nicotine

NNK (Nicotine-derived nitrosamine ketone) 是尼古丁亚硝化衍生物。它可以激活 ERK1 2和 PKCα，并在 Ser70 激活 Bcl2磷酸化，以及在 Thr58和 Ser62激活 c-Myc。它可用于构建肺癌小鼠模型，以及诱导人肺癌细胞的增殖和存活。

(Z)-Metanicotine 2HCl 具有镇痛活性，可用于治疗中枢系统疾病。

Arecoline 是一种来自棕榈科植物槟榔的天然生物碱，是有效的烟碱和毒蕈碱乙酰胆碱受体的部分激动剂。Arecoline 具有抗焦虑和抗寄生虫活性，可诱导氧化应激，可用于研究阿尔茨海默病和老年性痴呆。

BPTU (BMS-646786) 是一种非核苷酸类P2Y1受体变构拮抗剂，能够阻断位于胃肠道神经肌肉接头的 P2Y1受体，具有抗血栓活性。

AZD-8529 mesylate 是高度选择性的可口服mGluR2正向调节剂，EC50值为 285 nM。它在 20-25 M 时，对 mGluR1、3、4、5、6、7 和 8 亚型没有显示正变构调节剂反应。

CP-809101 hydrochloride 是选择性 5-HT2C 受体激动剂，对于人类 5-HT2C 5-HT2B 5-HT2A 受体。

3-Pyridylacetic acid hydrochloride （3-PAA-HCl）尼克酸的高同系物，是尼古丁（和其它烟草生物碱）的分解产物，还可与胺、醇和羧酸等反应，也可在反应中作为酸催化剂。

Ajmalicine (Raubasine) 是一种有效的抗肾上腺素 (adrenolytic) 剂，优先阻断 α1-肾上腺素受体 (α1-adrenoceptor)。Ajmalicine 是一种可逆性但非竞争性尼古丁受体 (nicotine receptor) 完全抑制剂，IC50 为 72.3 μM。Ajmalicine 还可用于降压、蛇毒，具有镇静活性。

Cotinine (NIH-10498) 是烟草中的生物碱, 也是尼古丁的主要代谢物。Cotinine (NIH-10498) 是测量烟草烟雾成分的生物指标。

Myosmine 是存在于木贼中的一种烟草生物碱，对 a4b2 烟碱乙酰胆碱受体具有低亲和力，Ki 值为 3300 nM。

beta-Nicotyrine 是一种 Nicotine 的代谢物。它是一种微量的烟草生物碱，提取自普通烟草植物的叶子和香烟烟雾冷凝物。

SKF-83566 是一种具有血脑渗透性和口服活性的 D1 样多巴胺受体拮抗剂和一种较弱的竞争性 5-HT2 受体拮抗剂，Ki 为 11 nM。它是竞争性多巴胺转运蛋白抑制剂，可用于研究帕金森氏症和对尼古丁渴望的缓解的相关研究。

Hirsuteine 是提取自钩藤属植物中的吲哚生物碱。它可阻断离子渗透通过烟碱受体通道复合物，非竞争性地拮抗烟碱介导的多巴胺释放。

CB1R Allosteric modulator 3 是一种有效的 CB1R 调制剂。CB1R Allosteric modulator 3 抑制 cAMP 和 β-Arrestin ，可用于研究肥胖和尼古丁成瘾。

Varenicline dihydrochloride是一种选择性 α4β2 烟碱乙酰胆碱受体部分激动剂。

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

(+ -)-NICOTINE-d4 是 (+ -)-NICOTINE 的氘代化合物。

(1'S,2'S)-Nicotine-1'-Oxide-d3 是 (1'S,2'S)-Nicotine-1'-Oxide 的氘代化合物。(1'S,2'S)-Nicotine-1'-Oxide 的 CAS 号为 51095-86-4。

(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.

Nicotinic receptor agonist

UB 165 fumarate 是 nAChR 的激动剂，α4β2 亚型的部分激动剂，是 α3β2 亚型的全激动剂，其在大鼠脑中测得的结合到 [3H]-nicotine 的 Ki 值为 0.27 nM，可用于研究神经系统疾病。

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.

(±)-Nornicotine-d4 (pyridine-d4) 是 (±)-Nornicotine 的氘代化合物。(±)-Nornicotine 的 CAS 号为 5746-86-1。

Rivanicline hemioxalate (RJR-2403 hemioxalate; (E)-Metanicotine hemioxalate) 是一种神经元烟碱受体 (neuronal nicotinic receptor) 激动剂，对 α4β2 亚型有高度选择性(Ki= 26 nM)，比对于 α7 受体的选择性高1000倍(Ki=3.6 μM)。

R-(+)-Cotinine ((+)-Cotinine) 是一种尼古丁代谢物，在广泛的药理靶标中缺乏显着活性。R-(+)-Cotinine 可以增强人 α7nAChR 中的 Ach 诱发电流。

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.

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

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

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

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

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.

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

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

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.

α-Helical CRF (9-41) 是一种合成的皮质酮释放因子（CRF）拮抗剂。它在0.5至5 µM浓度范围内，能抑制CRF诱导的大鼠前叶垂体细胞释放促肾上腺皮质激素（ACTH）。在体内研究中，α-Helical CRF (9-41) (0.02-0.6 µmol/kg) 能够抑制未经麻醉的完整大鼠体内CRF诱导的ACTH释放，并在0.6 µmol/kg剂量下抑制大鼠应激诱导的ACTH释放。此外，α-Helical CRF (9-41) 在尼古丁诱导的条件性焦虑大鼠模型中增加社交互动时间，并减少小鼠的类似暴饮暴食的乙醇消费。

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].

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)

nAChR agonist CMPI hydrochloride is a potent and selective positive allosteric modulator (PAM) of nAChR containing a α4:α4 subunit interface. nAChR agonist CMPI hydrochloride enhances the response of (α4) 3 (β2) 2 nAChR to ACh (10 μM) with an EC 50 of 0.26 μM. nAChR agonist CMPI hydrochloride has potential for the research of nicotine dependence and many neuropsychiatric conditions associated with decreased brain cholinergic activity.

(S)-UFR2709 hydrochloride ((S)-UFR2709 HCl) 是一种具有选择性和高效性的 nAChR 拮抗剂，具有抗焦虑活性，抑制 α4β2 nAChR 和 α7 nAChR ，可用于研究尼古丁成瘾。

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.

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.

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

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.

Myosmine-2,4,5,6-d4 是 Myosmine 的氘代化合物。Myosmine 的 CAS 号为 532-12-7。Myosmine 是存在于木贼中的一种烟草生物碱，对 a4b2 烟碱乙酰胆碱受体具有低亲和力，Ki值为 3300 nM。