A positive allosteric modulator of α4β2 subunit-containing nAChRs; potentiates ACh-induced currents in HEK293 cells expressing human α4β2 subunit-containing nAChRs (EC50 = 4 μM); potentiates ABT-594 analgesic efficacy in rat models of carrageenan-induced thermal hyperalgesia

NS 9283 – 10 mg

Brand:
Cayman
CAS:
913830-15-6
Storage:
-20
UN-No:
Non-Hazardous - /

NS 9283 is a positive allosteric modulator of α4β2 subunit-containing nicotinic acetylcholine receptors (nAChRs) that potentiates ACh-induced currents in HEK293 cells expressing human α4β2 subunit-containing nAChRs (EC50 = 4 μM).{53135} In vivo, NS 9283 potentiates ABT-594 (Item No. 22822) analgesic efficacy in rat models of carrageenan-induced thermal hyperalgesia, paw skin incision post-operative pain, and monoiodoacetate-induced osteoarthritis.{53136} It reduces nicotine, but not sucrose, self-administration and reinstatement in rats when administered at a dose of 3.5 mg/kg.{53137}  

 

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Description

A positive allosteric modulator of α4β2 subunit-containing nAChRs; potentiates ACh-induced currents in HEK293 cells expressing human α4β2 subunit-containing nAChRs (EC50 = 4 μM); potentiates ABT-594 analgesic efficacy in rat models of carrageenan-induced thermal hyperalgesia, paw skin incision post-operative pain, and monoiodoacetate-induced osteoarthritis; reduces nicotine self-administration and reinstatement in rats at 3.5 mg/kg

Formal name: 3-[3-(3-pyridinyl)-1,2,4-oxadiazol-5-yl]-benzonitrile

Synonyms: 

Molecular weight: 248.2

CAS: 913830-15-6

Purity: ≥98%

Formulation: A crystalline solid

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