Agonist- and antagonist-induced up-regulation of surface 5-HT3A receptors

British Journal of Pharmacology

Volumn 172, Issue 16, 2015, Pages 4066-4077

  Morton, Russell A ^a,b   Baptista Hon, Daniel T ^c   Hales, Tim G ^b,c   Lovinger, David M ^a,b  

^a NATIONAL INSTITUTE ON ALCOHOL ABUSE AND ALCOHOLISM   (United States)

^b GEORGE WASHINGTON UNIVERSITY SCHOOL OF MEDICINE AND HEALTH SCIENCES   (United States)

^c UNIVERSITY OF DUNDEE   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

BEMESETRON; BETA BUNGAROTOXIN; BUNGAROTOXIN RECEPTOR; CITALOPRAM; CYCLOHEXIMIDE; SEROTONIN 3 AGONIST; SEROTONIN 3 ANTAGONIST; SEROTONIN 3A RECEPTOR; 1-(3-CHLOROPHENYL)BIGUANIDE; BIGUANIDE DERIVATIVE; MORPHINE; SEROTONIN; SEROTONIN 3 RECEPTOR; SEROTONIN AGONIST; SEROTONIN ANTAGONIST; TROPANE DERIVATIVE;

ARTICLE; CELL LABELING; CELL SURFACE; CELLULAR DISTRIBUTION; CONCENTRATION RESPONSE; CONTROLLED STUDY; DRUG EXPOSURE; DRUG MECHANISM; DRUG RECEPTOR BINDING; DRUG RESPONSE; DRUG TARGETING; FLUORESCENCE MICROSCOPY; HUMAN; HUMAN CELL; IMAGE ANALYSIS; INCUBATION TIME; LONG TERM EXPOSURE; NERVE CELL CULTURE; PRIORITY JOURNAL; PROTEIN DETERMINATION; PROTEIN EXPRESSION; PROTEIN LOCALIZATION; QUANTITATIVE STUDY; RECEPTOR UPREGULATION; VOLTAGE CLAMP TECHNIQUE; ANIMAL; HEK293 CELL LINE; MOUSE; PHYSIOLOGY; RAT; TUMOR CELL LINE; UPREGULATION;

ANIMALS; BIGUANIDES; CELL LINE, TUMOR; HEK293 CELLS; HUMANS; MICE; MORPHINE; RATS; RECEPTORS, SEROTONIN, 5-HT3; SEROTONIN; SEROTONIN ANTAGONISTS; SEROTONIN RECEPTOR AGONISTS; TROPANES; UP-REGULATION;

EID: 84937522533     PISSN: 00071188     EISSN: 14765381     Source Type: Journal    
DOI: 10.1111/bph.13197     Document Type: Article

References (44)

1. Alexander SPH, Benson HE, Faccenda E, Pawson AJ, Sharman JL, Catterall WA, et al., CGTP Collaborators. (2013). The Concise Guide to PHARMACOLOGY 2013/14: Ion Channels. Br J Pharmacol 170: 1607-1651.
2. Baptista-Hon DT, Deeb TZ, Othman NA, Sharp D, Hales TG, (2012). The 5-HT3B subunit affects high-potency inhibition of 5-HT3 receptors by morphine. Br J Pharmacol 165: 693-704.
3. Barnes NM, Hales TG, Lummis SC, Peters JA, (2009). The 5-HT3 receptor-the relationship between structure and function. Neuropharmacology 56: 273-284.
4. Bencherif M, Fowler K, Lukas RJ, Lippiello PM, (1995). Mechanisms of up-regulation of neuronal nicotinic acetylcholine receptors in clonal cell lines and primary cultures of fetal rat brain. J Pharmacol Exp Ther 275: 987-994.
5. 3H]nicotine binding sites in human brain. J Neurochem 50: 1243-1247.
6. Bhatnagar S, Nowak N, Babich L, Bok L, (2004). Deletion of the 5-HT3 receptor differentially affects behavior of males and females in the Porsolt forced swim and defensive withdrawal tests. Behav Brain Res 153: 527-535.
7. Chu LF, Liang DY, Li X, Sahbaie P, D'Arcy N, Liao G, et al. (2009). From mouse to man: the 5-HT3 receptor modulates physical dependence on opioid narcotics. Pharmacogenet Genomics 19: 193-205.
8. Costall B, Naylor RJ, (2004). 5-HT3 receptors. Curr Drug Targets CNS Neurol Disord 3: 27-37.
9. Das P, Bell-Horner CL, Machu TK, Dillon GH, (2003). The GABA(A) receptor antagonist picrotoxin inhibits 5-hydroxytryptamine type 3A receptors. Neuropharmacology 44: 431-438.
10. Davies PA, Pistis M, Hanna MC, Peters JA, Lambert JJ, Hales TG, et al. (1999). The 5-HT3B subunit is a major determinant of serotonin-receptor function. Nature 397: 359-363.
11. Eshaq RS, Stahl LD, Stone R 2nd, Smith SS, Robinson LC, Leidenheimer NJ, (2010). GABA acts as a ligand chaperone in the early secretory pathway to promote cell surface expression of GABAA receptors. Brain Res 1346: 1-13.
12. Fan P, (1995). Nonopioid mechanism of morphine modulation of the activation of 5-hydroxytryptamine type 3 receptors. Mol Pharmacol 47: 491-495.
13. Ferguson SS, (2001). Evolving concepts in G protein-coupled receptor endocytosis: the role in receptor desensitization and signaling. Pharmacol Rev 53: 1-24.
14. Filtz TM, Guan W, Artymyshyn RP, Facheco M, Ford C, Molinoff PB, (1994). Mechanisms of up-regulation of D2L dopamine receptors by agonists and antagonists in transfected HEK-293 cells. J Pharmacol Exp Ther 271: 1574-1582.
15. Glatzle J, Sternini C, Robin C, Zittel TT, Wong H, Reeve JR Jr, et al. (2002). Expression of 5-HT3 receptors in the rat gastrointestinal tract. Gastroenterology 123: 217-226.
16. Govind AP, Vezina P, Green WN, (2009). Nicotine-induced upregulation of nicotinic receptors: underlying mechanisms and relevance to nicotine addiction. Biochem Pharmacol 78: 756-765.
17. Hassaine G, Deluz C, Grasso L, Wyss R, Tol MB, Hovius R, et al. (2014). X-ray structure of the mouse serotonin 5-HT3 receptor. Nature 512: 276-281.
18. van Hooft JA, Vijverberg HP, (2000). 5-HT(3) receptors and neurotransmitter release in the CNS: a nerve ending story? Trends Neurosci 23: 605-610.
19. Karnovsky AM, Gotow LF, McKinley DD, Piechan JL, Ruble CL, Mills CJ, et al. (2003). A cluster of novel serotonin receptor 3-like genes on human chromosome 3. Gene 319: 137-148.
20. Kilpatrick GJ, Jones BJ, Tyers MB, (1987). Identification and distribution of 5-HT3 receptors in rat brain using radioligand binding. Nature 330: 746-748.
21. Kuryatov A, Luo J, Cooper J, Lindstrom J, (2005). Nicotine acts as a pharmacological chaperone to up-regulate human alpha4beta2 acetylcholine receptors. Mol Pharmacol 68: 1839-1851.
22. Lester HA, Xiao C, Srinivasan R, Son CD, Miwa J, Pantoja R, et al. (2009). Nicotine is a selective pharmacological chaperone of acetylcholine receptor number and stoichiometry. Implications for drug discovery. AAPS J 11: 167-177.
23. Li TK, Spanagel R, Colombo G, McBride WJ, Porrino LJ, Suzuki T, et al. (2001). Alcohol reinforcement and voluntary ethanol consumption. Alcohol Clin Exp Res 25: 117S-126S.
24. Liang DY, Li X, Clark JD, (2011). 5-Hydroxytryptamine type 3 receptor modulates opioid-induced hyperalgesia and tolerance in mice. Anesthesiology 114: 1180-1189.
25. Machu TK, (2011). Therapeutics of 5-HT3 receptor antagonists: current uses and future directions. Pharmacol Ther 130: 338-347.
26. Maricq AV, Peterson AS, Brake AJ, Myers RM, Julius D, (1991). Primary structure and functional expression of the 5HT3 receptor, a serotonin-gated ion channel. Science 254: 432-437.
27. Millan MJ, Veiga S, Girardon S, Brocco M, (2003). Blockade of serotonin 5-HT1B and 5-HT2A receptors suppresses the induction of locomotor activity by 5-HT reuptake inhibitors, citalopram and fluvoxamine, in NMRI mice exposed to a novel environment: a comparison to other 5-HT receptor subtypes. Psychopharmacology (Berl) 168: 397-409.
28. Morales M, Wang SD, (2002). Differential composition of 5-hydroxytryptamine3 receptors synthesized in the rat CNS and peripheral nervous system. J Neurosci 22: 6732-6741.
29. Morton RA, Luo G, Davis MI, Hales TG, Lovinger DM, (2011). Fluorophore assisted light inactivation (FALI) of recombinant 5-HT(3)A receptor constitutive internalization and function. Mol Cell Neurosci 47: 79-92.
30. Mothersill C, Saroya R, Smith RW, Singh H, Seymour CB, (2010). Serum serotonin levels determine the magnitude and type of bystander effects in medium transfer experiments. Radiat Res 174: 119-123.
31. Moykkynen T, Korpi ER, Lovinger DM, (2003). Ethanol inhibits alpha-amino-3-hydyroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor function in central nervous system neurons by stabilizing desensitization. J Pharmacol Exp Ther 306: 546-555.
32. Niesler B, Frank B, Kapeller J, Rappold GA, (2003). Cloning, physical mapping and expression analysis of the human 5-HT3 serotonin receptor-like genes HTR3C, HTR3D and HTR3E. Gene 310: 101-111.
33. Pawson AJ, Sharman JL, Benson HE, Faccenda E, Alexander SP, Buneman OP, et al.; NC-IUPHAR. (2014). The IUPHAR/BPS Guide to PHARMACOLOGY: an expert-driven knowledge base of drug targets and their ligands. Nucl Acids Res 42 (Database Issue): D1098-D1106.
34. Peng X, Gerzanich V, Anand R, Whiting PJ, Lindstrom J, (1994). Nicotine-induced increase in neuronal nicotinic receptors results from a decrease in the rate of receptor turnover. Mol Pharmacol 46: 523-530.
35. Perry DC, Davila-Garcia MI, Stockmeier CA, Kellar KJ, (1999). Increased nicotinic receptors in brains from smokers: membrane binding and autoradiography studies. J Pharmacol Exp Ther 289: 1545-1552.
36. Raybould HE, Glatzle J, Robin C, Meyer JH, Phan T, Wong H, et al. (2003). Expression of 5-HT3 receptors by extrinsic duodenal afferents contribute to intestinal inhibition of gastric emptying. Am J Physiol Gastrointest Liver Physiol 284: G367-G372.
37. Sanghvi M, Hamouda AK, Davis MI, Morton RA, Srivastava S, Pandhare A, et al. (2009). Hydrophobic photolabeling studies identify the lipid-protein interface of the 5-HT3A receptor. Biochemistry 48: 9278-9286.
38. Schreiter C, Hovius R, Costioli M, Pick H, Kellenberger S, Schild L, et al. (2003). Characterization of the ligand-binding site of the serotonin 5-HT3 receptor: the role of glutamate residues 97, 224, and 235. J Biol Chem 278: 22709-22716.
39. 3H]acetylcholine recognition sites in brain by nicotinic cholinergic drugs. J Neurochem 45: 427-433.
40. Shahsavar A, Kastrup JS, Nielsen EO, Kristensen JL, Gajhede M, Balle T, (2012). Crystal structure of Lymnaea stagnalis AChBP complexed with the potent nAChR antagonist DHbetaE suggests a unique mode of antagonism. PLoS ONE 7: e40757.
41. Vallejo YF, Buisson B, Bertrand D, Green WN, (2005). Chronic nicotine exposure upregulates nicotinic receptors by a novel mechanism. J Neurosci 25: 5563-5572.
42. Wang F, Nelson ME, Kuryatov A, Olale F, Cooper J, Keyser K, et al. (1998). Chronic nicotine treatment up-regulates human alpha3 beta2 but not alpha3 beta4 acetylcholine receptors stably transfected in human embryonic kidney cells. J Biol Chem 273: 28721-28732.
43. Wang Q, Lynch JW, (2011). Activation and desensitization induce distinct conformational changes at the extracellular-transmembrane domain interface of the glycine receptor. J Biol Chem 286: 38814-38824.
44. Wonnacott S, (1990). The paradox of nicotinic acetylcholine receptor upregulation by nicotine. Trends Pharmacol Sci 11: 216-219.