Nicotine
Minor tobacco alkaloids as biomarkers for tobacco use: comparison of users of cigarettes, smokeless tobacco, cigars, and pipes. (1/42)
OBJECTIVES: This study (1) determined levels of various tobacco alkaloids in commercial tobacco products. (2) determined urinary concentrations, urinary excretion, and half-lives of the alkaloids in humans; and (3) examined the possibility that urine concentrations of nicotine-related alkaloids can be used as biomarkers of tobacco use. METHODS: Nicotine intake from various tobacco products was determined through pharmacokinetic techniques. Correlations of nicotine intake with urinary excretion and concentrations of anabasine, anatabine, nornicotine, nicotine, and cotinine were examined. By using urinary excretion data, elimination half-lives of the alkaloids were calculated. RESULTS: Alkaloid levels in commercial tobacco products, in milligrams per gram, were as follows: nicotine, 6.5 to 17.5; nornicotine, 0.14 to 0.66; anabasine, 0.008 to 0.030; and anatabine, 0.065 to 0.27. Measurable concentrations of all alkaloids were excreted in the urine of most subjects smoking cigarettes, cigars, and pipes and using smokeless tobacco. Correlations between nicotine intake and alkaloid concentrations were good to excellent. CONCLUSIONS: Anabasine and anatabine, which are present in tobacco but not in nicotine medications, can be used to assess tobacco use in persons undergoing nicotine replacement therapy. (+info)Insecticidal and neural activities of candidate photoaffinity probes for neonicotinoid binding sites. (2/42)
Photoreactive derivatives of imidacloprid and its nitromethylene analogue were synthesized as candidate photoaffinity probes for identifying the amino acid residues of nicotinic acetylcholine receptors (nAChRs) that interact with the neonicotinoid insecticides. When the candidate probes were injected into American cockroaches, the nerve cord neural activity initially increased, then ceased and death of the insect followed. Both the nerve cord and toxicity were enhanced by changing the photoreactive substituent from the para position to the meta position on the spacer benzyl moiety. When tested on a Drosophila SAD/chicken beta2 hybrid, recombinant nAChR expressed in Xenopus oocytes, the nitromethylene candidate probes showed agonist activity similar to that previously observed for imidacloprid. (+info)Benzylidene analogs of anabaseine display partial agonist and antagonist properties at the mouse 5-hydroxytryptamine(3A) receptor. (3/42)
The nicotinic receptor drug candidate, 3-(2,4-dimethoxybenzylidene)-anabaseine (also known as GTS-21; DMXBA), its hydroxy metabolites, and some related analogs were evaluated with the two-electrode voltage-clamp technique in mouse 5-hydroxytryptamine (5-HT)(3A) receptors expressed in Xenopus oocytes. Although DMXBA lacked partial agonist activity, its hydroxy-benzylidene metabolites and related analogs were partial agonists, displaying the following rank order of potency (EC(50)) and apparent efficacy: 5-HT, 0.9 +/- 0.06 microM (100% efficacy) > 3-(2-hydroxy,4-methoxybenzylidene)-anabaseine (2-OH-MBA), 2.0 +/- 0.3 microM (63% efficacy) > 3-(2,4-dihydroxybenzylidene)-anabaseine, 2.6 +/- 0.3 microM (63% efficacy) > 3-(2-methoxy,4-hydroxybenzylidene)-anabaseine, 17.2 +/- 1.0 microM (30% efficacy). To examine the influence of a benzylidene ring hydroxy substituent, the agonist actions of the three possible monohydroxy isomers were examined. The rank order of potency, based on EC(50) determinations, and apparent efficacy was: 3-(2-hydroxybenzylidene)-anabaseine, 20.3 +/- 2.6 microM (63% efficacy) > 3-(4-hydroxybenzylidene)-anabaseine, 32.3 +/- 5.9 microM (14% efficacy) > 3-(3-hydroxybenzylidene)-anabaseine (3-OH-BA) (no agonist activity). Both DMXBA and 3-OH-BA antagonized 5-HT-mediated currents, with IC(50) values of 15.7 +/- 0.9 and 27.5 +/- 4.7 microM, respectively. DMXBA demonstrated both competitive and noncompetitive forms of antagonism over the range of concentrations tested. These results suggest that a hydroxy substituent at the 2' position of the benzene ring is necessary and sufficient for partial agonist activity; substitution at the 4' position with a hydroxy or methoxy group further enhances agonist potency. Because 2-OH-MBA is a primary metabolite of DMXBA, it may contribute to the physiological, biochemical, and behavioral effects of the parent compound when administered in vivo. (+info)Comparative pharmacology of rat and human alpha7 nAChR conducted with net charge analysis. (4/42)
1. Pharmacological studies of alpha7 nicotinic acetylcholine receptors are confounded by the fact that rapid desensitization to high agonist concentration causes alpha7 peak responses to occur well in advance of complete solution exchange. For this reason, peak currents are an invalid measure of response to applied agonist concentrations. We show that results comparable to those that have been corrected for instantaneous concentration are obtained if net charge is used as the measure of receptor response. 2. Dose response curves obtained with these methods indicate that alpha7 receptors are approximately 10 fold more sensitive to agonist than previously reported. The agonists, ACh, choline, cytisine, GTS-21, 4OH-GTS-21 and 4-MeO-CA have the same rank order potency for both human and rat receptors: 4-MeO-CA > 4OH-GTS-21 > GTS-21 > cytisine > ACh > choline. However, differences in efficacy exist between rat and human receptors. GTS-21 is more efficacious for rat than human alpha7 receptors and cytosine more efficacious for human than rat alpha7 receptors. 3. Choline is the least potent agonist for both human and rat alpha7, with a potency approximately 10 fold lower than that of ACh. While the EC50 for the activation of alpha7 receptors by choline (400-500 microM) is outside the normal physiological range (10-100 microM), choline can nonetheless produce detectable levels of channel activation in the physiological concentration range. Since these concentrations are relatively non-desensitizing, the contribution of choline-activated alpha7 receptor current may play a significant role in the regulation of calcium homeostasis in alpha7-expressing neurons. (+info)Simultaneous analysis of nicotine, nicotine metabolites, and tobacco alkaloids in serum or urine by tandem mass spectrometry, with clinically relevant metabolic profiles. (5/42)
BACKGROUND: Assessment of nicotine metabolism and disposition has become an integral part of nicotine dependency treatment programs. Serum nicotine concentrations or urine cotinine concentrations can be used to guide nicotine patch dose to achieve biological concentrations adequate to provide the patient with immediate relief from nicotine withdrawal symptoms, an important factor in nicotine withdrawal success. Absence of nicotine metabolites and anabasine can be used to document abstinence from tobacco products, an indicator of treatment success. METHODS: The procedure was designed to quantify nicotine, cotinine, trans-3'-hydroxycotinine, anabasine, and nornicotine in human serum or urine. The technique required simple extraction of the sample with quantification by HPLC-tandem mass spectrometry. RESULTS: The procedure for simultaneous analysis of nicotine, its metabolites, and tobacco alkaloids simultaneously quantified five different analytes. Test limit of quantification, linearity, imprecision, and accuracy were adequate for clinical evaluation of patients undergoing treatment for tobacco dependency. The test readily distinguished individuals who had no exposure to tobacco products from individuals who were either passively exposed or were abstinent past-tobacco users from those who were actively using a tobacco or nicotine product. CONCLUSIONS: Nicotine, cotinine, trans-3'-hydroxycotinine, nornicotine, and anabasine can be simultaneously and accurately quantified in either serum or urine by HPLC-tandem mass spectrometry with imprecision <10% at physiologic concentrations and limits of quantification ranging from 0.5 to 5 micro g/L. Knowledge of serum or urine concentrations of these analytes can be used to guide nicotine replacement therapy or to assess tobacco abstinence in nicotine dependency treatment. These measurements are now an integral part of the clinical treatment and management of patients who wish to overcome tobacco dependence. (+info)Anabasine and anatabine as biomarkers for tobacco use during nicotine replacement therapy. (6/42)
In this study we determined urine concentration of the tobacco alkaloids anabasine and anatabine, nicotine and its metabolites cotinine, and nornicotine in 99 cigarette smokers and 205 smokeless tobacco users. We also investigated the possibility that anabasine and anatabine can be used as biomarkers for tobacco use during nicotine replacement therapy. Urine samples and data on self-reported tobacco use were obtained from subjects enrolled in tobacco cessation programs. Urine concentrations of tobacco alkaloids and metabolites were measured and correlated with self-reported tobacco use. Concentrations of anabasine and anatabine were used to validate abstinence in smokeless tobacco users who used nicotine gum as part of the therapy. Correlations of alkaloid concentration with self-reported tobacco use before treatment ranged from fair to poor. In subjects abstaining from smokeless tobacco but using nicotine gum, anabasine and anatabine levels were below the cut-point of 2 ng/ml despite high concentrations of nicotine and cotinine resulting from nicotine gum use. Anabasine and anatabine concentrations in urine can be used to validate abstinence or measure the extent of tobacco use in persons undergoing nicotine replacement therapy. (+info)Regulation of neuronal function by choline and 4OH-GTS-21 through alpha 7 nicotinic receptors. (7/42)
A unique feature of alpha7 nicotinic acetylcholine receptor physiology is that, under normal physiological conditions, alpha7 receptors are constantly perfused with their natural selective agonist, choline. Studying neurons of hypothalamic tuberomammillary (TM) nucleus, we show that choline and the selective alpha7 receptor agonist 4OH-GTS-21 can regulate neuronal functions directly, via activation of the native alpha7 receptors, and indirectly, via desensitizing those receptors or transferring them into a state "primed" for desensitization. The direct action produces depolarization and thereby increases the TM neuron spontaneous firing (SF) rate. The regulation of the spontaneous firing rate is robust in a nonphysiological range of choline concentrations >200 microM. However, modest effects persist at concentrations of choline that are likely to be attained perineuronally under some conditions (20-100 microM). At high physiological concentration levels, the indirect choline action reduces or even eliminates the responsiveness of alpha7 receptors and their availability to other strong cholinergic inputs. Similarly to choline, 4OH-GTS-21 increases the TM neuron spontaneous firing rate via activation of alpha7 receptors, and this regulation is robust in the range of clinically relevant concentrations of 4OH-GTS-21. We conclude that factors that regulate choline accumulation in the brain and in experimental slices such as choline uptake, hydrolysis of ACh, membrane phosphatidylcholine catabolism, and solution perfusion rate influence alpha7 nAChR neuronal and synaptic functions, especially under pathological conditions such as stroke, seizures, Alzheimer's disease, and head trauma, when the choline concentration in the CSF is expected to rise. (+info)Components of cigarette smoke inhibit expansion of oocyte-cumulus complexes from porcine follicles. (8/42)
The role of alkaloids in cigarette smoke was investigated in the cumulus expansion of oocyte-cumulus complexes (OCC) isolated from large antral porcine follicles. Suppression of the cumulus expansion stimulated by FSH was observed in the presence of different concentration of cadmium, anabasine and nicotine but not its metabolite cotinine. There were comparable inhibitory effects of cadmium and nicotine on the synthesis and accumulation of hyaluronic acid in the cell/matrix compartment of OCC. The inhibitory effect of tested compounds on the cumulus expansion was accompanied by decreased progesterone synthesis by cumulus cells during 42 h incubation of OCC with FSH. The results suggest that cigarette smoking may affect intrafollicular processes, which are responsible for normal ovulation and fertilization. (+info)Anabasine is a toxic alkaloid found in the tobacco plant (Nicotiana tabacum) and some other species of the Nicotiana genus. It is one of the main alkaloids responsible for the addictive properties of tobacco and is also responsible for many of the harmful effects of smoking, including respiratory problems, heart disease, and cancer. In the medical field, anabasine is not typically used as a therapeutic agent. However, it has been studied for its potential as an anti-inflammatory and anti-cancer agent. Some studies have suggested that anabasine may have anti-inflammatory effects by inhibiting the production of inflammatory cytokines, and it has also been shown to have anti-cancer effects by inhibiting the growth of cancer cells in vitro. Despite these potential benefits, anabasine is still considered a toxic substance and is not recommended for use as a therapeutic agent. The use of tobacco products, which contain anabasine and other harmful chemicals, is strongly discouraged by medical professionals due to the serious health risks associated with smoking.
Nicotine is a highly addictive psychoactive substance found in tobacco plants. It is a stimulant that affects the central nervous system and can produce feelings of pleasure and relaxation. In the medical field, nicotine is used as a treatment for smoking cessation, as it can help reduce cravings and withdrawal symptoms associated with quitting smoking. Nicotine is available in various forms, including patches, gum, lozenges, inhalers, and e-cigarettes. However, it is important to note that nicotine is also highly toxic and can be dangerous if not used properly. Long-term use of nicotine can lead to addiction, respiratory problems, heart disease, and other health issues.
Alkaloids are a diverse group of naturally occurring organic compounds that are derived from plants and have a basic or alkaline nature. They are often found in the leaves, seeds, bark, and roots of plants and are known for their bitter taste and pharmacological properties. In the medical field, alkaloids have been used for centuries as traditional remedies for a variety of ailments, including pain relief, fever reduction, and digestive disorders. Many alkaloids have also been isolated and synthesized for use in modern medicine, particularly in the treatment of cancer, infections, and neurological disorders. Some well-known examples of alkaloids include caffeine, nicotine, morphine, codeine, and quinine. These compounds have a wide range of effects on the body, including stimulating the central nervous system, reducing pain and inflammation, and affecting heart rate and blood pressure. However, it is important to note that many alkaloids can also be toxic in high doses and can cause side effects such as nausea, vomiting, and dizziness. Therefore, the use of alkaloids in medicine is typically closely monitored and regulated by healthcare professionals.
Anabasine
Pyridine alkaloids
Anabaseine
Xiphotheca
Caffeine
Parasympathomimetic drug
Acetylcholinesterase inhibitor
Streptosolen
Nicotiana glauca
Anabasis aphylla
Anabasis (plant)
Lupinine
Nicotiana tabacum
TC-1698
May Berenbaum
Project CHATTER
Rivanicline
Health effects of electronic cigarettes
Trail pheromone
Alkaloid
Construction of electronic cigarettes
C10H14N2
List of MeSH codes (D03)
Piperidine
List of insecticides
Alpha-7 nicotinic receptor
Nicotine
Anatabine
Nicotiana
Tobacco
UCOT I
NTF Takeover w/ Anabasine • Charlatan • Dinzy • Stiglitz | mtljtm
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Anatabine7
- Lastly, anatabine and anabasine are nicotine analogs in tobacco product, and are precursors for nitrosamines. (cdc.gov)
- Anabasine and anatabine are minor alkaloids in tobacco products and are precursors for tobacco-specific nitrosamines (TSNAs). (cdc.gov)
- The concentrations of urinary anabasine and anatabine were measured in a representative sample of U.S. adults who smoked cigarettes (N = 770) during the 2013-2014 National Health and Nutrition Examination Survey (NHANES) study cycle, which was the first cycle where urinary anabasine and anatabine data became available. (cdc.gov)
- Weighted geometric means (GM) and geometric least squares means (LSM) with 95% confidence intervals were calculated for urinary anabasine and anatabine categorized by tobacco-use status [cigarettes per day (CPD) and smoking frequency] and demographic characteristics. (cdc.gov)
- Smoking 20 CPD was associated with 3.6 higher anabasine GM and 4.8 higher anatabine GM compared with smoking <10 CPD. (cdc.gov)
- Compared with non-daily smoking, daily smoking was associated with higher GMs for urinary anabasine (1.41 ng/mL vs. 6.28 ng/mL) and anatabine (1.62 ng/mL vs. 9.24 ng/mL). (cdc.gov)
- This is the first time that anabasine and anatabine are reported for urine collected from a U.S. population-representative sample of NHANES study participants, providing a snapshot of exposure levels for adults who smoked during 2013-2014. (cdc.gov)
Cotinine2
- 6. Influence of nicotine, cotinine, anabasine and cigarette smoke extract on human granulosa cell progesterone and estradiol synthesis. (nih.gov)
- Previously, the identification of ancient plant residues relied on the detection of a limited number of biomarkers, such as nicotine, anabasine, cotinine and caffeine. (wsu.edu)