[Phe1Ψ(CH2-NH)Gly2]Nociceptin(1-13)NH2 - CAS 213130-17-7
Category: Inhibitor
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Molecular Formula:
Molecular Weight:
Opioid Receptor
[Phe1Ψ(CH2-NH)Gly2]Nociceptin(1-13)NH2 is the first selective antagonist to prevent the binding of the endogenous ligand orphanin FQ​/Nociceptin (OFQ​/N) at the orphan opioid-​like receptor, demonstrated both in vitro and in vivo. It is selective, competitive antagonism at the nociceptin receptor has also been reported (pA2 = 7.02 and 6.75 in the guinea pig ileum and mouse vas deferens respectively).
(Modifications: Phe-1-Gly-2 peptide bond replace with Psi-(CH2-NH), Lys-13 = C-terminal amide)
(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[2-[[(2S,3R)-2-[[(2S)-2-[[2-[[2-[[(2S)-2-amino-3-phenylpropyl]amino]acetyl]amino]acetyl]amino]-3-phenylpropanoyl]amino]-3-hydroxybutanoyl]amino]acetyl]amino]propanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]hexanoyl]amino]-3-hydroxypropanoyl]amino]propanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]hexanamide; N-[(2S)-2-Amino-3-phenylpropyl]glycylglycyl-L-phenylalanyl-L-threonylglycyl-L-alanyl-L-arginyl-L-lysyl-L-seryl-L-alanyl-L-arginyl-L-lysinamide; N-[(2S)-2-Amino-3-phenylpropyl]-13-L-lysinamide-2-13-orphanin FQ (swine)
Soluble to 0.70 mg/ml in water
Store in a cool and dry place (or refer to the Certificate of Analysis).
Canonical SMILES:
1.Spontaneous transient outward currents: modulation by nociceptin in murine dentate gyrus granule cells.
Shirasaki T;Houtani T;Sugimoto T;Matsuda H Brain Res. 2001 Nov 2;917(2):191-205.
Spontaneous transient outward currents have been found in peripheral neurons and smooth muscle cells, but rarely in central neurons. Using a nystatin-perforated patch clamp technique, we succeeded in recording spontaneous transient outward currents in mouse dentate gyrus granule cells. Nociceptin/orphanin FQ increased the amplitude and frequency of transient outward currents. We consider modulation of spontaneous transient outward currents to be a new means to regulate cell activity in central neurons, and studied their characteristics and mechanism of augmentation. The whole-cell current-voltage relationship showed outward rectification and the reversal potential was close to the equilibrium potential for K+. The frequency of spontaneous transient outward currents increased at depolarized potentials. Tetraethylammonium, iberiotoxin and a Ca2+ chelator BAPTA-AM inhibited spontaneous transient outward currents. These results suggest the involvement of large-conductance Ca2+-activated K+ channels. Single-channel recordings in the inside-out configuration revealed Ca2+-activated K+ channels with a conductance ranging from 82 to 352 pS. The augmenting effect of nociceptin/orphanin FQ was cancelled by [Phe1psi(CH2-NH)Gly2]Nociceptin(1-13)NH2.
2.Modulation of the cardiac autonomic transmission of pithed rats by presynaptic opioid OP4 and cannabinoid CB1 receptors.
Malinowska B;Piszcz J;Koneczny B;Hryniewicz A;Schlicker E Naunyn Schmiedebergs Arch Pharmacol. 2001 Sep;364(3):233-41.
We studied the effects of nociceptin, the endogenous ligand of the opioid OP4 receptor, and of two cannabinoid receptor agonists WIN 55,212-2 and CP-55,940 (0.001-1 micromol/kg each) on the neurogenic tachycardia and bradycardia in pithed rats. Electrical stimulation (1 Hz, 1 ms, 50 V for 10 s) of the preganglionic sympathetic nerve fibres and injection of nicotine 2 micromol/kg or isoprenaline 0.5 nmol/kg increased heart rate by about 70 beats/min (bpm) in pithed rats pretreated with atropine 1.5-2 micromol/kg. The electrically induced tachycardia was reduced dose dependently by nociceptin, WIN 55,212-2 and CP-55,940 (by 60, 30 and 20% at the highest dose, respectively). The OP4 and cannabinoid receptor agonists diminished the nicotine- but not the isoprenaline-stimulated increase in heart rate. In pithed rats pretreated with propranolol 3 micromol/kg, vagal stimulation (5 Hz, 1 ms, 15 V for 10 s) or injection of methacholine (5-10 nmol/kg) decreased heart rate by about 30 bpm. Nociceptin, but not WIN 55,212-2 or CP-55,940 decreased the vagal bradycardia dose dependently (the inhibitory effect of 1 micromol/kg was about 40%). Nociceptin failed to modify the methacholine-induced decrease in heart rate.
3.[Phe1psi(CH2-NH)Gly2]nociceptin-(1-13)-NH2 acts as an agonist of the orphanin FQ/nociceptin receptor in vivo.
Grisel JE;Farrier DE;Wilson SG;Mogil JS Eur J Pharmacol. 1998 Sep 11;357(1):R1-3.
The orphanin FQ/nociceptin (OFQ/N) derivative peptide, [Phe1psi(CH2-NH)Gly2] nociceptin-(1-13)-NH2 (Phe(psi)), has been claimed to be both an antagonist and an agonist of the orphan opioid receptor (ORL1) in different in vitro assays. We now report the dose-dependent inhibition of morphine analgesia by Phe(psi) in mice, an effect parallel to that of OFQ/N. Further, the anti-opioid actions of OFQ/N are not blocked by Phe(psi). Thus, Phe(psi) acts as an ORL1 receptor agonist, not an antagonist, in vivo.
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CAS 213130-17-7 [Phe1Ψ(CH2-NH)Gly2]Nociceptin(1-13)NH2

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