Comparative biochemical and pharmacological characterization of a novel, NOP receptor selective hexapeptide, Ac-RYYRIR-ol.
作者： Engin Bojnik , Fruzsina Babos , Carmela Fischetti , Anna Magyar , Valeria Camarda
DOI: 10.1016/J.BRAINRESBULL.2009.09.013
关键词:
摘要: Abstract Nociceptin/orphanin FQ (N/OFQ) is an endogenous neuropeptide, which widely distributed in central and peripheral nervous system. Some N/OFQ sequence unrelated hexapeptides can effectively bind to the peptide (NOP) receptor they were used as template for structure-activity studies that lead discovery of new NOP selective ligands. In present study, pharmacological profile novel hexapeptide Ac-RYYRIR-ol was investigated using various vitro assays including binding G-protein activation rat brain membranes, mouse vas deferens, guinea pig ileum, colon Ca 2+ mobilization assay chinese hamster ovary (CHO) cells co-expressing human recombinant C-terminally modified Gα qi5 protein. membranes displaced both [ 3 H]nociceptin/OFQ H]Ac-RYYRIK-ol with high affinity (p K i 9.35 8.81, respectively) stimulated 35 S]GTPγS showing however lower maximal effects than ( α = 0.28). The stimulatory effect antagonized by antagonist UFP-101. electrically deferens displayed negligible agonist activity while antagonizing a competitive manner (pA 2 7.99) inhibitory N/OFQ. Similar results obtained deferens. produced concentration dependent contractile similar potency Finally, performed CHO-hNOP-Gα = 0.87) compared conclusion, has been shown have fine selectivity, potency, furthermore toward receptors measured assays; this likely due its partial activity.
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Paola F. Zaratin, Giuseppe Petrone, Massimo Sbacchi, Martine Garnier, Claudia Fossati, Paola Petrillo, Silvio Ronzoni, Giuseppe A. M. Giardina, Mark A. Scheideler, 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-5H-benzocyclohepten-5-ol (SB-612111). Journal of Pharmacology and Experimental Therapeutics. ,vol. 308, pp. 454- 461 ,(2004) , 10.1124/JPET.103.055848
Zhizhong Z. Pan, Naomi Hirakawa, Howard L. Fields, A Cellular Mechanism for the Bidirectional Pain-Modulating Actions of Orphanin FQ/Nociceptin Neuron. ,vol. 26, pp. 515- 522 ,(2000) , 10.1016/S0896-6273(00)81183-6
Hartmut Berger, Raffaella Bigoni, Erika Albrecht, Regina M Richter, Eberhard Krause, Michael Bienert, Girolamo Calo’, The nociceptin/orphanin FQ receptor ligand acetyl-RYYRIK-amide exhibits antagonistic and agonistic properties Peptides. ,vol. 21, pp. 1131- 1139 ,(2000) , 10.1016/S0196-9781(00)00251-5
Özge Gündüz, Anna Rizzi, Anna Baldisserotto, Remo Guerrini, Barbara Spagnolo, Elaine C Gavioli, László Kocsis, Anna Magyar, Sándor Benyhe, Anna Borsodi, Girolamo Calò, None, In vitro and in vivo pharmacological characterization of the nociceptin/orphanin FQ receptor ligand Ac-RYYRIK-ol. European Journal of Pharmacology. ,vol. 539, pp. 39- 48 ,(2006) , 10.1016/J.EJPHAR.2006.03.075
Remo Guerrini, Girolamo Calo, Anna Rizzi, Raffaella Bigoni, Clementina Bianchi, Severo Salvadori, Domenico Regoli, A new selective antagonist of the nociceptin receptor British Journal of Pharmacology. ,vol. 123, pp. 163- 165 ,(1998) , 10.1038/SJ.BJP.0701640
Mahmoud Al-Khrasani, György Orosz, László Kocsis, Viktor Farkas, Anna Magyar, Imre Lengyel, Sándor Benyhe, Anna Borsodi, András Z Rónai, Receptor constants for endomorphin-1 and endomorphin-1-ol indicate differences in efficacy and receptor occupancy European Journal of Pharmacology. ,vol. 421, pp. 61- 67 ,(2001) , 10.1016/S0014-2999(01)01014-7
S.L. Mason, M. Ho, J. Nicholson, A.T. McKnight, In vitro characterization of Ac-RYYRWK-NH2, Ac-RYYRIK-NH2 and [Phe1CΨ(CH2-NH)Gly2] nociceptin(1-13)NH2 at rat native and recombinant ORL1 receptors Neuropeptides. ,vol. 35, pp. 244- 256 ,(2001) , 10.1054/NPEP.2001.0882
Daniel R. Kapusta, Melissa A. Burmeister, Girolamo Calo', Remo Guerrini, Helmut B. Gottlieb, Velga A. Kenigs, Functional Selectivity of Nociceptin/Orphanin FQ Peptide Receptor Partial Agonists on Cardiovascular and Renal Function Journal of Pharmacology and Experimental Therapeutics. ,vol. 314, pp. 643- 651 ,(2005) , 10.1124/JPET.104.082768
Engin Bojnik, Judit Farkas, Anna Magyar, Csaba Tömböly, Ümit Güçlü, Özge Gündüz, Anna Borsodi, Maïthe Corbani, Sándor Benyhe, None, Selective and high affinity labeling of neuronal and recombinant nociceptin receptors with the hexapeptide radioprobe [3H]Ac-RYYRIK-ol Neurochemistry International. ,vol. 55, pp. 458- 466 ,(2009) , 10.1016/J.NEUINT.2009.04.014
John R.W Menzies, Tracey Glen, Matthew R.P Davies, Stewart J Paterson, Alistair D Corbett, In vitro agonist effects of nociceptin and [Phe1ψ(CH2-NH)Gly2]nociceptin(1-13)NH2 in the mouse and rat colon and the mouse vas deferens European Journal of Pharmacology. ,vol. 385, pp. 217- 223 ,(1999) , 10.1016/S0014-2999(99)00700-1