(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.
Arecaidine propargyl ester is an agonist of M2muscarinic acetylcholine receptors (mAChRs).1It selectively binds to M2over M1, M3, M4, and M5mAChRs in CHO cells expressing the human receptors (Kis = 0.0871, 1.23, 0.851, 0.977, and 0.933 μM, respectively). Arecaidine propargyl ester induces contractions in isolated guinea pig atrium (pD2= 8.67). It induces apoptosis and the production of reactive oxygen species (ROS) in U87 and U251 glioblastoma cells when used at a concentration of 100 μM.2Arecaidine propargyl ester decreases mean arterial blood pressure in normotensive cats (ED25= 1.9 nmol/kg).3It is toxic to house flies (Musca) when administered at a dose of 75 μg/fly.4
1.Scapecchi, S., Matucci, R., Bellucci, C., et al.Highly chiral muscarinic ligands: the discovery of (2S,2’R,3’S,5’R)-1-methyl-2-(2-methyl-1,3-oxathiolan-5-yl)pyrrolidine 3-sulfoxide methyl iodide, a potent, functionally selective, M2 partial agonistJ. Med. Chem.49(6)1925-1931(2006) 2.Di Bari, M., Tombolillo, B., Conte, C., et al.Cytotoxic and genotoxic effects mediated by M2 muscarinic receptor activation in human glioblastoma cellsNeurochem. Int.90261-270(2015) 3.Porsius, A.J., and Van Zwieten, P.A.Central action of some cholinergic drugs (arecaidine esters) and nicotine on blood pressure and heart rate of catsProg. Brain Res.47131-135(1977) 4.Honda, H., Tomizawa, M., and Casida, J.E.Insect muscarinic acetylcholine receptor: Pharmacological and toxicological profiles of antagonists and agonistsJ. Agric. Food Chem.55(6)2276-2281(2007)
PA Nic is a coumarin-caged nicotine. Releases nicotine when exposed to 390 ± 10 nm wavelength light (λmax = 404 nm). Suitable for two-photon uncaging at <900 nm (Maximum two-photon cross-section at 810 nm). Extinction coefficient (ε) 17,400 M-1cm-1. Evokes nicotinic currents in mouse brain slices under one and two-photon activation conditions.
Endogenous peptide agonist of Mas related GPR X2 (MRGPRX2, EC50 = 251 nM). Also a noncompetitive nicotinic cholinergic antagonist. Inhibits nicotine-stimulated catecholamine secretion from PC12 cells in vitro, and from sympathetic nerve endings and adrena
JKC 301, a selective Endothelin A receptor antagonist, attenuates the pressor effects of nicotine in rats and can be used to study cardiovascular disease caused by smoking [1] [2].