Uses
(-)-Epibatidine has binding affinities for α4β2 and α3β4 nicotinic receptors.
Definition
ChEBI: 3-(6-chloro-3-pyridinyl)-7-azabicyclo[2.2.1]heptane is an alkaloid.
Biological Activity
(+)-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]. kullingsj? 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, l?fberg 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.
