In-vivo rat striatal 5-HT4 receptor occupancy using non-radiolabelled SB207145

Journal of Pharmacy and Pharmacology

Volumn 65, Issue 5, 2013, Pages 704-712

  Nirogi, Ramakrishna ^a   Kandikere, Vishwottam ^a   Bhyrapuneni, Gopinadh ^a   Saralaya, Ramanatha ^a   Ajjala, Devender Reddy ^a   Aleti, Raghupathi Reddy ^a   Rasheed, Mohammed Abdul ^a  

^a SUVEN LIFE SCIENCES LTD   (India)

Author keywords

5 HT4 receptor occupancy; LC MS MS; rat; SB207145

Indexed keywords

1 (4 AMINO 5 CHLORO 2 METHOXYPHENYL) 3 (1 BUTYL 4 PIPERIDINYL) 1 PROPANONE; 1 METHYL 3 INDOLECARBOXYLIC ACID [1 [2 (METHYLSULFONYLAMINO)ETHYL] 4 PIPERIDINYLMETHYL] ESTER; PF 04995274; PIBOSEROD; PRUCALOPRIDE; SB 207145; SEROTONIN 4 ANTAGONIST; SEROTONIN 4 RECEPTOR; TD 8954; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; BRAIN STEM; CEREBELLUM; CONTROLLED STUDY; CORPUS STRIATUM; DOSE RESPONSE; DRUG BLOOD LEVEL; DRUG BRAIN LEVEL; DRUG DISTRIBUTION; DRUG RECEPTOR BINDING; DRUG UPTAKE; FRONTAL CORTEX; HIPPOCAMPUS; IN VIVO STUDY; ISOTOPE LABELING; MALE; NONHUMAN; RAT; THALAMUS;

ANILINE COMPOUNDS; ANIMALS; BENZOFURANS; BINDING, COMPETITIVE; BRAIN; DRUG DISCOVERY; INDOLES; LIGANDS; MALE; OXAZINES; PIPERIDINES; RATS; RATS, SPRAGUE-DAWLEY; RECEPTORS, SEROTONIN, 5-HT4; SEROTONIN RECEPTOR AGONISTS; SULFONAMIDES; TANDEM MASS SPECTROMETRY; TISSUE DISTRIBUTION;

EID: 84876473491     PISSN: 00223573     EISSN: 20427158     Source Type: Journal    
DOI: 10.1111/jphp.12030     Document Type: Article

References (47)

1. Bockaert J, et al. Pharmacological characterization of 5-hydroxytryptamine4 (5-HT4) receptors positively coupled to adenylate cyclase in adult guinea-pig hippocampal membranes: effect of substituted benzamide derivatives. Mol Pharmacol 1990; 37: 408-411.
2. Eglen RM, et al. Central 5-HT4 receptors. Trends Pharmacol Sci 1995; 16: 391-398.
3. Bonaventure P, et al. Mapping of serotonin 5-HT4 receptor mRNA and ligand binding sites in the post mortem human brain. Synapse 2000; 36: 35-46.
4. Domenech T, et al. Identification and characterization of serotonin 5-HT4 receptor binding sites in human brain: comparison with other mammalian species. Brain Res Mol Brain Res 1994; 21: 176-180.
5. Waeber C, et al. [3H]-GR113808 labels 5-HT4 receptors in the human and guinea-pig brain. Neuroreport 1993; 4: 1239-1242.
6. Medhurst AD, et al. Quantitative mRNA analysis of five C-terminal splice variants of the human 5-HT4 receptor in the central nervous system by TaqMan real time RT-PCR. Mol Brain Res 2001; 90: 125-134.
7. Dumuis A, et al. A nonclassical 5-hydroxytryptamine receptor positively coupled with adenylate cyclase in the central nervous system. Mol Pharmacol 1988; 34: 880-887.
8. Markstein R, et al. Pharmacological characterisation of 5-HT receptors positively coupled to adenylyl cyclase in the rat hippocampus. Naunyn Schmiedebergs Arch Pharmacol 1999; 359: 454-459.
9. Torres GE, et al. Cyclic AMP and protein kinase A mediate 5-hydroxytryptamine type 4 receptor regulation of calcium-activated potassium current in adult hippocampal neurons. Mol Pharmacol 1995; 47: 191-197.
10. Ullmer C, et al. Distribution of 5-HT4 receptor mRNA in the rat brain. Naunyn Schmiedebergs Arch Pharmacol 1996; 354: 210-212.
11. Kilbinger H, Wolf D,. Effect of 5-HT4 receptor stimulation on basal and electrically evoked release of acetylcholine from guinea pig myenteric plexus. Naunyn-Schmiedeberg's Arch Pharmacol 1992; 345: 270-275.
12. Matsuyama S, et al. Identification of putative 5-hydroxytryptamine 4 receptors in guinea pig stomach: the effect of TSK159, a novel agonist, on gastric motility and acetylcholine release. J Pharmacol Exp Ther 1996; 276: 989-995.
13. Takada K, et al. Regional difference in correlation of 5-HT4 receptor distribution with cholinergic transmission in the guinea pig stomach. Eur J Pharmacol 1999; 374: 489-494.
14. Consolo S, et al. 5-HT4 receptor stimulation facilitates acetylcholine release in rat frontal cortex. Neuroreport 1994; 5: 1230-1232.
15. Mohler EG, et al. VRX-03011, a novel 5-HT4 agonist, enhances memory and hippocampal acetylcholine efflux. Neuropharmacology 2007; 53: 563-573.
16. Fontana DJ, et al. The effects of novel, selective 5-hydroxytryptamine (5-HT)4 receptor ligands in rat spatial navigation. Neuropharmacology 1997; 36: 689-696.
17. Lamirault L, Simon H,. Enhancement of place and object recognition memory in young adult and old rats by RS 67333, a partial agonist of 5-HT4 receptors. Neuropharmacology 2001; 41: 844-853.
18. Moser PC, et al. SL65.0155, a novel 5-hydroxytryptamine(4) receptor partial agonist with potent cognitionenhancing properties. J Pharmacol Exp Ther 2002; 302: 731-741.
19. Yamaguchi T, et al. Evidence for 5-HT4 receptor involvement in the enhancement of acetylcholine release by p-chloroamphetamine in rat frontal cortex. Brain Res 1997a; 772: 95-101.
20. Yamaguchi T, et al. Facilitation of acetylcholine release in rat frontal cortex by indeloxazine hydrochloride: involvement of endogenous serotonin and 5-HT4 receptors. Naunyn Schmiedebergs Arch Pharmacol 1997b; 356: 712-720.
21. Reynolds GP, et al. 5-Hydroxytryptamine (5-HT)4 receptors in post mortem human brain tissue: distribution, pharmacology and effects of neurodegenerative diseases. Br J Pharmacol 1995; 114: 993-998.
22. Cachard-Chastel M, et al. Prucalopride and donepezil act synergistically to reverse scopolamine- induced memory deficit in C57Bl/6j mice. Behav Brain Res 2008; 187: 455-461.
23. Fontana DJ, et al. Stereoselective effects of (R)- and (S)-zacopride on cognitive performance in a spatial navigation task in rats. Neuropharmacology 1996; 35: 321-327.
24. Galeotti N, et al. Role of 5-HT4 receptors in the mouse passive avoidance test. J Pharmacol Exp Ther 1998; 286: 1115-1121.
25. Cachard-Chastel M, et al. 5-HT4 receptor agonists increase sAPPalpha levels in the cortex and hippocampus of male C57BL/6j mice. Br J Pharmacol 2007; 150: 883-892.
26. Lezoualc'h F, Robert SJ,. The serotonin 5-HT4 receptor and the amyloid precursor protein processing. Exp Gerontol 2003; 38: 159-166.
27. Robert SJ, et al. The human serotonin 5-HT4 receptor regulates secretion of non-amyloidogenic precursor protein. J Biol Chem 2001; 276: 44881-44888.
28. Turner PR, et al. Roles of amyloid precursor protein and its fragments in regulating neural activity, plasticity and memory. Prog Neurobiol 2003; 70: 1-32.
29. Johnson DE, et al. The 5-hydroxytryptamine 4 receptor agonists prucalopride and PRX-03140 increase acetylcholine and histamine levels in the rat prefrontal cortex and the power of stimulated hippocampal θ oscillations. JPET 2012; 341: 681-691.
30. Shen F, et al. 5-HT4 receptor agonist mediated enhancement of cognitive function in vivo and amyloid precursor protein processing in vitro: a pharmacodynamic and pharmacokinetic assessment. Neuropharmacology 2011; 61: 69-79.
31. Barth VN, et al. Comparison of rat dopamine D2 receptor occupancy for a series of antipsychotic drugs measured using radio labeled or nonlabeled raclopride tracer. Life Sci 2006; 78: 3007-3012.
32. Chernet E, et al. Use of LC/MS to assess brain tracer distribution in preclinical, in vivo receptor occupancy studies: dopamine D2, serotonin2A and NK-1 receptors as examples. Life Sci 2005; 78: 340-346.
33. Need AB, et al. In vivo rat brain opioid receptor binding of LY255582 assessed with a novel method using LC/MS/MS and the administration of three tracers simultaneously. Life Sci 2007; 81: 1389-1396.
34. 3 receptor antagonist in rats using non-radiolabeled tracer. J Pharmacol Toxicol Methods 2012; 65: 115-121.
35. 2 neuronal nicotinic acetylcholine receptor occupancy assay using LC-MS/MS. J Pharmacol Toxicol Methods 2012; 65: 136-141.
36. Pike VW, et al,. Synthesis and Evaluation of Radioligands for Imaging Brain Nociceptin/Orphanin FQ Peptide (NOP) Receptors with Positron Emission Tomography. J Med Chem 2011; 54: 2687-2700.
37. Mitch CH,. Discovery of aminobenzyloxyarylamides as K opioid receptor selective antagonists: application to preclinical development of a K opioid receptor antagonist receptor occupancy tracer. J Med Chem 2011; 54: 8000-8012.
38. Gee AD, et al. Synthesis and evaluation of [11C]SB207145 as the first in vivo serotonin 5-HT4 receptor radioligand for PET imaging in man. Curr Radiopharm 2008; 1: 110-114.
39. Kornum BR, et al. Evaluation of the novel 5-HT4 receptor PET ligand [11C]SB207145 in the Gottingen minipig. J Cereb Blood Flow Metab 2009; 29: 186-196.
40. Madsen K, et al. Mass dose effects and in vivo affinity in brain PET receptor studies a study of cerebral 5-HT4 receptor binding with [11C]SB207145. Nucl Med Biol 2011; 38: 1085-1091.
41. Marner L, et al. Kinetic modeling of 11C-SB207145 binding to 5-HT4 receptors in the human brain in vivo. J Nucl Med 2009; 50: 900-908.
42. Marner L, et al. Brain imaging of serotonin 4 receptors in humans with [11C] SB207145-PET. Neuroimage 2010; 50: 855-861.
43. Grimwood S, et al. Translational receptor occupancy for the 5-HT4 partial agonist PF-04995274 in rats, non-human primates and healthy volunteers. Alzheimers Dement 2011; 7 (4 Suppl.) S653.
44. Curtet S, et al. New arylpiperazine derivatives as antagonists of the human cloned 5-HT4 receptor isoforms. J Med Chem 2000; 43: 3761-3769.
45. Mialet J, et al. Pharmacological characterization of the human 5-HT4(d) receptor splice variant stably expressed in Chinese hamster ovary cells. Br J Pharmacol 2000; 131: 827-835.
46. Wardle KA, et al. Selective and functional 5-hydroxytryptamine4 receptor antagonism by SB 207266. Br J Pharmacol 1996; 118: 665-670.
47. Beattie D, et al. The pharmacology of TD-8954, a potent and selective 5-HT4 receptor agonist with gastrointestinal prokinetic properties. Front Pharmacol 2011; 2: 25.