist (Kis = 4.8, 1A, other 5-HT receptors, and D2, α1-adrenergic, and H1 receptors, respectively); inhibits forskolin-induced cAMP stimulation in HA7 cells transfected with human 5-HT1A receptors; increases extracellular 5-HT in the hippocampus (ED50 = 0.049 mg/kg) and serum corticosterone levels when administered p.o. or i.p. (ED50s = 0.16 and 0.057 mg/kg, respectively); decreases immobility in rats in a forced swim test and increases punished responding in a pigeon conflict procedure; attenuates sibutramine-induced hypertension and tachycardia with no effect on hypophagia in rats

Formal name: 4-methyl-2-[4-[4-(2-pyrimidinyl)-1-piperazinyl]butyl]-1,2,4-triazine-3,5(2H,4H)-dione

Synonyms:  F 11440

Molecular weight: 345.4

CAS: 179756-58-2

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Agonists||Research Area|Cardiovascular System|Cardiovascular Diseases|Hypertension||Research Area|Cardiovascular System|Heart|Arrhythmia||Research Area|Neuroscience|Behavioral Neuroscience|Anxiety||Research Area|Neuroscience|Behavioral Neuroscience|Depression

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