Pharmacological characterization of SIB-1765F: A novel cholinergic ion channel agonist

Journal of Pharmacology and Experimental Therapeutics

Volumn 280, Issue 1, 1997, Pages 373-383

  Sacaan, Aida I ^a   Reid, Richard T ^a   Santori, Emily M ^a   Adams, Pamala ^a   Correa, Lucia D ^a   Mahaffy, Lorrence S ^a   Bleicher, Leo ^a   Cosford, Nicholas D P ^a   Stauderman, Kenneth A ^a   Mcdonald, Ian A ^a   Rao, Tadimeti S ^a   Kenneth Lloyd, G ^a  

^a MERCK RESEARCH LABORATORIES   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

3 ETHYNYL 5 (1 METHYL 2 PYRROLIDINYL)PYRIDINE FUMARATE; ACETYLCHOLINESTERASE; ALPHA BUNGAROTOXIN; AMFEBUTAMONE; CHOLINERGIC RECEPTOR BLOCKING AGENT; CHOLINERGIC RECEPTOR STIMULATING AGENT; CHOLINESTERASE; CYTISINE; DIHYDRO BETA ERYTHROIDINE; DOPAMINE; EPIBATIDINE; MECAMYLAMINE; NICOTINE; NOMIFENSINE; NORADRENALIN; QUINUCLIDINYL BENZILATE; TRITIUM; TUBOCURARINE CHLORIDE; UNCLASSIFIED DRUG;

ALZHEIMER DISEASE; ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; BRAIN SYNAPTOSOME; CHOLINERGIC SYSTEM; CYTOSOL; DEGENERATIVE DISEASE; DRUG EFFICACY; ENZYME ACTIVITY; LIGAND BINDING; MALE; MICRODIALYSIS; NEUROTRANSMITTER RELEASE; NONHUMAN; PARKINSON DISEASE; PRIORITY JOURNAL; RAT; SUBCUTANEOUS DRUG ADMINISTRATION;

ANIMALS; CALCIUM; CORPUS STRIATUM; DOPAMINE; ION CHANNELS; MALE; MICRODIALYSIS; NICOTINIC AGONISTS; NOREPINEPHRINE; OLFACTORY PATHWAYS; PYRIDINES; PYRROLIDINES; RADIOLIGAND ASSAY; RATS; RATS, SPRAGUE-DAWLEY; RECEPTORS, NICOTINIC;

EID: 8244261278     PISSN: 00223565     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article

References (64)

1. AMANO, H., GOSHIMA, Y., AKEMA, N., UEDA, H., KUBO, T. AND MISU, Y.: Effects of acute nicotine on catecholamine turnover in various rat brain regions. J. Pharmacobio-Dyn. 12: 18-23, 1989.
2. ANDERSSON, K., FUXE, K., ENEROTH, P., GUSTAFSSON, J. A. AND AGNATI, L. F.: Mecamylamine induced blockade of nicotine-induced inhibition of gonadotrophin and TSH secretion and of nicotine induced increases of catecholamine turnover in rat hypothalamus. Acta Physiol. Scand. Suppl. 479: 27-29, 1979.
3. ANDERSSON, K., FUXE, K., AGNATI, L. F. AND ENEROTH, P.: Effects of acute central and peripheral administration of nicotine on ascending dopamine pathways in the male rat brain. Evidence for nicotine induced increases of dopamine turnover in various telencephalic dopamine nerve terminal regions. Med. Biol. 59: 170-176, 1981.
4. ARCAVA, Y., DESHPANDE, S. S., SWNSON, K. L., RAPOPORT, M., WONNACOTT, S., LUNT, G. G. AND ALBUQUERQUE, E. X.: Nicotinic acetylcholine receptors in cultured neurones from hippocampus and brain stem of the rat characterized by single channel recording. FEBS Lett. 222: 63-70, 1987.
5. ARNERIC, S. P., SULLIVAN, J. P., BRIGGS, C. A., DONNELLY-ROBERTS, D., ANDERSON, D. J., RASZKIEWICZ, J. L., HUGHES, M. L., CADMAN, E. D., ADAMS, P., GARVEY, D. S., WASICAK, J. T. AND WILLIAMS, M.: (S)-3-Methyl- 5-(1-methy]-2-pyrrolidinyl) isoxazole (ABT 418): A novel cholinergic ligand with cognition-enhancing and anxiolytic activities: I. In vitro characterisation. J. Pharmacol. Exp. Ther. 270: 310-318, 1994.
6. ARNERIC, S. P., ANDERSON, D. J., BANNON, A. J., BRIGGS, C. A., BUCCAFUSCO, J. J., BRIONI, J. A., CANNON, J. A., DECKER, M. W., DONNELY-RQBERTS, D., OPALAKRISHNAN, M., HOLLADAY, M. W., KUNCL, J., MARSH, K. C., PAULY, J., RADEK, R., RODRIGUES, A. D. AND SULLIVAN, J. P.: Preclinical pharmacology of ABT-418: A prototypical cholinergic channel activator for the potential treatment of Alzheimer's disease. CNS Drug Rev. 1: 1-27, 1995.
7. ARQUEROS, L., NAQUIRA, D. AND ZUNINO, E.: Nicotine-induced release of catecholamines from rat hippocampus and striatum. Biochem. Pharmacol. 27: 2667-2674, 1978.
8. AUBERT, I., ARAUJO, D. M., CECYRE, D., ROBITAILLE, Y., GAUTHEIR, S. AND QUIRION, R.: Comparative alterations of nicotinic and muscarinic binding sites in Alzheimer's and Parkinson's diseases. J. Neurochem. 58: 529-541, 1992.
9. BADIO, B. AND DALY, J. W.: Epibatidine, a potent analgetic and nicotinic agonist. Mol. Pharmacol. 45: 563-569, 1994.
10. BALFOUR, D. J. K.: The effects of nicotine on brain neurotransmitter system. Pharmacol. Ther. 16: 269-282, 1982.
11. BENCHERIF, M. AND LUKAS, R.: Differential regulation of nicotinic acetylcholine receptor expression by human TE671/RD cells following second messenger modulation and sodium butyrate treatments. Mol. Cellular. Neurosci. 2: 52-65, 1991.
12. BENOWITZ, N.: Clinical pharmacology of nicotine, Ann. Rev. Med. 37: 21-32, 1986.
13. 50) of an enzymatic reaction. Biochem. Pharmacol. 22: 3099-3018, 1973.
14. COSFORD, N. D. P., BLEICHER, L., HERBAUT, A., MCCALLUM, S., VERNIER, J-M., DAWSON, H., WHITTEN, J. P., ADAMS, P., CHAVEZ-NORIEGA, L., CORREA, L. D., CRONA, J. H., MAHAFFY. L. S., MENZAGHI, F., RAO, T. S., REID, R. T., SACAAN, A. I., SANTORI, E. M., STAUDERMAN, K. A., WHELAN, K. D., LLOYD, G. K. AND MCDONALD, I. A.: (S)-(-)-5-Ethynyl-3-(1-methyl-2-pyrrolidinyl)pyridine maleate (SIB-1508Y): A novel antiparkinsonian agent with selectivity for neuronal nicotinic acetyicholine receptors. J. Med. Chem. 39: 3235-3237, 1996.
15. 3H]-dopamine release. Br. J. Pharmacol. 117: 595-606, 1996.
16. COOPER, E., COUTURIER, S. AND BALLIVET, M.: Pentameric structure and subnit stoichimetry of a neuronal nicotinic acetylcholine receptor. Nature 350: 235-238, 1991.
17. 125I]-α-bugarotoxin receptor subtype. Mol. Pharmacol. 47: 164-171, 1995.
18. DUVOISIN, R. M., DENERIS, E. S., PATRICK, J. AND HEINEMANN, S.: The functional diversity of the neuronal nicotinic acetylcholine receptors is increased by a novel subunit: β4. Neuron 3: 487-496, 1989.
19. EL-BIZRI, H. AND CLARKE, P. B. S.: Blockade of nicotinic receptor-mediated release of dopamine from striatal synaptosomes by chlorisondamine and other nicotinic antagonists administered in vitro. Br. J. Pharmacol. 111: 406-413, 1994.
20. ELGOYHEN, A. B., JOHNSON, D. S., BOULTER, J., VETTER, D. E. AND HEINEMANN, S.: α9: An acetylcholine receptor with novel pharmacological properties expressed in rat cochlear hair cells. Cell 79: 705-715, 1994.
21. ELLMAN, G. L., COURTNEY, K. D., ANDRES, V., JR. AND FEATHERSTONE, R. B.: A new rapid colorimetric determination of acetylcholinesterase activity. Biochem. Pharmacol. 7: 88-95, 1961.
22. FAGERSTROM, K. O., POMERLEAU, O., GIORDANI, B. AND STELSON, F.: Nicotine may relieve symptoms of Parkinson's disease. Psychopharmacology 116: 119-119, 1994.
23. FLORES, C. M., ROGERS, S. W., PABREZA, L. A., WOLFE, B. B. AND KELLER, K. J.: A subtype of nicotinic cholinergic receptor is composed of α4β2 subunits and upregulated by chronic nicotine treatment. Mol. Pharmacol. 41: 31-37, 1992.
24. 3H]-nicotine binding in human cerebral cortex: Comparison between Alzheimer's disease and the normal. J. Neurochem. 47: 1948-1954, 1986.
25. GERBANICH, V., PENG, X., WANG, F., WELLS, G., ANAND, R., FLETCHER, S. AND LINDSTROM, J.: Comparative pharmacology of epibatidine: A potent agonist for neuronal nicotinic acetylcholine receptors. Mol. Pharmacol. 48: 774-782, 1995.
26. GIORGUIEFF, M. F., FLOC'H, M. L., GLOWINSKI, J. AND BESSON, M. J.: Involvement of cholinergic presynaptic receptors of nicotinic and muscarinic types in the control of the spontaneous release of dopamine from striatal dopaminergic terminals in the rat. J. Pharmacol. Exp. Ther. 200: 535-544, 1977.
27. 3H]-dopamine release from synaptosomes prepared from mouse striatum. J. Neurochem. 59: 848-856, 1992.
28. 2+ indicators with greatly improved fluorescence properties. J. Biol. Chem. 260: 3440-3450, 1985.
29. GURNEY, A. M. AND RANG, H. P.: The channel blocking action of methonium compounds on rat submandibular ganglion cells. Br. J. Pharmacol. 82: 623-642, 1984.
30. 3H]-Epibatidine binding to nicotinic cholinergic receptors in brain. Med. Chem. Res. 4: 538-546, 1994.
31. 3H]-epibatidine binding to nicotinic cholinergic receptors in rat and human brain. Mol. Pharmacol. 48: 280-287, 1995.
32. HUNTER, B. E., DE FIEBRE, C. M., PAPKE, R. L., KEM, W. R. AND MEYER, E. M.: A novel nicotinic agonist facilitates induction of long term potentiation in the rat hippocampus. Neurosci. Letts. 168: 130-134, 1994.
33. I CHIARA, G.: Nicotine preferentially stimulates dopamine release in the limbic system of freely moving rats. Eur. J. Pharmacol. 132: 337-339, 1986.
34. 3H]-dopamine release in rat striatum. J. Neurochem. 56: 603-610, 1991.
35. KUBO, T., AMANO, H., KURAHASHI, K. AND MISU, Y.: Nicotine-induced regional changes in brain noradrenaline and dopamine turnover in rats. J. Pharmacobio-Dyn. 12: 107-112, 1989.
36. LANGE, K. W., WELLS, F. R., JENNER, P. AND MARSDEN, C. D.: Altered muscarinic and nicotinic receptor densities in cortical and subcortical brain regions in Parkinson's disease. J. Neurochem. 60: 197-203, 1993.
37. LUETJE, C. W. AND PATRICK, J.: Both α- and β-subunits contribute to the agonist sensitivity of neuronal nicotinic acetylcholine receptors. J. Neurosci. 11: 837-346, 1991.
38. MARKS, M., STITZEL, J. A., ROMM, E., WEHNER, J. M. AND COLLINS, A. C.: Nicotinic binding sites in rat and mouse brain: Comparison of acetylcholine, nicotine and α-bungarotoxin. J. Pharmacol. Exp. Ther. 30: 427-436, 1986.
39. MARSHALL, J. AND SCHNIEDEN, H.: Effect of adrenaline, noradrenaline, atropine and nicotine on some types of human tremor. Neurol. Neurosurg. Psychiatry 29: 214-218, 1966.
40. MENZAGHI, F., WHELAN, K. T., REID, R., SACAAN, A. I., RISBROUGH, V. B., RAO, T. S. AND LLOYD, G. K.: SIB-1765F: A novel nicotinic agonist with locomotor stimulant properties in rats. Soc. Neurosci. Abs. 25: 247.5, 1995.
41. MOLL, H.: The treatment of post-encephalitic parkinsonism by nicotine. Br. Med. J. 26: 1079-1081, 1926.
42. NEWHOUSE, P., SUNDERLAND, T. AND TARIOT, P.: Intravenous nicotine in AD. Psychopharmacology 95: 171-175, 1988.
43. PAXINOS, G. AND WATSON, C.: The Rat Brain in Stereotaxic Coordinates. Academic Press, New York, 1986.
44. RAO, T. S., CORREA, L. D., REID, R. T. AND LLOYD, G. K.: Evaluation of antinociceptive effects of neuronal nicotinic acetylcholine (NAChR) ligands in the rat tail-flick assay. Neuropharmacology 35: 393-405, 1996.
45. RAPIER, C., LUNT, G. G. AND WONNACOTT, S.: Stereoselective nicotine-induced release of dopamine from striatal synaptosomes concentration dependence and repetitive stimulation. J. Neurochem. 50: 1123-1130, 1988.
46. RUPNIAK, N. M. J., PATEL, S., MARWOOD, R., WEBB, J., TRAYNOR, J. R., ELLIOT, J., FREEDMAN, S. B., FLETCHER, S. R. AND HILL, R. G.: Antinociceptive and toxic effects of (+)-epibatidine oxalate attributable to nicotinic agonist activity. Br. J. Pharmacol. 113: 1487-1493, 1994.
47. SACAAN, A. I., DUNLOP, J. L. AND LLOYD, G. K.: Pharmacological characterization of neuronal acetylcholine-gated ion channel receptor-mediated hippocampal norepinephrine and striatal dopamine release from rat brain slices. J. Pharmacol. Exp. Ther. 274: 224-230, 1995.
48. SACAAN, A. I., MENZAGHI, F., DUNLOP, J. L., CORREA, L. D., WHELAN, K. T. AND LLOYD, G. K.: Epibatidine: A nicotinic acetylcholine receptor agonist releases monoaminergic neurotransmitters: In vitro and in vivo evidence in rats. J. Pharmacol. Exp. Ther. 276: 509-515, 1996.
49. SAHAKIAN, B. J. AND COULL, J. T.: Nicotine and tetrahydroaminoacridine: Evidence for improved attention in patients with dementia of the Alzheimer type. Drug Dev. Res. 31: 80-88, 1994.
50. SARGENT, P. B.: The diversity of neuronal nicotinic acetylcholine receptors. Annu. Rev. Neurosci. 16: 403-443, 1993.
51. SCHOEPFER, R., CONROY, W. G., WHITING, P., GORE, M. AND LINDSTROM, J.: Brain α-bungarotoxin binding protein cDNA and Mabs reveal subtypes of this branch of the ligand-gated ion channel gene superfamily. Neuron 5: 35-48, 1990.
52. SEGUELA, P., WADICHE, J., DINELEY-MILLER, K., DANI, J. AND PATRICK, J. W.: Molecular cloning, functional properties, and distribution of rat brain α7: A nicotinic cation channel highly permeable to calcium. J. Neurosci. 13: 596-604, 1993.
53. SHARMAN, D. F.: The turnover of catecholamines. In Central Neurotransmitter Turnover, ed by C. J. Pycock and P. V. Taberner, pp. 20-58, Croom Helm, University Park Press, London, UK, 1981.
54. STAUDERMAN, K., MAHAFFY, L. S., CHAVEZ-NORIEGA, L., JOHNSON, E. C., TRAN, C., ELLOITT, K. AND COREY-NAEVE, J.: Characterization of recombinant human neuronal nicotinic acetylcholine receptor subtypes α4β4 and α2β4 stably expressed in HEK cells. Soc. Neurosci. Abs. 25: 36.4, 1995.
55. WADA, E., WADA, K., BOULTER, J., DENERIS, E., HEINEMANN, S., PATRICK, J. AND SWANSON, L. W.: Distribution of alpha2, alpha3, alpha4, and beta2 neuronal nicotinic receptor subunit mRNAs in the central nervous system: A hybridization and histochemical study in the rat. J. Comp. Neurol. 284: 314-335, 1989.
56. WALKER, J. M., BOWEN, W. D., WALKER, F. O., MATUSMOTO, R. R., DECOSTA, B. D. AND RICE, K. C.: Sigma receptors: Biology and function. Pharmacol. Rev. 42: 355-402, 1990.
57. 3H]toiyl)guanidine: A selective ligand that binds sigma type receptors for psychotomimetic opiates and antipsychotic drugs. Proc. Natl. Acad. Sci. U.S.A. 83: 8748-8788, 1986.
58. 3H]-dopamine from rat brain slices. Neuropharmacology 13: 693-700, 1974.
59. WESTFALL, T. C., PERRY, H. AND VICKERY, L.: Mechanisms of nicotine regulation of dopamine. In Tobacco Smoking and Nicotine, pp. 209-224, Plenum Press, New York, 1987.
60. 3H]nicotinic acetylcholine binding in Alzheimer's disease and Parkinson's disease: An autoradiographic study. Neurology 38: 720-723, 1988.
61. WILLIAMS, M. AND ROBINSON, J. L.: Binding of the nicotinic cholinergic antagonist, dihydro-beta-erythroidine (DHβE) to rat brain tissue. J. Neurosci. 4: 2916-2911, 1984.
62. WONNACOTT, S., IRONS, J., RAPIER, C., THORNE, B. AND LUNT, G. G.: Presynaptic modulation of transmitter release by nicotinic receptors. In Progress in Brain Research ed by A. Nordberg, K. Fuxe, B. Holmstedt and A. Sundwall, pp. 157-163, Elsevier, Amsterdam, 1990.
63. YAMAMURA, H. I. AND SNYDER, S. H.: Muscarinic cholinergic binding in rat brain. Proc. Natl. Acad. Sci. U.S.A. 71: 1725-1729, 1974.
64. ZDONCZYK, D., ROYSE, V. AND KOLLER, W. C.: Nicotine and tremor. Clin. Neuropharmacol. 11: 282-286, 1988.