NNK (Nicotine-derived nitrosamine ketone) is a procarcinogen and a major tobacco-specific toxicant. It inhibits the expression of lysyl oxidase which is a tumor suppressor.

Nicotine tartrate 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.

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 1'-N-oxide is a natural product from tobacco smoke.

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 dicitrate 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-d4 is a deuterated compound of (+/-)-NICOTINE.

(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.

(1'S,2'S)-Nicotine-1'-Oxide-d3 is a deuterated compound of (1'S,2'S)-Nicotine-1'-Oxide. (1'S,2'S)-Nicotine-1'-Oxide has a CAS number of 51095-86-4. Nicotine 1'-N-oxide is a natural product from tobacco smoke.

Nicotinic receptor agonist

(Z)-Metanicotine 2HCl has analgesic activity and is used in the treatment of central system disorders.

UB 165 fumarate is an agonist of the nAChR, a partial agonist of the α4β2 subtype, and a full agonist of the α3β2 subtype, with a Ki value of 0.27 nM for binding to [3H]-nicotine measured in rat brain.

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)

Metanicotine is a selective nicotinic agonist with antinociceptive properties.

Hydroxycotinine is the main nicotine metabolite detected in smokers' urine.

Marcfortine A is an indole alkaloid originally isolated from P. roqueforti. It has nematocidal activity against the parasitic nematode H. contortus (LD99 = 0.06 μg/ml) and inhibits motility of adult worms (EC50 = 2 μM)., Marcfortine A eliminates H. contortus, T. colubriformis, and O. ostertagi from experimentally infected jirds (ED95s = 0.33, 0.11, and 2.5 mg/animal, respectively). It dose-dependently inhibits nicotine-induced calcium mobilization in SH-SY5Y and TE-671 cells expressing α3 subunit-containing human nicotinic acetylcholine receptors (nAChRs) and muscle-type nAChRs, respectively.

AMPD2 inhibitor 1 is an inhibitor of adenosine monophosphate deaminase 2 (AMPD2), used in the research of salt craving, sugar craving, umami craving, and addictions including tobacco, drug, nicotine and alcohol addictions.

Cotinine (NIH-10498) is an alkaloid found in tobacco and is also the predominant metabolite of nicotine.

Myosmine is a minor tobacco alkaloid that is structurally related to nicotine.

3-Pyridineacetic acid is a homolog of nicotinic acid, a breakdown product of nicotine and other tobacco alkaloids.

Rivanicline hemioxalate, also known as RJR-2403 hemioxalate or (E)-Metanicotine hemioxalate, is a chemical compound acting as a neuronal nicotinic receptor agonist with pronounced selectivity for the α4β2 receptor subtype, showing over 1,000-fold greater selectivity for this subtype (Ki=26 nM) compared to α7 receptors (Ki=3.6 μM). Its in vitro studies demonstrate no significant activation of nAChRs in PC12 cells, muscle type nAChRs, or muscarinic receptors at concentrations up to 1 mM. Furthermore, Rivanicline displayed less than one-tenth the potency of nicotine in inducing ileum contraction, with substantially lower efficacy, and failed to antagonize nicotine-induced stimulation of muscle or ganglionic nAChR functions, with an IC50 value greater than 1 mM. Chronic exposure to Rivanicline at 10 microM led to up-regulation of high-affinity nAChRs in M10 cells, mimicking effects observed with nicotine. In vivo studies revealed that Rivanicline significantly reversed scopolamine-induced amnesia and improved working and reference memory in a rat model, while being 15 to 30 times less potent than nicotine in affecting body temperature, respiration, and other physiological responses. Metanicitone’s potency was approximately five times lower than nicotine in tail-flick tests following subcutaneous administration, yet slightly more potent upon central administration.

R-(+)-Cotinine ((+)-Cotinine), a metabolite of Nicotine, demonstrates minimal activity across numerous pharmacological targets. However, it is capable of enhancing the acetylcholine (Ach)-evoked current in human α7 nicotinic acetylcholine receptors (nAChRs) [1].

BHF-177 is a positive allosteric modulator of the GABAB receptor. BHF-177 reduces self-administration of nicotine in animal studies.

Anatabine is a minor tobacco alkaloid with a chemical structural similarity to nicotine. Anatabine is produced in plants of the Solanacea family including tobacco, green tomatoes, peppers, and eggplants. Anatabine is an Aβ inhibitor. (R,S)-Anatabine (tart

α-Helical CRF (9-41) is a synthetic peptide antagonist that targets corticotropin-releasing factor (CRF), effectively inhibiting CRF-induced adrenocorticotropic hormone (ACTH) release both in vitro, with isolated rat anterior pituitary cells at concentrations of 0.5 to 5 µM, and in vivo, in non-anesthetized, intact rats at doses ranging from 0.02 to 0.6 µmol/kg. Moreover, it prevents stress-induced ACTH release at a dose of 0.6 µmol/kg in rats and demonstrates the ability to enhance social interaction times in a rat model addressing nicotine-induced conditioned anxiety, in addition to decreasing binge-like ethanol consumption in mice.

Bifeprunox is a partial dopamine and serotonin agonist potentially for the treatment of schizophrenia. Bifeprunox suppresses in vivo VTA dopaminergic neuronal activity via D2 and not D3 dopamine autoreceptor activation. Bifeprunox influences nicotine-seek

(S)-UFR2709 is a competitive antagonist of the nicotinic acetylcholine receptor (nAChR), exhibiting a greater affinity for α4β2 nAChRs compared to α7 nAChRs. It effectively reduces anxiety and ethanol consumption, as well as ethanol preference, in alcohol-preferring rats. Additionally, (S)-UFR2709 functions as an anxiolytic agent and holds the potential for investigating nicotine addiction.

AT-1001 is an α3β4 nAChR partial agonist. AT-1001 attenuates stress-induced reinstatement of nicotine seeking in a rat model of relapse and induces minimal withdrawal in dependent rats. AT-1001 also potently and reversibly blocks epibatidine-induced inward currents in HEK cells transfected with α3β4 nAChR. Importantly, AT-1001 potently and dose-dependently blocks nicotine self-administration in rats, without affecting food responding. When tested in a nucleus accumbens (NAcs) synaptosomal preparation, AT-1001 inhibits nicotine-induced [³H]dopamine release poorly and at significantly higher concentrations compared with mecamylamine and conotoxin MII.

Lobeline, (+)- is an alkaloid that has actions similar to nicotine on nicotinic cholinergic receptors but is less potent. It has been proposed for a variety of therapeutic uses including in respiratory disorders, peripheral vascular disorders, insomnia, a

High affinity and subtype selective α6β2 and α4β2 partial agonist (Ki values are 12 and 26nM for rat α6β2 and α4β2 receptors respectively). Has low affinity for α3β4 and α7 receptors (Ki values are 4.8 and 13 μM for human α3β4 and rat α7 receptors respectively). Stimulates dopamine release from striatal slices in vitro. Attenuates nicotine-induced self-administration and conditional place preference in rats. Sala et al (2013) CC4, a dimer of cytisine, is a selective partial agonist at α4β2/α6β2 nAChR with improved selectivity for tobacco smoking c Br.J.Pharmacol. 168 835 PMID:22957729 |Riganti et al (2005) Long-term exposure to the new nicotinic antagonist 1,2-bisN-cytisinylethane upregulates nicotinic receptor subtypes of SH-SY5Y human neuroblastoma cells. Br.J.Pharmacol. 146 1096 PMID:16273122 |Carbonnelle et al (2003) Nitrogen substitution modifies the activity of cytisine on neuronal nicotinic receptor subtypes. Eur.J.Pharmacol. 471 85 PMID:12818695

AZD-8418 is an mGlu2 receptor positive allosteric modulators that attenuates nicotine-taking and nicotine-seeking behavior. Acute treatment with AZD8418 (0.37, 1.12, 3.73, 7.46, and 14.92 mg/kg) and AZD8529 (1.75, 5.83, 17.5, and 58.3 mg/kg) deceased nicotine self-administration and had no effect on food-maintained responding. Chronic treatment with AZD8418 attenuated nicotine self-administration, but tolerance to this effect developed quickly. The inhibition of nicotine self-administration by chronic AZD8529 administration persisted throughout the 14 days of treatment. Chronic treatment with either PAMs inhibited food self-administration. AZD8418 (acute) and AZD8529 (acute and subchronic) blocked cue-induced reinstatement of nicotine- and food-seeking behavior.

AZD-8529 mesylate is a highly selective, and orally bioavailable positive allosteric modulator of mGluR2 (EC50: 285 nM). It shows no positive allosteric modulator responses at 20-25 M on the mGluR1, 3, 4, 5, 6, 7, and 8 subtypes.

CMPI hydrochloride, a potent and selective nAChR agonist, functions as a positive allosteric modulator (PAM) specifically targeting the α4:α4 subunit interface of the nAChR. It enhances the response of the (α4)3(β2)2 nAChR to acetylcholine (ACh) (10 μM) with an EC 50 of 0.26 μM. With its potential for researching nicotine dependence and various neuropsychiatric conditions linked to reduced brain cholinergic activity, CMPI hydrochloride stands as a significant compound in neurological research.

Varenicline dihydrochloride is a Selective α4β2 nicotinic acetylcholine receptor partial agonist.

Nicotelline, also known as Nicotellin, is an alkaloid associated with nicotine and acts as a modest inhibitor of the enzyme human cDNA-expressed cytochrome P-450 2A6 (CYP2A6), which is responsible for coumarin 7-hydroxylation. However, Nicotelline does not show inhibitory effects at a concentration of 300 μM. It serves as a tracer and biomarker for particulate matter (PM) originating from tobacco smoke [1] [2].

Lobelin sulphate is an alkaloid that has actions similar to nicotine on nicotinic cholinergic receptors but is less potent. It has a variety of therapeutic uses including in insomnia, and smoking cessation, peripheral vascular disorders, respiratory disor

Arecoline is a natural alkaloid derived from areca nut in the palm family and is a potent nicotine and partial agonist of muscarinic acetylcholine receptors. Arecoline has anti-anxiety and anti-parasitic activity, can induce oxidative stress and can be used to study Alzheimer's disease and Alzheimer's disease.

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)

Myosmine-2,4,5,6-d4 is a deuterated compound of Myosmine. Myosmine has a CAS number of 532-12-7. Myosmine is a minor tobacco alkaloid that is structurally related to nicotine.

α-Conotoxin M I selectively inhibits mAChR and α1β1γδ nAChR without affecting nicotine-stimulated dopamine release. It belongs to the α-conotoxins class, which are small, disulfide-rich peptides known to competitively inhibit muscle and neuronal nicotinic AChRs [1] [2].

beta-Nicotyrine is a tobacco alkaloids Metabolite in the liver.

Pozanicline reverses nicotine withdrawal-induced cognitive deficits, may be an effective component of novel therapeutic strategies for nicotine addiction. Pozanicline selectively activate neuronal nicotinic acetylcholine receptor (nAChR) subtypes, is a no

(S)-UFR2709 hydrochloride ((S)-UFR2709 HCl) is a selective and potent nAChR antagonist with anxiolytic activity, inhibits α4β2 nAChR and α7 nAChR, and can be used to study nicotine addiction.

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.

TMB 8 is a non-competitive antagonist of nicotinic acetylcholine receptors (nAChRs) with IC50 values of 390 and 350 nM, respectively, for human muscle-type and α3β4 subunit-containing ganglionic nAChRs expressed in TE671/RD or SH-SY5Y cells. It inhibits nicotine-induced dopamine release from rat brain synaptosomes (IC50 = 480 nM). TMB 8 also reduces calcium availability in smooth and skeletal muscle, blocking the contractile response in isolated rabbit aortic strip when used at a concentration of 50 μM and inhibiting calcium influx and efflux in isolated guinea pig ileum when used at a concentration of 65 μM. It has been used in the study of intracellular calcium dynamics, particularly in smooth muscle. TMB 8 also inhibits protein kinase C (PKC) activity in a dose-dependent manner.

3-Pyridylacetic acid hydrochloride (3-PAA-HCl) is a high homologue of niacin. It is a decomposition product of nicotine (and other tobacco alkaloids). It can also react with amines, alcohols and carboxylic acids, and can also act as an acid in the reaction. catalyst.

Hirsuteine is a natural product. It non-competitively antagonizes nicotine-mediated dopamine release by blocking ion permeation through nicotinic receptor channel complexes.

CP-809101 hydrochloride is a potent and selective 5-HT2C receptor agonist (pEC50: 9.96/7.19/6.81 for human 5-HT2C/5-HT2B/5-HT2A receptors).

BPTU (BMS-646786) is an allosteric antagonist of P2Y1 (EC50 = 0.06-0.3 μM). Non-nucleotide ligand. Binds receptor outside of the helical bundle. Blocks inhibition of spontaneous contraction of rat and mouse colon induced by electrical field stimulation, nicotine and P2Y agonists. Antithrombotic; reduces platelet aggregation.