N-terminal domains in mouse and human 5-hydroxytryptamine3A receptors confer partial agonist and antagonist properties to benzylidene analogs of anabaseine

Journal of Pharmacology and Experimental Therapeutics

Volumn 317, Issue 3, 2006, Pages 1276-1284

  Zhang, Ran ^a   White, Natalie A ^a   Soti, Ferenc S ^b   Kem, William R ^b   Machu, Tina K ^a,c  

^a TEXAS TECH UNIVERSITY   (United States)

^b UNIVERSITY OF FLORIDA   (United States)

^c UNIVERSITY OF NORTH TEXAS   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

3 (2 HYDROXY, 4 METHOXYBENZYLIDENE) ANABASEINE; 3 (2 METHOXY, 4 HYDROXYBENZYLIDENE) ANABASEINE; 3 (2,4 DIHYDROXYBENZYLIDENE) ANABASEINE; 3 (2,4 DIMETHOXYBENZYLIDENE) ANABASEINE; BENZYLIDENE DERIVATIVE; SEROTONIN 3 RECEPTOR; SEROTONIN AGONIST; UNCLASSIFIED DRUG;

AMINO TERMINAL SEQUENCE; ANIMAL EXPERIMENT; ARTICLE; CHIMERA; DRUG INHIBITION; DRUG MECHANISM; DRUG POTENCY; DRUG STRUCTURE; HUMAN; MOUSE; NONHUMAN; PRIORITY JOURNAL;

ANABASINE; ANIMALS; BENZYLIDENE COMPOUNDS; CLONING, MOLECULAR; HUMANS; MICE; MOLECULAR STRUCTURE; OOCYTES; PATCH-CLAMP TECHNIQUES; PROTEIN STRUCTURE, TERTIARY; RECEPTORS, SEROTONIN; SEROTONIN AGONISTS; SEROTONIN ANTAGONISTS; XENOPUS LAEVIS;

EID: 33646757888     PISSN: 00223565     EISSN: 15210103     Source Type: Journal    
DOI: 10.1124/jpet.106.101485     Document Type: Article

References (36)

1. Arendash GW, Sengstock GJ, Sanberg PR, and Kem WR (1995) Improved learning and memory in aged rats with chronic administration of the nicotinic receptor agonist GTS-21. Brain Res 674:252-259.
2. 3A receptors: possible involvement of an allosteric modulatory site. Br J Pharmacol 137:589-596.
3. 3A) and nicotinic acetylcholine receptors: the anomalous binding properties of nicotine. Biochem 41:10262-10269.
4. 3 receptor revealed by unnatural amino acid mutagenesis. J Neurosci 24:9097-9104.
5. Bouzat C, Gumllar F, Spitzmaul G, Wang H-L, Rayes D, Hansen SB, Taylor P, and Sine SM (2004) Coupling of agonist binding to channel gating in an ACh-binding protein linked to an ion channel. Nature (Lond) 430:896-900.
6. Brejc K, van Dijk WJ, Klaassen RV, Schuurmans M, van Der Oost J, Smit AB, and Sixma TK (2001) Crystal structure of an ACh-binding protein reveals the ligand-binding domain of nicotinic receptors. Nature (Lond) 411:269-276.
7. 3B subunit is a major determinant of serotonin-receptor function. Nature (Lond) 397:359-363.
8. 3 receptors. J Neurosci 18:6528-6538.
9. 125I-α-bungarotoxin receptor subtypes. Mol Pharmacol 47:164-171.
10. 3B receptor subunit. J Biol Chem 274:30799-30810.
11. Eisele JL, Bertrand S, Galzi JL, Deillers-Thiery A, Changeux J-P, and Bertrand D (1993) Chimeric nicotinic-serotonergic receptor combines distinct ligand binding and channel specificities. Nature (Lond) 336:479-483.
12. 3 receptor. Biophys J 84:1720-1733.
13. 3A receptor subunits. Mol Pharmacol 55:1037-1043.
14. Karnovsky AM, Gotow LF, McKinley DD, Piechan JL, Ruble CL, Mills CJ, Schellin KAB, Slightom JL, Fitzgerald LR, Benjamin CW, et al. (2003) A cluster of novel serotonin receptor 3-like genes on human chromosome 3. Gene (Amst) 319:137-148.
15. Kem WR, Mahnir VM, Prokai L, Papke RL, Cao X, LeFrancois S, Wildeboer K, Prokai-Tatrai K, Porter-Papke J, and Soti F (2004) Hydroxy metabolites of the Alzheimer's drug candidate 3-[(2,4-dimethoxy)benzylidene]-anabaseine dihydrochloride (GTS-21): their molecular properties, interactions with brain nicotinic receptors, and brain penetration. Mol Pharmacol 65:56-67.
16. Kem WR, Mahnir VM, Papke RL, and Lingle CJ (1997) Anabaseine is a potent agonist upon muscle and neuronal alpha-bugarotoxin-sensitive nicotinic receptors. J Pharmacol Exp Ther 283:979-992.
17. Lankiewicz S, Lobbitz S, Lobitz N, Wetzel CHR, Rupprecht R, Gisselmann G, and Hatt H (1998) Molecular cloning, functional expression, and pharmacological characterization of 5-hydroxytryptamine3 receptor cDNA and its splice variants from guinea pig. Mol Pharmacol 53:202-212.
18. Lummis SCR, Beene DL, Lee LW, Lester HA, Broadhurst RW, and Dougherty DA (2005) Cis-trans isomerization at a proline opens the pore of a neurotransmitter-gated ion channel. Nature (Lond) 438:248-252.
19. 3A receptor. J Pharmacol Exp Ther 299:1112-1117.
20. Mahnir VM, Lin B, Prokai-Tatrai K, and Kem WR (1998) Pharmacokinetics and urinary excretion of DMXBA (GTS-21), a compound enhancing cognition. Biopharm Drug Dis 19:147-151.
21. 3A receptor models. J Recept Signal Transduct Res 23:255-270.
22. 3 receptor, a serotonin-gated ion channel. Science (Wash DC) 254:432-437.
23. Meyer EM, Kuryatov A, Gerzanich V, Lindstrom J, and Papke RL (1998a) Analysis of 3-(4-hydroxy, 2-methoxybenzylidene)-anabaseine selectivity and activity at human and rat alpha-7 nicotinic receptors. J Pharmacol Exp Ther 287:918-925.
24. Meyer EM, Tay ET, Zoltewicz JA, Meyers C, King MA, Papke RL, and DeFiebre CM (1998b) Neuroprotective and memory-related actions of novel alpha-7 nicotinic agents with different mixed agonist/antagonist properties. J Pharmacol Exp Ther 284:1026-1032.
25. 3 receptors. Eur J Pharmacol 369:125-132.
26. 3 receptors synthesized in the rat CNS and peripheral nervous system. J Neurosci 22:6732-6741.
27. Niesler B, Frank B, Kapeller J, and Rappold GA (2003) Cloning, physical mapping and expression analysis of the human 5-HT3 serotonin receptor-like genes HTR3C, HTR3D and HTR3E. Gene (Amst) 319:137-148.
28. Papke RL, McCormack TJ, Jack BA, Wang D, Bugaj-Gaweda B, Schiff HC, Buhr JD, Waber AJ, and Stokes C (2005) Rhesus monkey α7 nicotinic acetylcholine receptors: comparisons to human α7 receptors expressed in Xenopus oocytes. Eur J Pharmacol 524:11-18.
29. 3 receptors. J Neurosci 25:9358-9366.
30. Reeves DC, Sayed MFR, Chau P-L, Price KL, Lummis SCR (2003) Prediction of 5-HT3 receptor agnoist-binding residues using homology modeling. Biophys J 84:2338-2344.
31. 3 receptor. J Biol Chem 278:22709-22715.
32. Sine SM (2002) The nicotinic receptor ligand binding domain. J Neurobiol 53:431-446.
33. Stokes C, Papke JKP, Horenstein NA, Kem WR, McCormack TJ, and Papke RL (2004) The structural basis for GTS-21 selectivity between human and rat nicotinic α7 receptors. Mol Pharmacol 66:14-24.
34. 3A receptor contributes to the differential actions of 5-hydroxytryptamine and m-chlorophenylbiguanide. Biochem 44:9140-9149.
35. 3 receptor binding site using modeling and radioligand binding. J Biol Chem 280:20476-20482.
36. 3 receptors facilitates GABA release in the hippocampus: in vitro slice and synaptosome studies. Neurosci 129:703-718.