Biological Activity
Technical Data
Solubility
Calculators
Datasheets
References
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)
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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Product Datasheets
Certificate of Analysis / Product Datasheet
Safety Datasheet
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References
References are publications that support the products' biological activity.
Guerriniet 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
Guerriniet al (1998) A new selective antagonist of the nociceptin receptor. Br.J.Pharmacol. 123 163 PMID: 9489602
Okawaet 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
Xuet 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