[Phe1Ψ(CH2-NH)Gly2]Nociceptin(1-13)NH2
![Cat.No. 1092 - [Phe1Psi(CH2-NH)Gly2]Nociceptin(1-13)NH2 | Phe(Ψ(CH2-NH))-Gly-Gly-Phe-Thr-Gly-Ala-Arg-Lys-Ser-Ala-Arg-Lys-NH2 | CAS No. 213130-17-7](http://resources.tocris.com/images/datasheets/structures/phe1-psich2-nhgly2nociceptin1-13nh2_1092.png "Cat.No. 1092 - [Phe1Psi(CH2-NH)Gly2]Nociceptin(1-13)NH2 | Phe(Ψ(CH2-NH))-Gly-Gly-Phe-Thr-Gly-Ala-Arg-Lys-Ser-Ala-Arg-Lys-NH2 | CAS No. 213130-17-7")
Biological Activity
Potent agonist of the nociceptin (ORL1) receptor, demonstrated both in vitro and in vivo. 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).
Technical Data
| M. Wt | 1367.6 |
| Formula | C61H102N22O14 |
| Sequence |
FGGFTGARKSARK (Modifications: Phe-1 - Gly-2 peptide bond replace with Psi-(CH2-NH), Lys-13 = C-terminal amide) |
| Storage | Desiccate at -20°C |
| CAS Number | 213130-17-7 |
| PubChem ID | 6324602 |
| InChI Key | ZHKMSRDIVOXQKP-YILJZHMHSA-N |
| Smiles | [H]N[C@H](CNCC(=O)NCC(=O)N[C@@H](CC1=CC=CC=C1)C(=O)N[C@@H]([C@@H](C)O)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCCCN)C(N)=O)CC1=CC=CC=C1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solubility | Soluble to 0.70 mg/ml in water |
Preparing Stock Solutions
The following data is based on the product molecular weight 1367.6. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 0.73 mL | 3.66 mL | 7.31 mL |
| 5 mM | 0.15 mL | 0.73 mL | 1.46 mL |
| 10 mM | 0.07 mL | 0.37 mL | 0.73 mL |
| 50 mM | 0.01 mL | 0.07 mL | 0.15 mL |
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References
References are publications that support the products' biological activity.
Guerrini et al (1997) Address and message sequences for the nociceptin receptor: a structure-activity study of nociceptin (1-13)-peptide amide. J.Med.Chem. 40 1789 PMID: 9191955
Guerrini et al (1998) A new selective antagonist of the nociceptin receptor. Br.J.Pharmacol. 123 163 PMID: 9489602
Okawa et al (1999) Comparison of the effects of [Phe1ω(CH2-NH)Gly2-nociceptin-(1-13)NH2 in rat brain, rat vas deferens and CHO cells expressing recombinant human nociceptin receptors. Br.J.Pharmacol. 127 123 PMID: 10369464
Xu et al (1998) [Phe1ω(CH2-NH)Gly2-nociceptin-(1-13)NH2, a proposed antagonist of the nociceptin receptor, is a potent and stable agonist in the rat spinal cord. Neurosci.Lett. 249 127 PMID: 9682833
If you know of a relevant reference for [Phe1Ψ(CH2-NH)Gly2]Nociceptin(1-13)NH2, please let us know.
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Keywords: Selective nociceptin agonists Receptors ORL1 OP4 NOP Opioid [Phe1Psi(CH2-NH)Gly2]Nociceptin(1-13)NH2 NOP Receptors
1 Citation for [Phe1Ψ(CH2-NH)Gly2]Nociceptin(1-13)NH2
Citations are publications that use Tocris products. Selected citations for [Phe1Ψ(CH2-NH)Gly2]Nociceptin(1-13)NH2 include:
McLeod et al (2001) Nociceptin inhibits cough in the guinea-pig by activation of ORL(1) receptors. J Biol Chem 132 1175 PMID: 11250866
Do you know of a great paper that uses [Phe1Ψ(CH2-NH)Gly2]Nociceptin(1-13)NH2 from Tocris? If so please let us know.
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