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(±)-Epibatidinenicotinic agonist

(±)-Epibatidine

Catalog No. B6406
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10mg $281.00 Ship Within 7 Days

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

(±)-Epibatidine

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Chemical Properties

Cas No. 148152-66-3 SDF Download SDF
Chemical Name (1S,2S,4R)-2-(6-chloropyridin-3-yl)-7-azabicyclo[2.2.1]heptane
Canonical SMILES ClC(N=C1)=CC=C1[C@H]2[C@H](CC3)N[C@H]3C2
Formula C11H13ClN2 M.Wt 208.69
Solubility Soluble to 5 mM in sterile water and to 100 mM in ethanol Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

Background

(+)-AJ 76 hydrochloride is an antagonist of dopamine autoreceptor with pKi values of 6.95, 6.67, 6.37, 6.21 and 6.07 for hD3, hD4, hD2S, hD2L and rD2 receptors, respectively.

Dopamine receptor is a G protein-coupled receptor and mainly exists in the vertebrate central nervous system (CNS). Dopamine receptor is a receptor for dopamine and plays a critical role in memory, learning, pleasure, cognition, motivation and fine motor control.

(+)-AJ 76 hydrochloride is a dopamine receptor antagonist. In rats, AJ76 stimulated locomotor activity and increased the levels of 3,4-dihydroxyphenylacetic acid (DOPAC) and HVA in brain, which were dopamine metabolites [1]. In rats injected with cocaine, (+)-A J76 increased the locomotor stimulation during the first 30 min. However, (+)-AJ76 inhibited the later more intense locomotor stimulation and cocaine-induced stereotypies [2]. In vivo, (+)-AJ76 induced dopamine release mainly through interaction with dopamine receptors in the terminal regions of the A9 and A10 dopaminergic fibers. However, (+)-AJ76 increased the level of DOPAC via the somatodendritic autoreceptors [3].

References:
[1].  Kullingsjö H, Carlsson A, Svensson K. Effects of repeated administration of the preferential dopamine autoreceptor antagonist, (+)-AJ76, on locomotor activity and brain DA metabolism in the rat. Eur J Pharmacol, 1991, 205(3): 241-246.
[2].  Piercey MF, Lum JT, Hoffmann WE, et al. Antagonism of cocaine's pharmacological effects by the stimulant dopaminergic antagonists, (+)-AJ76 and (+)-UH232. Brain Res, 1992; 588(2): 217-222.
[3].  Waters N, Hansson L, Löfberg L, et al. Intracerebral infusion of (+)-AJ76 and (+)-UH232: effects on dopamine release and metabolism in vivo. Eur J Pharmacol, 1994, 251(2-3): 181-190.