Nociceptin inhibits capsaicin-induced bronchoconstriction in isolated guinea pig lung

Corboz, Michel R.; Rivelli, Maria A.; Egan, Robert W.; Tulshian, Deen; Matasi, Julius J.; Fawzi, Ahmad; Benbow, Lawrence; Smith-Torhan, April; Zhang, Hongtao; Hey, John A.

doi:10.1016/s0014-2999(00)00505-7

Cited by 55 publications

(40 citation statements)

References 45 publications

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“…J-113397 is a nonpeptide compound recently identified by investigators at Banyu as a selective antagonist of the recombinant human OP 4 receptor (Kawamoto et al, 1999). The antagonist properties and selectivity of action of J-113397 have later been confirmed in vitro on the native OP 4 receptor expressed in isolated tissues (Bigoni et al, 2000;Corboz et al, 2000) and in several in vivo studies (Ozaki et al, 2000;Ueda et al, 2000;McLeod et al, 2001 Bigoni et al, 2000;Calo' et al, 2000b) These data indicate that the addition of two positively charged residues, Arg 14 and Lys 15 , to the sequence of NC leads to increased potency, possibly through an increase in receptor affinity. However, Okada et al (2000) than the natural peptide.…”

Section: Discussionmentioning

confidence: 99%

[Arg¹⁴,Lys¹⁵]Nociceptin, a Highly Potent Agonist of the Nociceptin/Orphanin FQ Receptor: in Vitro and in Vivo Studies

Rizzi¹,

Rizzi²,

Bigoni³

et al. 2002

J Pharmacol Exp Ther

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Nociceptin (NC)/orphanin FQ is the endogenous ligand of a seven-transmembrane domain G protein-coupled receptor, referred to as OP 4 . NC and the OP 4 receptor are structurally related to opioid peptides and receptors; however, NC does not interact with classical opioid receptors, and the OP 4 receptor does not bind any selective opioid receptor ligand (for recent reviews, see Calo' et al., 2000c;Meunier, 2000). It has been demonstrated that NC modulates several biological functions, including pain threshold, morphine analgesia, food intake, anxiety, locomotor activity, memory processes, and cardiovascular, renal, respiratory, and gastrointestinal functions (Calo' et al., 2000c;Meunier, 2000). Further investigations of physiological and pathological roles of the NC/OP 4 system require new molecules that potently activate (agonists) or block (antagonists) the OP 4 receptor. Identification of such new molecules (at least of peptide nature) should be facilitated by the knowledge of the amino acid residues of the NC sequence that are critical for receptor occupation and activation. Over the last 5 years, several structure-activity relationship studies have been performed on NC (Dooley and

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Section: Discussionmentioning

confidence: 99%

[Arg¹⁴,Lys¹⁵]Nociceptin, a Highly Potent Agonist of the Nociceptin/Orphanin FQ Receptor: in Vitro and in Vivo Studies

Rizzi¹,

Rizzi²,

Bigoni³

et al. 2002

J Pharmacol Exp Ther

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“…NOP receptor binding assays were performed as described by Fawzi et al (1997) and Corboz et al (2000). In brief, CHO cell membranes expressing human NOP receptors were incubated with 125 I-[Tyr14]-N/OFQ (PerkinElmer Life and Analytical Sciences, Waltham, MA) and increasing concentrations of compound in binding assay buffer containing 50 mM HEPES, pH 7.4, 2.5 mM CaCl 2 , 1 mM MgCl 2 , 10 mM NaCl, 0.025% bacitracin, and 0.1% bovine serum albumin.…”

Section: Methodsmentioning

confidence: 99%

“…Total and nonspecific binding was determined in quadruplicates. Opioid receptor binding assays (-, -, and ␦-opioid receptors) were performed on CHO cell membranes expressing the human opioid receptors (Receptor Biology, Beltsville, MD) as described by Corboz et al (2000). In brief, CHO cell membranes were incubated with [ 3 H]diprenorphine (PerkinElmer Life and Analytical Sciences) and increasing concentrations of compounds in binding assay buffer for 60 min at room temperature.…”

Section: Methodsmentioning

confidence: 99%

The Anxiolytic-Like Effects of the Novel, Orally Active Nociceptin Opioid Receptor Agonist 8-[bis(2-Methylphenyl)methyl]-3-phenyl-8-azabicyclo[3.2.1]octan-3-ol (SCH 221510)

Varty¹,

Lu²,

Morgan³

et al. 2008

J Pharmacol Exp Ther

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Orphanin FQ/nociceptin (OFQ/N) is the endogenously occurring peptide ligand for the nociceptin opioid receptor (NOP) that produces anxiolytic-like effects in mice and rats. The present study assessed the anxiolytic-like activity of 8-[bis(2-methylphenyl)-methyl]-3-phenyl-8-azabicyclo[3.2.1]octan-3-ol (SCH 221510), a novel potent piperidine NOP agonist (EC 50 ϭ 12 nM) that binds with high affinity (K i ϭ 0.3 nM) and functional selectivity (Ͼ50-fold over the -, -, and ␦-opioid receptors). The anxiolytic-like activity and side-effect profile of SCH 221510 were assessed in a variety of models and the benzodiazepine, chlordiazepoxide (CDP), was included for comparison. The effects of chronic dosing of SCH 221510 were also assessed. Furthermore, the specificity of the anxiolytic-like effect of SCH 221510 was investigated with the NOP receptor antagonist 1-[(3R,4R)-1-cyclooctylmethyl-3-hydroxymethyl-4-piperidyl]-3-ethyl-1,3-dihydro-2H-benzimidazol-2-one (J-113397) and the opioid receptor antagonist naltrexone. Like CDP (1-30 mg/kg i.p.), SCH 221510 (1-30 mg/kg p.o.) produced anxiolytic-like effects in the elevated plus-maze (rat and gerbil), Vogel conflict (rat), conditioned lick suppression (rat), fear-potentiated startle (rat), and pup separation-induced vocalization (guinea pig) assays. In the Vogel conflict, the anxiolytic-like effect of SCH 221510 (10 mg/kg) was attenuated by J-113397 (3-10 mg/kg p.o.), but not naltrexone (3-30 mg/kg i.p.). Additionally, the anxiolytic-like effects of SCH 221510 did not change appreciably following 14-day b.i.d. dosing in rats (10 mg/kg). Furthermore, unlike CDP, SCH 221510 (3-30 mg/kg) produced anxiolytic-like activity at doses that did not disrupt overt behavior. Collectively, these data suggest that NOP agonists such as SCH 221510 may have an anxiolytic-like profile similar to benzodiazepines, with a reduced side-effect liability.The nociceptin opioid receptor (NOP) was identified using a human cDNA library on the basis of close homology with the -, -, and ␦-opioid receptors (Bunzow et al., 1994;Mollereau et al., 1994). Subsequently, the endogenous ligand for the NOP receptor, orphanin FQ/nociceptin (OFQ/N), was identified from brain extracts and found to bind with high affinity to the NOP site, but not to -, -, or ␦-opioid receptors (Meunier et al., 1995;Reinscheid et al., 1995). Immunohistochemical studies demonstrated that the mRNA for OFQ/N and its precursor prepronociceptin, as well as immunoreactivity for the NOP receptor, are localized to corticolimbic regions of the central nervous system (CNS). These regions include the amygdaloid complex, septohippocampal regions, periaqueductal gray, locus coeruleus, and dorsal raphe nucleus (Darland et al., 1998). In vitro electrophysiological studies using brain slices have shown that OFQ/N has potent Article, publication date, and citation information can be found at

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“…By use of the specific nociceptin receptor antagonist [Phe1p-si(CH2-NH)Gly2]NC(1-13)NH2 ([F/G]NC(1-13)NH2), the nociceptin-induced inhibition of tachykinergic contraction was subsequently identified (116). A further report using the new ORL1 receptor nonpeptide antagonist J-113397 indicates that nociceptin may inhibit capsaicin-evoked tachykinin release from sensory nerve terminals in guinea pig lung by a prejunctional mechanism (117).…”

Section: Blockage Of Neuropeptide Releasementioning

confidence: 99%

Neurogenic mechanisms in bronchial inflammatory diseases

Groneberg

Quarcoo

Frossard

et al. 2004

Allergy

153

103

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Neurogenic inflammation encompasses the release of neuropeptides from airway nerves leading to inflammatory effects. This neurogenic inflammatory response of the airways can be initiated by exogenous irritants such as cigarette smoke or gases and is characterized by a bi‐directional linkage between airway nerves and airway inflammation. The event of neurogenic inflammation may participate in the development and progression of chronic inflammatory airway diseases such as allergic asthma or chronic obstructive pulmonary disease (COPD). The molecular mechanisms underlying neurogenic inflammation are orchestrated by a large number of neuropeptides including tachykinins such as substance P and neurokinin A, or calcitonin gene‐related peptide. Also, other biologically active peptides such as neuropeptide tyrosine, vasoactive intestinal polypeptide or endogenous opioids may modulate the inflammatory response and recently, novel tachykinins such as virokinin and hemokinins were identified. Whereas the different aspects of neurogenic inflammation have been studied in detail in laboratory animal models, only little is known about the role of airway neurogenic inflammation in human diseases. However, different functional properties of airway nerves may be used as targets for future therapeutic strategies and recent clinical data indicates that novel dual receptor antagonists may be relevant new drugs for bronchial asthma or COPD.

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Nociceptin inhibits capsaicin-induced bronchoconstriction in isolated guinea pig lung

Cited by 55 publications

References 45 publications

[Arg¹⁴,Lys¹⁵]Nociceptin, a Highly Potent Agonist of the Nociceptin/Orphanin FQ Receptor: in Vitro and in Vivo Studies

[Arg¹⁴,Lys¹⁵]Nociceptin, a Highly Potent Agonist of the Nociceptin/Orphanin FQ Receptor: in Vitro and in Vivo Studies

The Anxiolytic-Like Effects of the Novel, Orally Active Nociceptin Opioid Receptor Agonist 8-[bis(2-Methylphenyl)methyl]-3-phenyl-8-azabicyclo[3.2.1]octan-3-ol (SCH 221510)

Neurogenic mechanisms in bronchial inflammatory diseases

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Nociceptin inhibits capsaicin-induced bronchoconstriction in isolated guinea pig lung

Cited by 55 publications

References 45 publications

[Arg14,Lys15]Nociceptin, a Highly Potent Agonist of the Nociceptin/Orphanin FQ Receptor: in Vitro and in Vivo Studies

[Arg14,Lys15]Nociceptin, a Highly Potent Agonist of the Nociceptin/Orphanin FQ Receptor: in Vitro and in Vivo Studies

The Anxiolytic-Like Effects of the Novel, Orally Active Nociceptin Opioid Receptor Agonist 8-[bis(2-Methylphenyl)methyl]-3-phenyl-8-azabicyclo[3.2.1]octan-3-ol (SCH 221510)

Neurogenic mechanisms in bronchial inflammatory diseases

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[Arg¹⁴,Lys¹⁵]Nociceptin, a Highly Potent Agonist of the Nociceptin/Orphanin FQ Receptor: in Vitro and in Vivo Studies

[Arg¹⁴,Lys¹⁵]Nociceptin, a Highly Potent Agonist of the Nociceptin/Orphanin FQ Receptor: in Vitro and in Vivo Studies