Nicotine hemicitrate is highly toxic alkaloid. It is the prototypical agonist at nicotinic cholinergic receptors where it dramatically stimulates neurons and ultimately blocks synaptic transmission. Nicotine is also important medically because of its presence in tobacco smoke.
Nicotine monomethiodide is highly toxic alkaloid. It is the prototypical agonist at nicotinic cholinergic receptors where it dramatically stimulates neurons and ultimately blocks synaptic transmission. Nicotine is also important medically because of its presence in tobacco smoke.
Nicotine is a naturally produced alkaloid in the nightshade family of plants (most predominantly in tobacco and Duboisia hopwoodii) and is widely used recreationally as a stimulant and anxiolytic. As a pharmaceutical drug, it is used for smoking cessation to relieve withdrawal symptoms. Nicotine acts as a receptor agonist at most nicotinic acetylcholine receptors (nAChRs), except at two nicotinic receptor subunits (nAChRα9 and nAChRα10) where it acts as a receptor antagonist.
(2'S)-Nicotine-1-oxide, a nicotine metabolite, arises from the liver's metabolism of nicotine via the cytochrome P450 (CYP) isoform CYP2A6. It has been identified in human sperm and semen.
N’-Nitrosonornicotine is a tobacco-specific N-nitrosamine and carcinogen that has been found in unburned tobacco and cigarette smoke.1It induces the formation of DNA adducts in isolated rat nasal mucosa and esophagus. N’-Nitrosonornicotine induces tumor formation in rat esophagus and nasal cavity, mouse lung, forestomach, and trachea, and hamster trachea and forebrain. Urinary levels of N’-nitrosonornicotine are positively correlated with the risk of esophageal cancer in smokers.2
1.Hecht, S.S.Biochemistry, biology, and carcinogenicity of tobacco-specific N-nitrosaminesChem. Res. Toxicol.11(6)559-603(1998) 2.Yuan, J.-M., Knezevich, A.D., Wang, R., et al.Urinary levels of the tobacco-specific carcinogen N’-nitrosonornicotine and its glucuronide are strongly associated with esophageal cancer risk in smokersCarcinogenesis32(9)1366-1371(2011)
Rivanicline is a neuronal nicotinic receptor agonist, showing high selectivity for the α4β2 subtype (Ki=26 nM). It show > 1,000 fold selectivity than α7 receptors(Ki= 36000 nM and IC50 : 26 nM).