In vivo pharmacological characterization of (± )-4-[2-(1-methyl-2-pyrrolidinyl)ethyl]thiophenol hydrochloride (SIB-1553A), a novel cholinergic ligand: Microdialysis studies

Brain Research

Volumn 986, Issue 1-2, 2003, Pages 71-81

  Rao, Tadimeti S ^a   Reid, Richard T ^b   Correa, Lucia D ^a   Santori, Emily M ^a   Gardner, Michael F ^a   Sacaan, Aida I ^c   Lorrain, Daniel ^a   Vernier, Jean Michel ^a  

^a MERCK RESEARCH LABORATORIES   (United States)

^b Arizeke Pharmaceuticals Inc   (United States)

^c Banck Clinical Research Center   (United States)

Author keywords

Hippocampal ACh release; Microdialysis; nAChR agonist; SIB 1553A

Indexed keywords

4 [[2 (1 METHYL 2 PYRROLIDINYL)ETHYL]THIO]PHENOL; 8 CHLORO 2,3,4,5 TETRAHYDRO 3 METHYL 5 PHENYL 1H 3 BENZAZEPIN 7 OL HYDROGEN MALEATE; ACETYLCHOLINE; CHOLINERGIC RECEPTOR; CHOLINERGIC RECEPTOR BLOCKING AGENT; CHOLINERGIC RECEPTOR STIMULATING AGENT; DIHYDRO BETA ERYTHROIDINE; DOPAMINE; DOPAMINE RECEPTOR BLOCKING AGENT; MECAMYLAMINE; NICOTINE;

ACETYLCHOLINE RELEASE; ANIMAL BEHAVIOR; ANIMAL EXPERIMENT; ARTICLE; BODY MOVEMENT; CONTROLLED STUDY; DOPAMINE RELEASE; DOSE RESPONSE; DRUG BRAIN LEVEL; DRUG EFFECT; DRUG ELIMINATION; DRUG HALF LIFE; DRUG PENETRATION; HIPPOCAMPUS; IN VIVO STUDY; INJECTION; MALE; MICRODIALYSIS; NONHUMAN; PREFRONTAL CORTEX; PRIORITY JOURNAL; RAT; STATISTICAL SIGNIFICANCE; SYNAPSE;

EID: 0142122140     PISSN: 00068993     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0006-8993(03)03174-3     Document Type: Article

References (35)

1. Bartus R.T., Dean R.L., Beer B., Lippa A.S. The cholinergic hypothesis of geriatric memory dysfunction. Science. 217:1982;408-417.
2. Bierer L.M., Hartounian V., Gabriel S., Knott P.J., Carlin L.S., Purohit D.P., Perl D.P., Schneider J., Kanof P., Davis K.L. Neurochemical correlates of dementia severity in Alzheimer's disease: relative importance of cholinergic deficits. J. Neurochem. 64:1995;749-760.
3. Bontempi B., Whelan K.T., Risbrough V.B., Lloyd G.K., Menzaghi F. Cognitive enhancing properties and tolerability of cholinergic agents in mice: a comparative study of nicotine, donepezil and SIB-1553A, a sub-type selective ligand for nicotinic acetylcholine receptors. Neuropsychopharmacology. 28:2003;1235-1246.
4. Bontempi B., Whelan K.T., Risbrough V.B., Rao T.S., Buccafusco J.J., Lloyd G.K., Menzaghi F. SIB-1553A, ((± )-4-[2-(1-methyl-2-pyrrolidinyl)ethyl]thiophenol hydrochloride, a subtype selective ligand for nicotinic acetylcholine receptors with putative cognitive-enhancing properties: effects on working and reference memory performances in aged rodents and non-human primates. J. Pharmacol. Exp. Ther. 299:2001;297-306.
5. Everitt B.J., Robbins T.W. Central cholinergic mechanisms and cognition. Ann. Rev. Psychol. 48:1997;649-684.
6. Farlow M. A clinical overview of cholinesterase inhibitors in Alzheimer's disease. Int. Psychogeriatr. 14:(Suppl. 1):2002;93-126.
7. Gerzanich V., Peng X., Wang F., Wells G., Anand R., Fletcher S., Lindstrom J. Comparative pharmacology of epibatidine: a potent agonist for neuronal nicotinic acetylcholine receptors. Mol. Pharmacol. 48:1995;774-782.
8. Graham A.J., Martin-Ruiz C.M., Teakton T., Ray M.A., Court J.A. Human brain nicotinic receptors, their distribution and participation in neuropsychiatric disorders. Curr. Drug targets CNS Neurological Disorders. 1:2002;387-397.
9. Gray R., Rajan A.S., Radcliff K.A., Yakehiro M., Dani J.A. Hippocampal synaptic transmission enhanced by low concentrations of nicotine. Nature (London). 383:1996;713-716.
10. Grottick A.J., Wyler R., Higgins G.A. A study of the nicotinic agonist SIB-1553A on locomotion, and attention as measured by five-choice serial reaction task. Pharmacol. Biochem. Behav. 70:2001;505-513.
11. Levin E.D. Nicotinic acetylcholine involvement in cognitive function in animals. Psychopharmacology. 138:1998;217-230.
12. McGhee D.S., Heath M.J.S., Gelber S., DeVay P., Role L. Nicotine enhancement of fast excitatory synaptic transmission in CNS by presynaptic receptorsm. Science. 269:1995;1692-1696.
13. Menzaghi F.M., McClure D.E., Lloyd G.K. Subtype-selective nAChR agonists for the treatment of neurological disorders: SIB-1508Y and SIB-1553A. Arneric S.P., Brioni J. Neuronal Nicotinic Receptors. 1999;379-394 Wiley-Liss, New York, NY.
14. Nakai K., Fujii T., Funimoto J., Suzuki T., Kawashima K. Effect of WAY-100135 on the hippocampal acetylcholine release potentiated by 8-OHDPAT, a serotonin 1A receptor agonist, in normal and p-chlorophenylalanine treated rats as measured by in vivo microdialysis. Neurosci. Res. 31:1998;23-29.
15. Newhouse P., Sunderland T., Tariot P. Intravenous nicotine in AD. Psychopharmacology. 95:1988;171-175.
16. Newhouse P.A., Potter A., Lewin E.D. Nicotinic system involvement in Alzheimer's and Parkinson's diseases: implications for therapeutics. Drugs Aging. 11:1997;206-228.
17. Nordberg A., Lijla A., Lindquist H., Hartvig P., Amberla K., Vittanen M., Warpman M., Warpman U., Johansson U., Hellstrom-Lindahl E., Bjurling P. Tacrine restores cholinergic nicotinic receptors and glucose metabolism in Alzheimer's patients as visualized by positron emission tomography. Neurobiol. Aging. 13:1992;747-758.
18. Paxinos G., Watson C. The Rat Brain in Stereotaxic Coordinates. 2nd Edition:1986;Academic Press, London.
19. Picciotto M.R., Zoli M. Nicotinic receptors in aging and dementia. J. Neurobiol. 53:2002;641-655.
20. Quirion R., Richard J., Wilson A. Muscarinic and nicotinic modulation of cortical acetylcholine monitored by in vivo microdialysis in freely moving adult rats. Synapse. 17:1994;92-100.
21. Rao T.S., Adams P.B., Correa L.D., Santori E.M., Saccan A.I., Reid R.T., Suto C.M., Venier J.-M. In vitro pharmacological characterization of (±)-4-[2-(1-methyl-2-pyrrolidinyl)ethyl]thiophenol hydrochloride (SIB-1553A), a nicotinic acetylcholine receptor ligand. Brain Res. 981:2003;85-90.
22. Reid R.T., Lloyd G.K., Rao T.S. Pharmacological characterization of nicotine-induced acetylcholine release in the rat hippocampus in vivo: evidence for a permissive dopamine synapse. Br. J. Pharmacol. 127:1999;1486-1494.
23. Sacaan A.I., Reid R.T., Santori E.M., Adams P.A., Correa L.D., Mahaffy L.S., Bleicher L., Cosford N.D.P., McDonald I.A., Rao T.S., Lloyd G.K. Pharmacological characterization of SIB-1765F: a novel cholinergic ion channel agonist. J. Pharmacol. Exp. Ther. 280:1997;373-383.
24. J.S. Schneider, J.P. Tinker, F. Menzaghi, G.K. Lloyd, The subtype selective nicotinic acetylcholine receptor agonist SIB-1553A improves both attention and memory components of a spatial working memory task in chronic low dose MPTP-treated monkeys, J. Pharmacol. Exp. Ther. Apr 29, (2003, epub).
25. D. H Small, L. R Fodero, Cholinergic regulation of synaptic plasticity as a therapeutic target in Alzheimer's disease. J. Alzheimers Dis. 4:(5):2002;349-355.
26. Summers K.L., Lippiello P., Giacobini E. A microdialysis study of the effects of the nicotinic agonist RJR-2403 on cortical release of acetylcholine and biogenic amines. Neurochem. Res. 21:1996;1181-1186.
27. Summers K.L., Kem W.R., Giacobini E. Nicotinic agonist modulation of neurotransmitter levels in the rat prefrontal cortex. Jpn. J. Pharmacol. 74:1997;139-146.
28. Tani Y., Saito K., Imoto M., Ohno T. Pharmacological characterization of nicotinic receptor mediated acetylcholine release in the rat brain: an in vivo microdialysis study. Eur. J. Pharmacol. 351:1998;181-188.
29. Terry Jr A.V., Risbrough V.B., Buccafusco J.J., Menzaghi F. Effects of ((±)-4-[2-(1-methyl-2-pyrrolidinyl)ethyl]thiophenol hydrochloride (SIB-1553A), a selective ligand for nicotinic acetylcholine receptors, in tests of visual attention and distractibility in rats and monkeys. J. Pharmacol. Exp. Ther. 301:2002;284-292.
30. Terry A.V., Clarke M.S.F. Nicotine stimulation of nerve growth factor receptor expression. Life Sci. 55:1994;PL91-PL98.
31. Testylier G., Dykes R.W. Acetylcholine release from frontal cortex in the waking rat measured by microdialysis without acetylcholinesterase inhibitors: effects of diisopropylfluorophosphate. Brain Res. 740:1996;307-315.
32. Vernier J.-M., Abdellaoui H., Holsenback H., Cosford N.D.P., Bleicher L., Barker G., Bontempi B., Chavez Noriega L.E., Mengazhi F.M., Rao T.S., Reid R.T., Sacaan A.I., Suto C., Washburn M., Lloyd G.K., McDonald I.A. 4[2-(Methyl-2-pyrrolidnyl)ethyl]thiophenol hydrochloride (SIB-1553A): a novel cognitive enhancer with selectivity for neuronal nicotinic acetylcholine receptors. Bioorg. J. Med. Chem. 42:1999;1684-1686.
33. Vizi S., Kiss J. Neurochemistry and pharmacology of the major hippocampal transmitter systems: synaptic and non-synaptic interactions. Hippocampus. 8:1998;566-607.
34. Wonnacott S. Presynaptic nicotinic ACh receptors. Trends Neurosci. 20:1997;92-98.
35. Zoli M., Lena C., Picciotto M.R., Changeux J.-P. Identification of four classes of brain nicotinic receptors using β2 mutant mice. J. Neurosci. 18:1998;4461-4472.