Pharmacological characterization of the nociceptin/orphanin FQ receptor antagonist SB-612111 [(-)-cis-1-methyl-7-[[4-(2,6-dichlorophenyl)piperidin-1-yl] methyl]-6,7,8,9-tetrahydro-5H-benzocyclohepten-5-ol]: In vitro studies

Journal of Pharmacology and Experimental Therapeutics

Volumn 321, Issue 3, 2007, Pages 961-967

  Spagnolo, Barbara ^a   Carrà, Giacomo ^a   Fantin, Martina ^a   Fischetti, Carmela ^a   Hebbes, Chris ^c   McDonald, John ^c   Barnes, Timothy A ^c   Rizzi, Anna ^a   Trapella, Claudio ^b   Fanton, Giulia ^b   Morari, Michele ^a   Lambert, Dave G ^c   Regoli, Domenico ^a   Calò, Girolamo ^a,d  

^a Istituto Nazionale di Neuroscience   (Italy)

^b UNIVERSITY OF FERRARA   (Italy)

^c UNIVERSITY OF LEICESTER   (United Kingdom)

^d Section of Pharmacology   (Italy)

Author keywords

[No Author keywords available]

Indexed keywords

1 (1 CYCLOOCTYLMETHYL 3 HYDROXYMETHYL 4 PIPERIDYL) 3 ETHYL 1,3 DIHYDRO 2H BENZIMIDAZOL 2 ONE; 7 [4 (2,6 DICHLOROPHENYL) 1 PIPERIDINYLMETHYL] 6,7,8,9 TETRAHYDRO 1 METHYL 5H BENZOCYCLOHEPTEN 5 OL; CYCLIC AMP; ENDOMORPHIN 1; GUANOSINE TRIPHOSPHATE; NOCICEPTIN RECEPTOR; NOCICEPTIN RECEPTOR ANTAGONIST; RECOMBINANT PROTEIN; UNCLASSIFIED DRUG;

ANIMAL CELL; ANIMAL TISSUE; ARTICLE; BINDING AFFINITY; BINDING COMPETITION; BRAIN CORTEX; CELL MEMBRANE; CONTROLLED STUDY; DRUG ANTAGONISM; DRUG BINDING; DRUG MECHANISM; DRUG POTENCY; DRUG RECEPTOR BINDING; DRUG SPECIFICITY; ELECTROSTIMULATION; GUINEA PIG; ILEUM; IN VITRO STUDY; MALE; MOUSE; NONHUMAN; PRIORITY JOURNAL; PROTEIN EXPRESSION; RAT; SYNAPTOSOME; VAS DEFERENS;

ANIMALS; BENZIMIDAZOLES; BINDING, COMPETITIVE; CELL MEMBRANE; CHO CELLS; CRICETINAE; CRICETULUS; CYCLIC AMP; CYCLOHEPTANES; FORSKOLIN; GUANOSINE 5'-O-(3-THIOTRIPHOSPHATE); GUINEA PIGS; HUMANS; ILEUM; MALE; MICE; NARCOTIC ANTAGONISTS; OPIOID PEPTIDES; PEPTIDE FRAGMENTS; PIPERIDINES; RATS; RATS, SPRAGUE-DAWLEY; RECEPTORS, OPIOID; SYNAPTOSOMES; TRANSFECTION; VAS DEFERENS;

EID: 34248525042     PISSN: 00223565     EISSN: 15210103     Source Type: Journal    
DOI: 10.1124/jpet.106.116764     Document Type: Article

References (25)

1. Bigoni R, Giuliani S, Calò G, Rizzi A, Guerrini R, Salvadori S, Regoli D, and Maggi CA (1999) Characterization of nociceptin receptors in the periphery: in vitro and in vivo studies. Naunyn-Schmiedeberg's Arch Pharmacol 359:160-167.
2. Bigoni R, Calò G, Rizzi A, Guerrini R, De Risi C, Hashimoto Y, Hashiba E, Lambert DG, and Regoli D (2000) In vitro characterization of J-113397, a non-peptide nociceptin/orphanin FQ receptor antagonist. Naunyn-Schmiedeberg's Arch Pharmacol 361:565-568.
3. Brown BL, Albano JD, Ekins RP, and Sgherzi AM (1971) A simple and sensitive saturation assay method for the measurement of adenosine 3′:5′-cyclic monophosphate. Biochem J 121:561-562.
4. Calò G, Guerrini R, Rizzi A, Salvadori S, Burmeister M, Kapusta DR, Lambert DG, and Regoli D (2005) UFP-101, a peptide antagonist selective for the nociceptin/orphanin FQ receptor. CNS Drug Rev 11:97-112.
5. Calò G, Guerrini R, Rizzi A, Salvadori S, and Regoli D (2000) Pharmacology of nociceptin and its receptor: a novel therapeutic target. Br J Pharmacol 129:1261-1283.
6. Calò G, Rizzi A, Bigoni R, Guerrini R, Salvadori S, and Regoli D (2002) Pharmacological profile of nociceptin/orphanin FQ receptors. Clin Exp Pharmacol Physiol 29:223-228.
7. 50) of an enzymatic reaction. Biochem Pharmacol 22:3099-3108.
8. Cox BM, Chavkin C, Christie MJ, Civelli O, Evans C, Hamon MD, Hoellt V, Kieffer B, Kitchen I, McKnight AT, et al. (2000) Opioid receptors, in The IUPHAR Compendium of Receptor Characterization and Classification (Girdlestone D ed) pp 321-333, IUPHAR Media Ltd., London, UK.
9. De Risi C, Piero Pollini G, Trapella C, Peretto I, Ronzoni S, and Giardina GA (2001) A new synthetic approach to 1-[(3R,4R)-1- cyclooctylmethyl-3-hydroxymethyl-4-piperidyl]-3-ethyl-1,3-dihydro-benzimidazol- 2-one(J-113397), the first non-peptide ORL-1 receptor antagonist. Bioorg Med Chem 9:1871-1877.
10. Goto Y, Arai-Otsuki S, Tachibana Y, Ichikawa D, Ozaki S, Takahashi Y, Okamoto O, Okuda S, Ohta H, and Sagara T (2006) Identification of a novel spiropiperidine opioid receptor-like 1 antagonist class by a focused library approach featuring 3D-pharmacophore similarity. J Med Chem 49:847-849.
11. Guerrini R, Calò G, Rizzi A, Bianchi C, Lazarus LH, Salvadori S, Temussi PA, and Regoli D (1997) Address and message sequences for the nociceptin receptor: a structure-activity study of nociceptin-(1-13)-peptide amide. J Med Chem 40:1789-1793.
12. Hughes J, Kosterlitz HW, and Leslie FM (1975) Effect of morphine on adrenergic transmission in the mouse vas deferens: assessment of agonist and antagonist potencies of narcotic analgesics. Br J Pharmacol 53:371-381.
13. 2. Naunyn-Schmiedeberg's Arch Pharmacol 368:528-537.
14. Lowry OH, Rosenbrough NJ, Farr AL, and Randall RJ (1951) Protein measurement with the Folin phenol reagent. J Biol Chem 193:265-275.
15. McDonald J, Calò G, Guerrini R, and Lambert DG (2003) UFP-101, a high affinity antagonist for the nociceptin/orphanin FQ receptor: radioligand and GTPgamma(35)S binding studies. Naunyn-Schmiedeberg's Arch Pharmacol 367: 183-187.
16. Mela F, Marti M, Ulazzi L, Vaccari E, Zucchini S, Trapella C, Salvadori S, Beani L, Bianchi C, and Morari M(2004) Pharmacological profile of nociceptin/orphanin FQ receptors regulating 5-hydroxytryptamine release in the mouse neocortex. Eur J Neurosci 19:1317-1324.
17. Meunier JC, Mollereau C, Toll L, Suaudeau C, Moisand C, Alvinerie P, Butour JL, Guillemot JC, Ferrara P, Monserrat B, et al. (1995) Isolation and structure of the endogenous agonist of opioid receptor-like ORL1 receptor. Nature (Lond) 377:532-535.
18. Neubig RR, Spedding M, Kenakin T, and Christopoulos A (2003) International Union of Pharmacology Committee on Receptor Nomenclature and Drug Classification: XXXVIII. Update on terms and symbols in quantitative pharmacology. Pharmacol Rev 55:597-606.
19. Palombi G and Ronzoni S (2003), inventors, GlaxoSmithKline S.P.A., assignee. Preparation of benzosuberonylpiperidine compounds. World patent WO 03/04009 A1. 2003 May 15.
20. Paton WDM (1957) The action of morphine and related substances on contraction and on acetylcholine output of coaxially stimulated guinea pig ileum. Br J Pharmacol 12:119-127.
21. Ozaki S, Kawamoto H, Itoh Y, Miyaji M, Azuma T, Ichikawa D, Nambu H, Iguchi T, Iwasawa Y, and Ohta H (2000) In vitro and in vivo pharmacological characterization of J-113397, a potent and selective non-peptidyl ORL1 receptor antagonist. Eur J Pharmacol 402:45-53.
22. Reinscheid RK, Nothacker HP, Bourson A, Ardati A, Henningsen RA, Bunzow JR, Grandy DK, Langen H, Monsma FJ Jr, and Civelli O (1995) Orphanin FQ: a neuropeptide that activates an opioidlike G protein-coupled receptor. Science (Wash DC) 270:792-794.
23. Sbrenna S, Marti M, Morari M, Calò G, Guerrini R, Beani L, and Bianchi C (2000) Modulation of 5-hydroxytryptamine efflux from rat cortical synaptosomes by opioids and nociceptin. Br J Pharmacol 130:425-433.
24. Schulz R, Faase E, Wuster M, and Herz A (1979) Selective receptors for betaendorphin on the rat vas deferens. Life Sci 24:843-850.
25. Zaratin PF, Petrone G, Sbacchi M, Garnier M, Fossati C, Petrillo P, Ronzoni S, Giardina GA, and Scheideler MA (2004) Modification of nociception and morphine tolerance by the selective opiate receptor-like orphan receptor antagonist (-)-cis-1-methyl-7-[[4-(2,6-dichlorophenyl)piperidin-1-yl] methyl]-6,7,8,9- tetrahydro-5Hbenzocyclohepten-5-ol (SB-612111). J Pharmacol Exp Ther 308:454-461.