Nicotinic acetylcholine receptor modulators

Rousseau SJ, Jones IW, Pullar lA, Wonnacott S (2005) Presynaptic alpha7 and non-alpha7 nicotinic acetylcholine receptors modulate [ H]d-aspartate release from rat frontal cortex in vitro. Neuropharmacology 49 59-72... [Pg.204]

Imoto, M., Iwanami, T., Akabane, M. (Suntory Ltd.) Use of cyclic amidine compounds as nicotinic acetylcholine receptor modulators, WO0181334 (2001). [Pg.443]

Alkondon M, Albuquerque EX (2002) A non-alpha 7 nicotinic acetylcholine receptor modulates excitatory input to hippocampal CA1 interneurons. J Neurophysiol 87 651 4... [Pg.514]

Ronde P, Nichols RA (1998) High calcium permeability of serotonin 5-HT3 receptors on presynaptic nerve terminals from rat striatum. J Neurochem 70 1094-1103 Rosenstein RE, Chuluyan HE, Cardinali DP (1990) Presynaptic effects of gamma-aminobutyric acid on norepinephrine release and uptake in rat pineal gland. J Neural Transm 82 131—40 Rousseau SJ, Jones IW, Pullar IA, Wonnacott S (2005) Presynaptic [alpha]7 and non-[alpha]7 nicotinic acetylcholine receptors modulate [3H]d-aspartate release from rat frontal cortex in vitro. Neuropharmacology 49 59... [Pg.524]

Holladay, M.W., Cosford, N.D.P., McDonald, I.A., 1999. Natural products as a source of nicotinic acetylcholine receptor modulators and leads for dmg discovery. In Americ, S.P., Brioni, J.D. (Eds.), Neuronal Nicotinic Receptors Pharmacology and Therapeutic Opportunities. Wiley-Liss, New York, pp. 253-270. [Pg.44]

DISCOVERY OF ABT-594 AND RELATED NEURONAL NICOTINIC ACETYLCHOLINE RECEPTOR MODULATORS AS ANALGESIC AGENTS ... [Pg.85]

ABT-594 evolved from several years of research at Abbott Laboratories on nicotinic acetylcholine receptor modulators, directed initially toward treatment of Alzheimer s disease, and subsequently toward novel agents for treatment of pain. ABT-594 represents the first of a new generation of nAChR modulators to be tested as an analgesic agent in human clinical trials. The outcome of these studies with respect to both efficacy and... [Pg.110]

Galantamine is a ChE inhibitor, which elevates acetylcholine in the cerebral cortex by slowing the degradation of acetylcholine.37 It also modulates the nicotinic acetylcholine receptors to increase acetylcholine from surviving presynaptic nerve terminals. In addition, it may increase glutamate and serotonin levels. The clinical benefit of action of these additional neurotransmitters is unknown. [Pg.519]

Ochoa, E., Chattopadhyay, A., McNamee, M. Desensitization of the nicotinic acetylcholine receptor Molecular mechanisms and effect of modulators. Cell Mol. Neurobiol. 9 141, 1989. [Pg.47]

Hopfield, J.F., Tank, D.W., Greengard, P. and Huganir, R.L. (1988) Functional modulation of the nicotinic acetylcholine receptor by tyrosine phosphorylation. Nature 336, 677-680. [Pg.472]

Huginir, R.L. and Miles, K. (1989) Functional modulation of the nicotinic acetylcholine receptors. Critical Reviews of Biochemical and Molecular Biology 24, 183-215. [Pg.472]

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]

Nicotine is an agonist at the nicotinic acetylcholine receptor (nAChR). Activation of this receptor depolarizes target cells (see Ch. 11). nAChRs are composed of five subunits surrounding a central ion-channel pore. Twelve different nicotinic receptor subunits are expressed in the nervous system (a2-oclO and (32—134). Of these, a subset is expressed in the VTA (a3-a7 and P2—134). It is thought that a7 receptors form homomeric receptors a3, a4 and a6 form heteromeric channels with 02 or 04 and a5 and 03 can associate with other a/0 pairs. Studies in knockout mice implicate several subunits in the ability of nicotine to modulate dopamine neurons (a4, a6, a7, 02, 03) but... [Pg.921]

Yates SL, Bencherif M, Fluhler EN, LippieUo PM (1995) Up-regulation of nicotinic acetylcholine receptors following chronic exposure of rats to mainstream cigarette smoke or alpha 4 beta 2 receptors to nicotine, Biochem Pharmacol 50 2001-2008 Yeomans J, Baptista M (1997) Both nicotinic and muscarinic receptors in ventral tegmental area contribute to brain-stimulation, Pharmacol Biochem Behav 57 915-921 Yoshida M, Yokoo H, Tanaka T, Mizoguchi K, Emoto H, Ishii H, Tanaka M (1993) Facilitatory modulation of mesolimbic dopamine neuronal-activity by a mu-opioid agonist and nicotine as examined with in-vivo microdialysis. Brain Res 624 277-280... [Pg.170]

Gentry CL, Lukas RJ (2002) Regulation of nicotinic acetylcholine receptor numbers and function by chronic nicotine exposure. Curr Drug Targets CNS Neurol Disord 1 359-385 Gerzanich V, Wang F, Kuryatov A, Lindstrom J (1998) Alpha 5 subunit alters desensitization, pharmacology, Ca++ permeability and Ca++ modulation of human neuronal alpha 3 nicotinic receptors. J Pharmacol Exp Ther 286 311-320... [Pg.199]

Jones IW, Wonnacott S (2004) Precise localization of alpha nicotinic acetylcholine receptors on glutamatergic axon terminals in the rat ventral tegmental area. J Neurosci 24 11244-11252 Kaiser S, Wonnacott S (2000) Alpha-bungarotoxin-sensitive nicotinic receptors indirectly modulate [ H]dopamine release in rat striatal slices via glutamate release. Mol Pharmacol 58 ... [Pg.200]

Vallejo YE, Buisson B, Bertrand D, Green WN (2005) Chronic nicotine exposure upregulates nicotinic receptors by a novel mechanism. J Neurosci 25 5563-5572 Vemino S, Amador M, Luetje CW, Patrick J, Dani JA (1992) Calcium modulation and high calcium permeability of neuronal nicotinic acetylcholine receptors. Neuron 8 127-134 Vizi ES, Lendvai B (1999) Modulatory role of presynaptic nicotinic receptors in synaptic and non-synaptic chemical communication in the central nervous system. Brain Res Brain Res Rev 30 219-235... [Pg.206]

Balfour DJ (2002) Neuroplasticity within the mesoaccumbens dopamine system and its role in tobacco Dependence, Curr Drug Targets CNS Neurol Disord 1 413-21 Balfour DJ (2004) The neurobiology of tobacco dependence a preclinical perspective on the role of the dopamine projections to the nucleus accumbens. Nicotine Tob Res 6 899-912 Barik J, Wonnacott S (2006) Indirect modulation by alpha7 nicotinic acetylcholine receptors of noradrenaline release in rat hippocampal slices interaction with glutamate and GABA systems and effect of nicotine withdrawal. Mol Pharmacol 69 618-628... [Pg.427]

Bannon, A. W., Decker, M. W., Holladay, M. W., Curzon, P., Donnelly-Roberts, D. L., Puttfarcken, P. S., Bitner, R. S., Diaz, A., Dickenson, A. H., Porsolt, R. D., Williams, M., Arneric, S. P. Broad-spectrum, non-opioid analgesic activity by selective modulation of neuronal nicotinic acetylcholine receptors, Science 1998, 279, 77-81. [Pg.442]

Alkondon M, Rocha ES, Maelicke A, Albuquerque EX (1996) Diversity of nicotinic acetylcholine receptors in rat brain. V. alpha-Bungarotoxin-sensitive nicotinic receptors in olfactory bulb neurons and presynaptic modulation of glutamate release. J Pharmacol Exp Ther 278 1460-71... [Pg.514]

Azam L, McIntosh JM (2006) Characterization of nicotinic acetylcholine receptors that modulate nicotine-evoked [3H]norepinephrine release from mouse hippocampal synaptosomes. Mol Pharmacol 70 967-76... [Pg.515]

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