A potent agonist of neuronal α4β2 subunit-containing nAChRs (Ki = 37 pM in a radioligand binding assay); selective for neuronal nAChRs over neuromuscular α1β1δγ subunit-containing nAChRs (Ki = 10

ABT-594 (hydrochloride) – 5 mg

Brand:
Cayman
CAS:
203564-54-9
Storage:
-20
UN-No:
Non-Hazardous - /

ABT-594 is a potent agonist of neuronal α4β2 subunit-containing nicotinic acetylcholine receptors (nAChRs; Ki = 37 pM in a radioligand binding assay).{43783} It is selective for neuronal nAChRs over neuromuscular α1β1δγ subunit-containing nAChRs (Ki = 10,000 nM), α1B-, α2B-, and α2C- adrenergic receptors (Kis = 890, 597, and 342 nM, respectively), and 70 other receptors, enzymes, and transporters (Kis = >1,000 nM) in radioligand binding assays. ABT-594 induces [86Rb+] efflux in K177 cells transfected with human neuronal α4β2 subunit-containing nAChRs (EC50 = 140 nM). In vivo, ABT-594 (0.05 and 0.01 mg/kg, s.c.) increases latency to paw withdrawal in a hot-plate test in rats.{43784} It also induces hypothermia, seizures, and an increase in blood pressure.  

 

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Description

A potent agonist of neuronal α4β2 subunit-containing nAChRs (Ki = 37 pM in a radioligand binding assay); selective for neuronal nAChRs over neuromuscular α1β1δγ subunit-containing nAChRs (Ki = 10,000 nM), α1B-, α2B-, and α2C-adrenergic receptors (Kis = 890, 597, and 342 nM, respectively), and 70 other receptors, enzymes and transporters (Kis = >1,000 nM) in radioligand binding assays; induces [86Rb+] efflux in K177 cells transfected with human neuronal α4β2 subunit-containing nAChRs (EC50 = 140 nM); increases latency to paw withdrawal in a hot-plate test in rats at 0.05 and 0.01 mg/kg; induces hypothermia, seizures, and an increase in blood pressure in rats

Formal name: 5-[(2R)-2-azetidinylmethoxy]-2-chloro-pyridine, monohydrochloride

Synonyms:  Ebanicline|Tebanicline

Molecular weight: 235.1

CAS: 203564-54-9

Purity: ≥95%

Formulation: A solid

Product Type|Biochemicals|Ion Channel Modulation||Research Area|Neuroscience|Pain Research

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