Nociceptin/Orphanin

The four opioid receptors display in vivo binding preference for mu-endorphins and endomorphins, delta-enkephalins, kappa-dynorphin and ORLl-nociceptin/orphanin FQ (Table 12.2). [Pg.258]

Compound 24 represents a series of potent spiropiperidine GlyT-1 inhibitors that showed significant binding to the p opioid and nociceptin/ orphanin FQ peptide (NOP) receptors [67]. The hydroxy analog 25 demonstrated improved selectivity and N-propyl analog 26 exhibited increased microsomal stability but reduced GlyT-1 potency (EC50 = 450 nM) [68]. [Pg.27]

The method appears to be particularly suitable for the study of expensive compounds and/or species available in very low amounts. Figure 10.19 shows the application of IM to the study of the adsorption equilibria of a polypeptide, nociceptin/orphanin FQ, on a C,g column [40]. Isotherms (Figure 10.20) were obtained by numerical procedure through the fitting of the overloaded band profiles obtained under different conditions. Adsorption data allowed for the prediction of the band profile under overloaded gradient conditions (Figure 10.21) with a minimal amount of compound consumption. [Pg.301]

Moran TD et al. Cellular neurophysiological actions of nociceptin/orphanin FQ. Peptides 2000 21 969-976. [Pg.329]

Figure 7.1 Amino acid structure of nociceptin/Orphanin FQ.

Lambert DG The nociceptin/orphanin FQ receptor A target with broad therapeutic potential. Nat Rev Drug Discov 2008 7 694. [PMID 18670432]... [Pg.710]

Calo, G., Bigoni, R., Rizzi, A., Guerrini, R., Salvadori, S., Regoli, D. Nociceptin/orphanin FQ receptor ligands, Peptides 2000, 21, 935-947. [Pg.147]

Ichikawa, D., Ozaki, S., Azuma, T., Nambu, H., Kawamoto, H., Iwasawa, Y., Takeshima, H., Ohta, H. In vitro inhibitory effects J-113397 on nociceptin/orphanin FQ-stimulated f5SJGTP/S binding to mouse brain, Neuroreport 2001, 12, 1757-1761. [Pg.473]

Meunier, J.-C. Nociceptin /orphanin FQ and the opioid receptor-like ORL1 receptor, Eur. J. Pharmacol. 1997, 340, 1-15. [Pg.474]

Schlicker E, Kathmann M (2000) Modulation of the release of noradrenaline and other transmitters via cannabinoid and opioid receptors. Fundam Clin Pharmacol 14 64 Schlicker E, Morari M (2000) Nociceptin/orphanin FQ and neurotransmitter release in the central... [Pg.433]

Chu, X., Xu, N., Li, P., Mao, L., and Wang, J.Q. 1999. Inhibition of cardiovascular activity following microinjection of novel opioid-like neuropeptide nociceptin (orphanin FQ) into the rat rostral ventrolateral medulla. Brain Res. 829, 134-142. [Pg.253]

Experimental agents were evaluated in a receptor binding assay with 3H-nociceptin/orphanin FQ with membranes of recombinant CHO-ORLj cells according to the method of Ardati (1). Testing results are provided in Table 2. [Pg.104]

Inoue K, Tsuda M, Tozaki-Saitoh H (2007) Modification of neuropathic pain sensation through microglial ATP receptors. Purinergic Signal 3 311-316 Inoue M, Kawashima T, AUen RG, Ueda H (2003) Nodstatin and prepro-nociceptin/orphanin FQ 160-187 cause nociception through activation of Gj/o in capsaidn-sensitive and... [Pg.502]

Joseph T, Lee TL, Li C, Siau C, Nishiuchi Y, Kimura T, Tachibana S (2007) Levels of neuropeptides nocistatin, nociceptin/orphanin FQ and their precursor protein in a rat neuropathic pain model. Peptides 28 1433-1440... [Pg.504]

Mabuchi T, Matsumura S, Okuda-Ashitaka E, Kitano T, Kojima H, Nagano T, Minami T, Ito S (2003) Attenuation of neuropathic pain by the nociceptin/orphanin FQ antagonist JTC-801 is mediated by inhibition of nitric oxide production. Eur J Neurosci 17 1384-1392 Mabuchi T, Shintani N, Matsumura S, Okuda-Ashitaka E, Hashimoto H, Muratani T, Minami T, Baba A, Ito S (2004) Pituitary adenylate cyclase-activating polypeptide is required for the development of spinal sensitization and induction of neuropathic pain. J Neurosci 24 7283-7291... [Pg.509]

Okuda-Ashitaka E, Ito S (2000) Nocistatin a novel neuropeptide encoded by the gene for the nociceptin/orphanin FQ precursor. Peptides 21 1101-1109 Okuda-Ashitaka E, Minami T, Tachibana S, Yoshihtira Y, Nishiuchi Y, Kimura T, Ito S (1998) Nocistatin, a peptide that blocks nociceptin action in ptiin transmission. Nature 392 286-289... [Pg.515]

Scoto GM, Santangelo N, Parent C (2005) Effect of supraspinal nocistatin on nociceptin/orphanin FQ antagonism of selective opioid analgesia. Neurosci Lett 387 126-129... [Pg.522]

Yamamoto T, Sakashita Y (1999) Effect of nocistatin and its interaction with nociceptin/orphanin... [Pg.532]

Ouagazzal AM, Moreau JL, Pauly-Evers M, Jenck F. Impact of environmental housing conditions on the emotional responses of mice deficient for nociceptin/orphanin FQ peptide precursor gene. Behav. Brain Res. 2003 144 111-117. [Pg.2262]

Waits PS, Purcell WM, Fulford AJ, McLeod JD (2004) Nociceptin/ orphanin FQ modulates human T cell function in vitro. J Neuroim-munol 149 110-120. [Pg.494]

Peluso J, LaForge KS, Matthes HW, Kreek Ml, Kieffer BL, Gaveriaux-Ruff C (1998) Distribution of nociceptin/orphanin FQ receptor transcript in human central nervous system and immune cells. J Neuroimmunol 81 184-192. [Pg.493]

Bridge KE, Wainwright A, Reilly K, Oliver KR (2003) Autoradiographic localization of I[Tyr ] nociceptin/orphanin EQ binding sites in macaque primate CNS. Neuroscience 118 513-523. [Pg.562]

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