Receptor binding thermodynamics at the neuronal nicotinic receptor

Current Topics in Medicinal Chemistry

Volumn 4, Issue 3, 2004, Pages 361-368

  Borea, Pier Andrea ^a   Varani, Katia ^a   Gessi, Stefania ^a   Merighi, Stefania ^a   Dal Piaz, Alessandro ^a   Gilli, Paola ^a   Gilli, Gastone ^a  

^a UNIVERSITY OF FERRARA   (Italy)

Author keywords

[No Author keywords available]

Indexed keywords

ADENOSINE A1 RECEPTOR; ADENOSINE A2A RECEPTOR; ADENOSINE A3 RECEPTOR; ARECOLINE; CARBACHOL; CYTISINE; DIHYDRO BETA ERYTHROIDINE; EPIBATIDINE; G PROTEIN COUPLED RECEPTOR; HEXAMETHONIUM; ION CHANNEL; METHYLCARBACHOL; NICOTINE; NICOTINIC AGENT; NICOTINIC RECEPTOR; SUXAMETHONIUM; TETRYLAMMONIUM; TUBOCURARINE CHLORIDE;

BINDING AFFINITY; CHANNEL GATING; DRUG RECEPTOR BINDING; ENTHALPY; ENTROPY; REVIEW; SIGNAL TRANSDUCTION; THERMODYNAMICS; ANIMAL; HUMAN; METABOLISM; NERVE CELL; PROTEIN BINDING;

ANIMALS; HUMANS; NEURONS; PROTEIN BINDING; RECEPTORS, NICOTINIC; THERMODYNAMICS;

EID: 1642286938     PISSN: 15680266     EISSN: None     Source Type: Journal    
DOI: 10.2174/1568026043451410     Document Type: Review

References (40)

1. Bylund, D.B.; Yamamura, H.I. in: Yamamura H.I., Enna S.J., Kuhar (Eds.). Methods in neurotransmitter receptor analysis, Raven Press, New York, 1990, 1-36.
2. Gilli, G.; Borea, P.A. in Jeffrey, G.A.; Pinella, J.F. (Eds.). The application of charge- density research to chemistry and drug-design, Plenum, New York, 1991, 241-286.
3. 1 adenosine receptors ligands. Mol. Neuropharmacol., 1992, 2, 273-281.
4. Weiland, G.A.; Minneman K.P.; Molinoff P.B. Fundamental difference between the molecular interactions of agonists and antagonists with the β-adrenergic receptor. Nature, 1979, 281, 114-117.
5. Weiland, G.A.; Minneman K.P.; Molinoff P.B. Thermodynamics of agonists and antagonists with mammalian beta adrenergic receptors. Mol. Pharmacol., 1980, 18, 341-347.
6. 2A adenosine receptors. Life Sci., 1996, 1373-1388.
7. Berea, P.A.; Dalpiaz, A.; Varani, K.; Gilli, P.; Gilli, G. Can thermodynamic measurements of receptor binding yield information on drug affinity and efficacy? Biochem Pharmacol., 2000, 11, 1549-1556.
8. 2A receptor ligands. Biochem Pharmacol., 1995, 49, 461-469.
9. 3 adenosine receptors. Biochem Pharmacol., 2002, 63, 157-161.
10. Kilpatrick, G.J.; el Tayar, N.; van der Waterbeemb, H.; Jenner, P.; Testa, E.; Marsden C.D. The thermodynamics of agonist and antagonist binding to dopamine D-2 receptors. Mol. Pharmacol., 1986, 30, 226-234.
11. Duarte, E.P.; Oliveira, C.R.; Carvalho, A.P. Thermodynamic analysis of antagonist and agonist interactions with dopamine receptors Eur. J. Pharmacol., 1988, 1, 227-239.
12. 1A receptor ligands. Eur. J. Pharmacol., 1996, 31, 107-114.
13. Mohler, H.; Richards, J.G. Agonists and Antagonists benzodiazepine receptor interaction in vitro. Nature 1981, 294, 763-765.
14. Doble, A. J. Comparative thermodynamic of benzodiazepine receptor ligand interaction in rat neuronal membranes. Neurochem. 1983, 1605-1612.
15. Gomez, A.R.; Garcia-Calvo M.; Vasquez, J.; Marvizon, G.C.; Valdivieso, T.; Mayor, F. Thermodynamics of agonist and antagonist interaction with the strychnine-sensitive glycine receptor. J. Neurochem., 1989, 52, 1775-1780.
16. A receptor binding to ionophorefunction. Neurochem. Int., 1996, 29, 361-370.
17. 3 receptors binding discriminate agonistic from antagonistic behaviour. Eur. J. Pharmacol., 1996, 29, 329-334.
18. 3H]granisetron binding. Neurochem., 1996, 67, 407-412.
19. Borea, P.A.; Varani, K.; Gessi, S.; Gilli, P.; Gilli, G. Binding thermodynamics at the human neuronal nicotine receptor. Biochem Pharmacol., 1998, 55, 1189-1197.
20. Role, L.W. Diversity in primary structure and function of neuronal nicotinic acetylcholine receptors. Curr Opin Neurobiol., 1992, 2, 254-264.
21. Sargent, P.B. The diversity of neuronal nicotinic acetylcholine receptors. Annu Rev Neurosci, 1993, 16, 403-443.
22. Elgoyhen, A.B.; Johnson, D.; Boutler, J.; Vetter, D.; Heinemann, S.F. Cloning and functional expression of alpha9: a novel acetylcholine gated ion channel. In: International Symposium on Nicotine: The effects of Nicotine on Biological Systems on Nicotine: The effects of Nicotine on Biological Systems II (Eds Clarke PBS, Quick M., Thuran K and Adlkoffer F) 7, Birkhauser Verlag, Basel, 1994.
23. Romano, C.; Goldstein, A. Stereospecific nicotine receptors on rat brain membranes. Science, 1980, 210, 647-649.
24. 3H]acetylcholine in rat brain. Mol. Pharmacol., 1982, 22, 56-62.
25. 3H] methylcarbamylcholine, a new radioligand specific for nicotinic acetylcholine receptors in brain. Eur. J. Pharmacol., 1987, 139, 323-333.
26. 3H]acetylcholine recognition sites in brain by nicotinic cholinergic drugs. J. Neurochem., 1985, 45, 427-433.
27. Marks, M.J.; Stitzel, J.A.; Collins, A.C. Time course study of the effects of chronic nicotine infusion on drug response and brain receptors. J. Pharmacol. Exp. Ther., 1985, 235, 619-629.
28. 3H] cytisine binding to nicotinic cholinergic receptors in brain. Mol. Pharmacol., 1990, 39, 9-12.
29. 3H]cytisine binding to human brain membrane preparations. Brain Res., 1993, 600, 127-133.
30. 50) of an enzymatic reaction. Biochem. Pharmacol., 1973, 22, 3099-3108.
31. Munson, P.J., Rodbard, D. Ligand: a versatile computerized approach for the characterization of ligand binding systems. Anal. Biochem., 1980, 107, 220-239.
32. Krug, R.R., Hunter, W.G., Grieger, R.A. Statistical interpretation of enthalpy-entropy compensation. Nature, 1976, 261, 566-567.
33. Waelbroeck, M., Van Obberghen, E., De Meyts, P. Thermodynamics of the interaction of insuline with its receptors. J. Biol. Chem., 1979, 254, 7736-7740.
34. Gilli, P., Ferretti, V., Gilli, G., Borea, P.A. Enthalpy-entropy compensation in drug-receptor binding. J. Phys. Chem., 1994, 98, 1515-1518.
35. Leffler, J.E., Grunwald, E. Rates and equilibria of organic reactions, 1964, Wiley, New York.
36. Tomlinson, E., Steel, C. Solvent reorganization and thermodynamic enthalpy-entropy compensation. J. Am. Chem. Soc., 1983, 13, 115-144.
37. Grunwald, E., Steel, C. Solvent reorganization and thermodynamic enthalpy-entropy compensation. J. Am. Chem. Soc., 1995, 117, 5687-5692.
38. Testa, B., Jenner, P., Kilpatrick, G.J., El Tayar, N., van de Waterbeemd H., Marsden, C.D. Do thermodynamic studies provide information on both the binding and the activation of dopaminergic and other receptors? Biochem. Pharmacol., 1987, 36, 4041-4046.
39. Miklavc, A., Kocjan, D., Mavri, J., Koller, J., Hadzi, D. On the fundamental difference in the thermodynamics of agonist and antagonist interactions with β-adrenergic receptors and the mechanism of entropy-driven binding. Biochem. Pharmacol., 1990, 40, 663-669.
40. Miklavc, A. Temperature nearly independent binding constant in several biochemical systems. The underlying entropy-driven binding mechanism and its practical significance. Biochem. Pharmacol., 1996, 51, 723-729.