A partial agonist of α7 subunit-containing nAChRs (IC50 = 22.38 nM); 1

EVP-6124 (hydrochloride) – 5 mg

Brand:
Cayman
CAS:
550999-74-1
Storage:
-20
UN-No:
Non-Hazardous - /

EVP-6124 is a partial agonist of α7 subunit-containing nicotinic acetylcholine receptors (nAChRs; IC50 = 22.38 nM).{52384} It is 1,000-fold selective for α7 subunit-containing nAChRs over α4β2 subunit-containing nAChRs at 10 µM, as well as a panel of 60 peptide and nonpeptide receptors, ion channels, and transporters. EVP-6124 induces inward currents in Xenopus oocytes expressing human α7 subunit-containing nAChRs (EC50 = 0.16 µM). In vivo, EVP-6124 (0.1, 0.3, and 1 mg/kg) reverses scopolamine-induced deficits in the novel object recognition task and prevents natural forgetting of a familiar object in rats. It reduces premature responding, a measure of impulsivity, by low-attentive but not high-attentive female rats in the 5-choice serial reaction time test (5CSRTT).{52385}  

 

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Description

A partial agonist of α7 subunit-containing nAChRs (IC50 = 22.38 nM); 1,000-fold selective for α7 subunit-containing nAChRs over α4β2 subunit-containing nAChRs at 10 µM, as well as a panel of 60 peptide and nonpeptide receptors, ion channels, and transporters; induces inward currents in Xenopus oocytes expressing human α7 subunit-containing nAChRs (EC50 = 0.16 µM); reverses scopolamine-induced deficits in the novel object recognition task and prevents natural forgetting of a familiar object in rats at 0.1, 0.3, and 1 mg/kg; reduces premature responding in the 5CSRTT in low-attentive female rats

Formal name: N-(3R)-1-azabicyclo[2.2.2]oct-3-yl-7-chloro-benzo[b]thiophene-2-carboxamide, monohydrochloride

Synonyms: 

Molecular weight: 357.3

CAS: 550999-74-1

Purity: ≥95%

Formulation: A crystalline solid

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