Nicotinic receptors acetylcholine and

Dajas-Bailador F, Wonnacott S (2004) Nicotinic acetylcholine receptors and the regulation of neuronal signalling. Trends Pharmacol Sci 25 317-324... 

The AMPA receptors for glutamate, the nicotinic acetylcholine receptor and the 5-HT3-receptor for serotonin are cation channels (Table 1). When they open, the major consequence is a sudden entry of Na+, depolarization and an excitatory postsynaptic potential (EPSP Fig. 1). 

Lukas, RJ, Changeux, JP, Le Novere, N, Albuquerque, EX, Balfour, DJ, Berg, DK, Bertrand, D, Chiappinelli, VA, Clarke, PB, Collins, AC, Dani, JA, Grady, SR, Kellar, KJ, Lindstrom, JM, Marks, MJ, Quik, M, Taylor, PW and Wonnacott, S (1999) International Union of Pharmacology. XX. Current status of the nomenclature for nicotinic acetylcholine receptors and their subunits. Pharmacol. Rev. 51(2) 397 01. 

Unwin, N (1995) Acetylcholine receptor channel imaged in the open state. Nature 373 37-43. Unwin, N (2000) Nicotinic acetylcholine receptor and the structural basis of fast synaptic transmission. Phil. Trans. Roy. Soc. Lond. Ser. B 355 1813-1829. 

Edmonds, B., Gibb, A. J., and Colquhoun, D., Mechanisms of activation of muscle nicotinic acetylcholine receptors and the time course of endplate currents, Annu. Rev. Physiol., 57, 469-493, 1995. 

Karlin, A., Akabas, M.H. Toward a structural basis for the function of nicotinic acetylcholine receptors and their cousins. Neuron. 15 1231, 1995. 

Figure 6.2. Diagrammatic representation of the 5-HT3 receptor. The 5-HT3 receptor is distinct from the other 5-HT receptor subtypes, in that it is a ligand gated ion channel that is permeable to sodium and potassium. The 5-HT3 receptor is structurally similar to the nicotinic acetylcholine receptor and is composed of five sub-units. Two sub-units have been cloned, 5-HT3A and 5-HT35, and homomeric (5-HT3A) and heteromeric (5-HT3a/5-HT3b) forms of the receptor have both been...

Nicotine affects the nervous system, interacting with the nicotinic acetylcholine receptors, and the tight binding is partially accounted for by the structural similarity between acetylcholine and nicotine. Curare-like antagonists also block nicotinic acetylcholine receptors (see Box 6.7). There are other acetylcholine receptors, termed muscarinic, that are triggered by the alkaloid muscarine. The tropane alkaloid hyoscyamine (see Box 10.9) binds to muscarinic acetylcholine receptors. 

There is considerable diversity among nicotinic acetylcholine receptors, and at least one source of this diversity is the multiplicity of acetylcholine receptor genes. Cholinergic-nicotinic receptors in skeletal muscle are different from those in autonomic ganglia and the central nervous system. 

Pyrantel pamoate (Antiminth) is a agonist at the nicotinic acetylcholine receptor, and its actions result in depolarization and spastic paralysis of the helminth muscle. Its selective toxicity occurs primarily because the neuromuscular junction of helminth muscle is more sensitive to the drug than is mammalian muscle. This drug is administered orally, and because very little is absorbed, high levels are achieved in the intestinal tract. Less than 15% of the drug and its metabolites are excreted in urine. 

The primary sequences of important channel peptides, such as the nicotinic acetylcholine receptors, and sodium, potassium, and calcium channels, have been determined by the innovative work of the late professor Numa and his group. " Thereafter, various structural models on the basis of empirical as well as molecular mechanics or molecular dynamics calculations were proposed " and tested by specific point mutation studies. 

Smulders CJ et al Selective effects of carbamate pesticides on rat neuronal nicotinic acetylcholine receptors and rat brain acetylcholinesterase. Toxicol Appl Pharmacol 2003 193 139. [PMID 14644616]... 

Wenger, B. W., Bryant, D. L., Boyd, R. T., McKay, D. B. Evidence for Spare Nicotinic Acetylcholine Receptors and a P4 Subunit in Bovine Adrenal Chromaffin Cells Studies... 

Luo S, Kulak JM, Cartier GE, Jacobsen RB, Yoshikami D, Olivera BM, McIntosh JM (1998) alpha-conotoxin AuIB selectively blocks alpha3 beta4 nicotinic acetylcholine receptors and nicotine-evoked norepinephrine release. J Neurosci 18 8571-9 MacDermott AB, Role LW, Siegelbaum S A (1999) Presynaptic ionotropic receptors and the control of transmitter release. Annu Rev Neurosci 22 443-85 Madden DR (2002) The structure and function of glutamate receptor ion channels. Nat Rev Neurosci 3 91-101... 

Liu Y, Ford B, Mann MA, Fischbach GD. 2001. Neuregulins increase alpha7 nicotinic acetylcholine receptors and enhance excitatory synaptic transmission in GABAergic interneurons of the hippocampus. J Neurosci 21 5660-5669. 

Dani JA, Bertrand D. 2007. Nicotinic acetylcholine receptors and nicotinic cholinergic mechanisms of the central nervous system. Annu Rev Pharmacol Toxicol 47 699-729. 

The modes of action of different alkaloids are diverse. For example, nicotine binds to and affects nicotinic acetylcholine receptors and shows toxicity. A recent molecular 3D model suggests that both acetylcholine and nicotine bind to the same pocket formed in a nicotinic acetylcholine receptor.15 Morphine binds to and activates opioid receptors, transmembrane-spanning G protein-coupled receptors, in the central nervous system of humans.16 Caffeine, which is structurally similar to adenine, inhibits cyclic AMP phosphodiesterase activity and inhibits the degradation of cAMP, thus exerting a toxic effect on insects 17 in human beings, binding of caffeine to the adenosine A2A receptor induces wakefulness.18 Atropine binds to muscarinic acetylcholine receptors, competing with acetylcholine, and blocks neurotransmission.1... 

Olefinic azacyclic derivatives, (I), prepared by Dull (5) selectively activated nicotinic acetylcholine receptors and were used in the treatment of neurodegenerative diseases. 

The insect GABA receptor-chloride ionophore complex is found in the CNS and also at peripheral neuromuscular sites. GABA receptors belong to a superfamily of ligand-gated ion channels known as Cys-loop receptors that include nicotinic acetylcholine receptors and glutamate-gated chloride channels (Lester, 2004). Cys-loop receptors are so named because... 

Portugal GS, Gould TJ (2008) Genetic vtiriability in nicotinic acetylcholine receptors and nicotine addiction converging evidence from human and animal research. Behav Brain Res 193 1-16... 

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