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Merck
CN
所有图片(1)

主要文件

487960

Sigma-Aldrich

Nociceptin

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

别名:

Nociceptin, Orphanin FQ, OFQ, NC, FGGFTGARKSARKLANQ

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About This Item

经验公式（希尔记法）:
C79H129N27O22
CAS号:
170713-75-4
分子量:
1809.04
MDL编号:
MFCD00677528
UNSPSC代码:
12352202
NACRES:
NA.77

质量水平

100

方案

≥98% (HPLC)

表单

lyophilized solid

制造商/商品名称

Calbiochem®

储存条件

OK to freeze
desiccated (hygroscopic)

颜色

white

溶解性

water: 10 mg/mL

运输

ambient

储存温度

−20°C

SMILES字符串

N([C@@H]([C@H](O)C)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCCN\C(=N\[H])\N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN\C(=N\[H])\N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(=O)N)C(=O)N[C@@H](CCC(=O)N)C(=O)O)

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

一般描述

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.

生化/生理作用

Cell permeable: no
Primary Target
Opioid-like G-protein coupled receptor, ORL1 (Opioid Receptor-Like 1)
Product does not compete with ATP.
Reversible: no

警告

Toxicity: Standard Handling (A)

序列

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

其他说明

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.

法律信息

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

储存分类代码

11 - Combustible Solids

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable

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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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