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Cholinergic Antagonists
Published in Sahab Uddin, Rashid Mamunur, Advances in Neuropharmacology, 2020
Vishal S. Gulecha, Manoj S. Mahajan, Aman Upaganlawar, Abdulla Sherikar, Chandrashekhar Upasani
Nicotine and lobeline like natural alkaloids stimulate autonomic ganglia peripherally. Nicotine was first isolated in 1828, from tobacco leaves, Nicotiana tabacum by Posselt and Reiman. Later, it was evaluated pharmacologically by Orfila in 1943. Langley and Dickinson carried experiments on the superior cervical ganglion of rabbits discovered that nicotine act on ganglia rather than preganglionic or postganglionic nerve fibers. Lobeline which was isolated from Lobelia inflate is less potent than nicotine. Various synthetic compounds were developed during the late 19th and early 20th century, showing distinguished effects at ganglionic receptor sites such as onium compounds like tetramehtylammonium (TMA) (Brunton et al., 2011).
Hydrolytic Enzymes for the Synthesis of Pharmaceuticals
Published in Peter Grunwald, Pharmaceutical Biocatalysis, 2019
Sergio González-Granda, Vicente Gotor-Fernández
(–)-Lobeline is a bioactive alkaloid used as am emetic or a respiratory stimulant, which is easily to produce by desymmetrisation of Lobelanidine through selective acylation of one of its hydroxyl groups (Chênevert and Morin, 2009). The combination of CAL-B and vinyl acetate, the ester used as both solvent and acyl donor, at 50°C for 18 h yielded the enantiopure (R,S)-monoacetate in 70% yield with little formation of the diacetate (3%) as byproduct (Scheme 9.35). Desymmetrisation of Lobelanidine for the synthesis of (–)-Lobeline.
Catalog of Herbs
Published in James A. Duke, Handbook of Medicinal Herbs, 2018
One Avante Garde publication “Herbal Highs”51 notes that it has been substituted for tobacco by people trying to kick the nicotine habit. It has a mildly euphoric marijuana-like quality while conferring to the mind a great sense of clarity. Taken as a tea, its effect is even more pronounced, acting simultaneously as both a relaxant and a stimulant. Three spoons of the stems are simmered in a liter of water.31 Feelings of mental clarity, happiness, and well-being are supposed to result from drinking the tea or taking lobelia capsule.37 If a bit of the leaf is chewed, there is a delayed stinging reaction like that from chewing tobacco leaves.1 It has been used to treat angina pectoris, asthma, bronchitis, convulsions, diptheria, epilepsy, erysipelas, hysteria, narcosis, ophthalmia, pneumonia, spasm, tetanus, tonsilitis, and whooping cough. It is convulsant, diaphoretic, expectorant, nauseant, and sedative.12 Lobeline is used for respiratory failures resulting from anesthesia or narcotic overdose. American Indians used the powdered leaves to treat dysentery. The minute seeds, which impart a greasy stain to paper, contain a higher percentage of the alkaloid lobeline than the rest of the plant. This alkaloid occurs in certain commercial preparations used to stop the tobacco smoking habit. Once again, there is scientific reason for our ancestors prescribing Indian tobacco to those who wish to give up true tobacco. The FDA has allowed the sale of pills containing lobeline as a smoking deterrent (“Washington Post”, January 11, 1982).
The effect of electronic cigarettes exposure on learning and memory functions: behavioral and molecular analysis
Published in Inhalation Toxicology, 2021
Karem H. Alzoubi, Rahaf M. Batran, Nour A. Al-Sawalha, Omar F. Khabour, Nareg Karaoghlanian, Alan Shihadeh, Thomas Eissenberg
The hippocampus plays an important role in the learning and memory. The dentate gyrus, and the Cornu ammonis 1 (CA1), Cornu ammonis 2 (CA2), and Cornu ammonis 3 (CA3) regions are among the involved hippocampal subregions. The corticohippocampal circuit, either in its classical or nonclassical pathways, participates in the process of memory formation (Basu and Siegelbaum 2015). Nicotinic acetylcholine receptors (nAChRs) are major type of receptors that are expressed in several areas of hippocampus. nAChRs regulate the release of several neurotransmitters in hippocampus and modulate synaptic plasticity and eventually mediates learning and memory (Placzek et al. 2009). The administration of nicotine enhanced learning and memory in aged rats (Arendash et al. 1995), and chronic stress and Alzheimer’s Disease animal models (Alkadhi 2011). Further, it has been shown that the administration of nAChRs agonists such as GTS-21 and lobeline resulted in enhanced learning and memory in animal models (Decker et al. 1993; Arendash et al. 1995). However, other studies revealed contradictory findings about the effect of nicotine. It has been shown that the administration of nicotine-induced learning and memory impairment by enhancing oxidative stress in the brain (Hritcu et al. 2009). Further, nicotine induced oxidative stress in the brain of young and old rats (Jain and Flora 2012).
Understanding the implications of the biobehavioral basis of nicotine addiction and its impact on the efficacy of treatment
Published in Expert Review of Respiratory Medicine, 2018
Nikki Bozinoff, Bernard Le Foll
As mentioned earlier, different subunits of nAChRs have been involved in nicotine addiction process. The focus has been initially on the role of β2 and α4 subunits, notably based on the findings that β2 subunit deletion decreases sensitivity to nicotine’s reinforcing effects [11] and the fact that α4 subunit overexpression increases sensitivity to nicotine reinforcement [51]. Varenicline and cytisine, both α4β2* receptor partial agonists, are used in the treatment of tobacco use disorder and are explored in more detail below. Lobeline, also a nicotinic receptor partial agonist, was the subject of a Cochrane review which found no evidence that it is helpful for smoking cessation [52]. Mecamylamine, a nonselective nicotine receptor antagonist, has been explored for its potential to decrease nicotine’s reinforcing effects and was the subject of two trials that used it in combination with NRT [53,54]. At this time, there is inconclusive evidence to support the use of mecamylamine in combination with NRT [4].
A short guide to insect oviposition: when, where and how to lay an egg
Published in Journal of Neurogenetics, 2019
Kevin M. Cury, Benjamin Prud’homme, Nicolas Gompel
D. melanogaster females also use gustatory cues to make oviposition decisions. As mentioned above, D. melanogaster sensory systems are tuned to many chemicals produced by fruit or during fermentation, some of which stimulate egg-laying behavior. For instance, females are stimulated to lay eggs when exposed to lobeline (Joseph & Heberlein, 2012), sugar (Schwartz, Zhong, Bellemer, & Tracey, 2012; Yang, Belawat, Hafen, Jan, & Jan, 2008; Yang, He, & Stern, 2015), acids (Chen & Amrein, 2017; Joseph et al., 2009), and polyamines (Hussain et al., 2016), all of which are abundant in overripe or fermenting fruits. All these compounds are detected by different gustatory receptors or ionotropic receptors (IRs), expressed in distinct subsets of gustatory neurons of the proboscis or the legs. Interestingly though, these chemical compounds have been shown to either elicit opposite behaviors, such as oviposition attraction and positional aversion, or to modulate oviposition preference in a context-dependent manner. Acetic acid, for instance, is aversive when it is detected by antennal olfactory sensory neurons, but acid detection by gustatory neurons of the forelegs stimulates egg-laying (Chen & Amrein, 2017; Joseph et al., 2009). Similarly, lobeline stimulates oviposition, but females avoid staying on it for too long (Joseph & Heberlein, 2012). In this case, the positional repulsion and oviposition stimulation are controlled by distinct sets of gustatory sensory neurons expressing the same gustatory receptor (Gr66) tuned to bitter compounds. A neuronal population of the leg dictates positional aversion, while a set of neurons in the internal mouthpart lining the pharynx stimulates oviposition (Joseph & Heberlein, 2012). In a converse manner, D. melanogaster females are strongly attracted to volatiles polyamines, but they avoid polyamine-rich agar oviposition substrates (Hussain et al., 2016). The preference is reversed, though, when polyamines are mixed with fruits: in this context females prefer to lay their eggs on polyamine-containing substrates (Hussain et al., 2016).