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Nocistatin (bovine)

Opposes action of nociceptin CAS# 208253-85-4

Nocistatin (bovine)

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Chemical structure

Nocistatin (bovine)

3D structure

Chemical Properties of Nocistatin (bovine)

Cas No. 208253-85-4 SDF Download SDF
PubChem ID 24868191 Appearance Powder
Formula C82H135N21O32 M.Wt 1927.07
Type of Compound N/A Storage Desiccate at -20°C
Solubility Soluble to 2 mg/ml in PBS
Sequence TEPGLEEVGEIEQKQLQ
SMILES CCC(C)C(C(=O)NC(CCC(=O)O)C(=O)NC(CCC(=O)N)C(=O)NC(CCCCN)C(=O)NC(CCC(=O)N)C(=O)NC(CC(C)C)C(=O)NC(CCC(=O)N)C(=O)O)NC(=O)C(CCC(=O)O)NC(=O)CNC(=O)C(C(C)C)NC(=O)C(CCC(=O)O)NC(=O)C(CCC(=O)O)NC(=O)C(CC(C)C)NC(=O)CNC(=O)C1CCCN1C(=O)C(CCC(=O)O)NC(=O)C(C(C)O)N
Standard InChIKey GUPWDFZVRDNEEX-GFTPUIGSSA-N
Standard InChI InChI=1S/C82H135N21O32/c1-10-41(8)67(80(132)97-48(21-29-62(114)115)71(123)94-45(16-24-55(84)105)69(121)92-43(14-11-12-32-83)68(120)93-46(17-25-56(85)106)72(124)100-53(35-39(4)5)76(128)99-51(82(134)135)18-26-57(86)107)102-73(125)44(19-27-60(110)111)90-58(108)37-89-79(131)66(40(6)7)101-74(126)49(22-30-63(116)117)95-70(122)47(20-28-61(112)113)96-75(127)52(34-38(2)3)91-59(109)36-88-77(129)54-15-13-33-103(54)81(133)50(23-31-64(118)119)98-78(130)65(87)42(9)104/h38-54,65-67,104H,10-37,83,87H2,1-9H3,(H2,84,105)(H2,85,106)(H2,86,107)(H,88,129)(H,89,131)(H,90,108)(H,91,109)(H,92,121)(H,93,120)(H,94,123)(H,95,122)(H,96,127)(H,97,132)(H,98,130)(H,99,128)(H,100,124)(H,101,126)(H,102,125)(H,110,111)(H,112,113)(H,114,115)(H,116,117)(H,118,119)(H,134,135)/t41-,42+,43-,44-,45-,46-,47-,48-,49-,50-,51-,52-,53-,54-,65-,66-,67-/m0/s1
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
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Biological Activity of Nocistatin (bovine)

DescriptionAn endogenous peptide derived from the same precursor as nociceptin, which is able to block nociceptin-induced allodynia and hyperalgesia and may play an opposing role in pain transmission. Shown to reverse nociceptin inhibition of glutamate release from rat brain slices; also modulates 5-HT transmission in the mouse neocortex via mechanisms separate from nociceptin/orphanin FQ.

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References on Nocistatin (bovine)

Nocistatin inhibits 5-hydroxytryptamine release in the mouse neocortex via presynaptic Gi/o protein linked pathways.[Pubmed:17618307]

Br J Pharmacol. 2007 Oct;152(4):549-55.

BACKGROUND AND PURPOSE: Nocistatin (NST) is a neuropeptide generated from cleavage of the nociceptin/orphanin FQ (N/OFQ) precursor. Evidence has been presented that NST acts as a functional antagonist of N/OFQ, although NST receptor and transduction pathways have not yet been identified. We previously showed that N/OFQ inhibited [(3)H]5-hydroxytryptamine ([(3)H]5-HT) release from mouse cortical synaptosomes via activation of NOP receptors. We now investigate whether NST regulates [(3)H]5-HT release in the same preparation. EXPERIMENTAL APPROACH: Mouse and rat cerebrocortical synaptosomes in superfusion, preloaded with [(3)H]5-HT and stimulated with 1 min pulses of 10 mM KCl, were used. KEY RESULTS: Bovine NST (b-NST) inhibited the K(+)-induced [(3)H]5-HT release, displaying similar efficacy but lower potency than N/OFQ. b-NST action underwent concentration-dependent and time-dependent desensitization, and was not prevented either by the NOP receptor antagonist [Nphe(1) Arg(14),Lys(15)]N/OFQ(1-13)-NH(2) (UFP-101) or by the non-selective opioid receptor antagonist, naloxone. Contrary to N/OFQ, b-NST reduced [(3)H]5-HT release from synaptosomes obtained from NOP receptor knockout mice. However, both N/OFQ and NST were ineffective in synaptosomes pre-treated with the G(i/o) protein inhibitor, Pertussis toxin. NST-N/OFQ interactions were also investigated. Co-application of maximal concentrations of both peptides did not result in additive effects, whereas pre-application of maximal b-NST concentrations partially attenuated N/OFQ inhibition. CONCLUSIONS AND IMPLICATIONS: We conclude that b-NST inhibits [(3)H]5-HT release via activation of G(i/o) protein linked pathways, not involving classical opioid receptors and the NOP receptor. The present data strengthen the view that b-NST is, per se, a biologically active peptide endowed with agonist activity.

Effect of nocistatin and its interaction with nociceptin/orphanin FQ on the rat formalin test.[Pubmed:10218885]

Neurosci Lett. 1999 Mar 12;262(3):179-82.

Nocistatin is a 17 amino acid peptide and is processed from prepronociceptin. Nocistatin does not bind to the nociceptin receptor, but nocistatin blocks allodynia induced by nociceptin/orphanin FQ. In this study, we examined the effect of intrathecal nocistatin and its interaction with nociceptin/orphanin FQ in the rat formalin test and the hot plate test. Intrathecal nocistatin attenuated the formalin induced phase 1, but not phase 2, flinching behavior. Coadministration of nocistatin with nociceptin/orphanin FQ did not block the analgesic effect of nociceptin/orphanin FQ. Nocistatin had no effect on the hot plate test. These data suggest that nocistatin produces analgesic effect in the formalin test, but not in the hot plate test, and that the mechanisms underlying the analgesic effect of nocistatin is complex.

Nocistatin reverses nociceptin inhibition of glutamate release from rat brain slices.[Pubmed:9774260]

Eur J Pharmacol. 1998 Sep 4;356(2-3):R1-3.

We have examined the effects of the recently described heptadecapeptide nocistatin on K+-evoked glutamate release from rat cerebrocortical slices in vitro. In vivo, nocistatin reverses the action of nociceptin. Nocistatin (100 nM, n = 7) did not inhibit K+-evoked glutamate release alone. Nociceptin (100 nM) inhibited glutamate release by 51.7 +/- 8.3% (P < 0.05, n = 6) and this was fully reversed by nocistatin (100 nM). Nocistatin also appears to be an antagonist of nociceptin action in vitro.

Nocistatin, a peptide that blocks nociceptin action in pain transmission.[Pubmed:9521323]

Nature. 1998 Mar 19;392(6673):286-9.

Prolonged tissue damage or injury often leads to chronic pain states such that noxious stimuli evoke hyperalgesia and innocuous tactile stimuli evoke pain (allodynia). The neuropeptide nociceptin, also known as orphanin FQ, is an endogenous ligand for the orphan opioid-like receptor which induces both hyperalgesia and allodynia when administered by injection through the theca of the spinal cord into the subarachnoid space (that is, intrathecally). Here we show that the nociceptin precursor contains another biologically active peptide which we call nocistatin. Nocistatin blocks nociceptin-induced allodynia and hyperalgesia, and attenuates pain evoked by prostaglandin E2. It is the carboxy-terminal hexapeptide of nocistatin (Glu-Gln-Lys-Gln-Leu-Gln), which is conserved in bovine, human and murine species, that possesses allodynia-blocking activity. We have also isolated endogenous nocistatin from bovine brain. Furthermore, intrathecal pretreatment with anti-nocistatin antibody decreases the threshold for nociceptin-induced allodynia. Although nocistatin does not bind to the nociceptin receptor, it binds to the membrane of mouse brain and of spinal cord with high affinity. Our results show that nocistatin is a new biologically active peptide produced from the same precursor as nociceptin and indicate that these two peptides may play opposite roles in pain transmission.

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