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487960

Nociceptin

Name: Nociceptin
Brand: MM

Endogenous ligand for the opioid-like G-protein coupled receptor, ORL1 (Opioid Receptor-Like 1).

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Synonym(s):

Nociceptin, Orphanin FQ, OFQ, NC, FGGFTGARKSARKLANQ

Empirical Formula (Hill Notation):

C₇₉H₁₂₉N₂₇O₂₂

CAS Number:

170713-75-4

Molecular Weight:

1809.04

MDL number:

MFCD00677528

Quality Level

100

Assay

≥98% (HPLC)

form

lyophilized solid

manufacturer/tradename

Calbiochem^®

storage condition

OK to freeze
desiccated (hygroscopic)

color

white

solubility

water: 10 mg/mL

shipped in

ambient

storage temp.

−20°C

InChI

1S/C79H129N27O22/c1-41(2)33-54(72(122)95-44(5)66(116)103-56(36-59(84)110)73(123)102-53(77(127)128)27-28-58(83)109)104-70(120)49(23-13-15-29-80)100-69(119)52(26-18-32-90-79(87)88)99-65(115)43(4)96-75(125)57(40-107)105-71(121)50(24-14-16-30-81)101-68(118)51(25-17-31-89-78(85)86)98-64(114)42(3)94-61(112)39-93-76(126)63(45(6)108)106-74(124)55(35-47-21-11-8-12-22-47)97-62(113)38-91-60(111)37-92-67(117)48(82)34-46-19-9-7-10-20-46/h7-12,19-22,41-45,48-57,63,107-108H,13-18,23-40,80-82H2,1-6H3,(H2,83,109)(H2,84,110)(H,91,111)(H,92,117)(H,93,126)(H,94,112)(H,95,122)(H,96,125)(H,97,113)(H,98,114)(H,99,115)(H,100,119)(H,101,118)(H,102,123)(H,103,116)(H,104,120)(H,105,121)(H,106,124)(H,127,128)(H4,85,86,89)(H4,87,88,90)/t42-,43-,44-,45+,48-,49-,50-,51-,52-,53-,54-,55-,56-,57-,63-/m0/s1

InChI key

PULGYDLMFSFVBL-SMFNREODSA-N

General description

Endogenous ligand for the opioid-like G-protein coupled receptor, ORL1 (Opioid Receptor-Like 1). Has no significant activity at the µ, δ, or κ opioid receptors; however, nanomolar concentrations of Nociceptin inhibit, forskolin-stimulated adenylyl cyclase activity in cells transfected with the G-protein coupled receptor LC132, which is similar in sequence to the opioid receptor. Also reported to cause hypertension and bradycardia in mice.

Endogenous ligand for the opioid-like G-protein coupled receptor, ORL1 (Opioid Receptor-Like 1). Has no significant activity on the µ, δ, or κ opioid receptors; however, nanomolar concentrations of nociceptin inhibit forskolin-stimulated adenylyl cyclase activity in cells transfected with the G-protein coupled receptor LC132, which is similar in sequence to the opioid receptor. Also reported to cause hypertension and bradycardia in mice.

Biochem/physiol Actions

Cell permeable: no

Primary Target
Opioid-like G-protein coupled receptor, ORL1 (Opioid Receptor-Like 1)

Product does not compete with ATP.

Reversible: no

Warning

Toxicity: Standard Handling (A)

Sequence

H-Phe-Gly-Gly-Phe-Thr-Gly-Ala-Arg-Lys-Ser-Ala-Arg-Lys-Leu-Ala-Asn-Gln-OH

Other Notes

Madeddu, P., et al. 1999. Hypertension 33, 914.
Sandin, J., et al. 1999. NeuroReport 10, 71.
Meunier, J., et al. 1995. Nature 377, 532.
Reinscheid, R.K., et al. 1995. Science 270, 792.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

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Comparison of Pharmacological Properties between the Kappa Opioid Receptor Agonist Nalfurafine and 42B, Its 3-Dehydroxy Analogue: Disconnect between in Vitro Agonist Bias and in Vivo Pharmacological Effects.

Danni Cao et al.

ACS chemical neuroscience, 11(19), 3036-3050 (2020-09-09)

Nalfurafine, a moderately selective kappa opioid receptor (KOR) agonist, is used in Japan for treatment of itch without causing dysphoria or psychotomimesis. Here we characterized the pharmacology of compound 42B, a 3-dehydroxy analogue of nalfurafine and compared with that of

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