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Acetylcholine receptors treatment

Antagonists of muscarinic acetylcholine receptors had widely been used since 1860 for the treatment of Parkinson s disease, prior to the discovery of l-DOPA. They block receptors that mediate the response to striatal cholinergic interneurons. The antiparkinsonian effects of drugs like benzatropine, trihexyphenidyl and biper-iden are moderate the resting tremor may sometimes respond in a favorable manner. The adverse effects, e.g., constipation, urinary retention, and mental confusion, may be troublesome, especially in the elderly. [Pg.166]

Ke, L., Eisenhour, C., Bencherif, M., Lukas, R. Effects of chronic nicotine treatment on expression of diverse nicotinic acetylcholine receptor subtypes. I. Dose- and time-dependent effects of nicotine treatment. J. Pharmacol. Exp. Ther. 286 825, 1998. [Pg.47]

Zhang, X., Gong, Z.-H., Hellstrom-Lindahl, E., Nordberg, A. Regulation of a4(32 nicotinic acetylcholine receptors in M10 cells following treatment with nicotinic agents. Neuroreport. 6 313, 1994. [Pg.48]

Harkness, P., Millar, N. Changes in conformation and subcellular distribution of a4b2 nicotinic acetylcholine receptors revealed by chronic nicotine treatment and expression of subunit chimeras. J. Neurosci. 22 10172, 2002. [Pg.48]

Wang, F., Nelson, M., Kuryatov, A. et al. Chronic nicotine treatment upregulates human a3 32 but not a3P4 acetylcholine receptors stably transfected in human embryonic kidney cells. J. Biol. Chem. 1998 28721, 1998. [Pg.48]

Fluorine has been used to modulate the basicity of amines which may lead to an improvement in brain exposure. Recently, the discovery of a series of a4(32 nicotinic acetylcholine receptor (nAChR) potentiators as possible treatment for Parkinson s disease and schizophrenia was were disclosed [40]. Optimization of isoxazole 40 included the bioisosteric replacement of the central amide by an imidazole ring. Introduction of a fluorine at the 6-position of the phenyl ring provided compound 41. This compound had excellent potency but was determined to be a substrate for P-gp (efflux ratio >10). In an attempt to reduce amine basicity and decrease the efflux propensity, the 4-fluoropiperidine 42 was identified which retained potency and had significantly reduced P-gp efflux liability (efflux ratio 1). CNS penetration of 42 was observed in rodents following intraperitoneal (IP) treatment at 5mg/kg and showed a brain concentration of 6.5 gM. [Pg.441]

Fucile S (2004) Ca + permeability of nicotinic acetylcholine receptors. Cell Calcium 35 1-8 Gaddnas H, Pietila K, Ahtee L (2000) Effects of chronic oral nicotine treatment and its withdrawal on locomotor activity and brain monoamines in mice. Behav Brain Res 113 65-72 Geisler S, Derst C, Veh RW, Zahm DS (2007) Glutamatergic afferents of the ventral tegmental area in the rat. J Neurosci 27 5730-5743... [Pg.199]

Ridley DL, Pakkanen J, Wonnacott S (2002) Effects of chronic drug treatments on increases in intracellular calcium mediated by nicotinic acetylcholine receptors in SH-SY5Y cells, Br J Pharmacol 135 1051-1059... [Pg.204]

Muscarinic Agonists. Another approach is to use a medication that directly activates subtypes of the acetylcholine receptors, namely, muscarinic receptor agonists. The muscarinic agonists used in the past have not been effective. This includes bethanecol, pilocarpine, and oxotremorine. This line of treatment, however, has not been entirely abandoned, and several medications are currently in testing. [Pg.299]

Riekkinen M, Sirvio J, Toivanen T, et al Combined treatment with a 5-HTj, receptor agonist and a muscarinic acetylcholine receptor antagonist disrupts water maze navigation behaviour. Psychopharmacology 122 137-146, 1995... [Pg.732]

The addiction to nicotine that makes smoking withdrawal so difficult for many is believed to be mediated by a subset of nicotinic acetylcholine receptors. A bridged bicylcic aryl-benzepine that acts as a partial agonist at those sites is now approved as an aid for tobacco smoking withdrawal. The synthesis starts with the known ben-zonorbomenone (3-1). Treatment of that compound with selenium dioxide leads to the oxidation of the carbon adjacent to the carbonyl group and thus the formation... [Pg.497]

Pesticides derived from natural sources include nicotine, rotenone, and pyrethrum. Nicotine is obtained from the dried leaves of Nicotiana tabacum and N rustica. It is rapidly absorbed from mucosal surfaces the free alkaloid, but not the salt, is readily absorbed from the skin. Nicotine reacts with the acetylcholine receptor of the postsynaptic membrane (sympathetic and parasympathetic ganglia, neuromuscular junction), resulting in depolarization of the membrane. Toxic doses cause stimulation rapidly followed by blockade of transmission. These actions are described in Chapter 7. Treatment is directed toward maintenance of vital signs and suppression of convulsions. [Pg.1220]

One of the best-understood autoimmune diseases is myasthenia gravis, a condition associated with a decrease in the number of functional post-synaptic nicotinic acetylcholine receptors (Fig. 30-23) in neuromuscular junctions. e The resulting extreme muscular weakness can be fatal. Myasthenia gravis is not rare and affects about one in 10,000 peopled An interesting treatment consists of the administration of physostigmine, diisopropyl-phosphofluoridate (Chapter 12, Section C,l), or other acetylcholinesterase inhibitors (Box 12-E). These very toxic compounds, when administered in controlled amounts, permit accumulation of higher acetylcholine concentration with a resultant activation of muscular contraction. The same compounds... [Pg.1864]


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Acetylcholine receptors

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