Substance P 7-11
目录号 : GC37698
Substance P (7-11) 是神经肽物质P的C-末端片段，其可引起细胞内钙浓度的增加。
Cas No.:51165-05-0
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
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- Purity: >98.00%
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Cell experiment: | Confluent chondrocytes are incubated for 24 h with SP or Substance P (7-11). TIMP activity is inactivated following reduction and alkylation with 2 mM dithiothreitol and 5 mM iodoacetamide for 30 min at 37°C. Samples are subsequently dialysed. Latent collagenase is activated with 1 mM APt followed by inactivation with soy bean trypsin inhibitor. Collagenase is measured[1]. |
References: [1]. Halliday DA, et al. The substance P fragment SP-(7-11) increases prostaglandin E2, intracellular Ca2+ and collagenase production in bovine articular chondrocytes. Biochem J. 1993 May 15;292 ( Pt 1):57-62. | |
Substance P (7-11) is a C-terminal fragment of Substance P which can cause an increase in the intracellular calcium concentration.
Substance P (7-11) increases PGE2 and collagenase production at concentrations greater than 1 μM. Substance P (7-11), but not intact SP, SP-(1-4), SP-(1-6), SP- (8-11) or SP-(9-1 1), nor the tachykinins NKA and NKB, causes an increase in the intracellular calcium concentration as measured by the fluorescent dye Fura-2. The maximal change in intracellular calcium induced by 10 μM Substance P (7-11) was 140±30 nM[1].
[1]. Halliday DA, et al. The substance P fragment SP-(7-11) increases prostaglandin E2, intracellular Ca2+ and collagenase production in bovine articular chondrocytes. Biochem J. 1993 May 15;292 ( Pt 1):57-62.
| Cas No. | 51165-05-0 | SDF | |
| 分子式 | C31H44N6O5S | 分子量 | 612.78 |
| 溶解度 | Soluble in DMSO | 储存条件 | Store at -20°C |
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.6319 mL | 8.1595 mL | 16.3191 mL |
| 5 mM | 0.3264 mL | 1.6319 mL | 3.2638 mL |
| 10 mM | 0.1632 mL | 0.816 mL | 1.6319 mL |
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The Substance P fragment SP-(7-11) increases prostaglandin E2, intracellular Ca2+ and collagenase production in bovine articular chondrocytes
Biochem J 1993 May 15;292 ( Pt 1)(Pt 1):57-62.PMID:7684899DOI:10.1042/bj2920057.
Substance P (SP) is found in increased concentrations in inflamed joints and is believed to play a role in joint pathology. Culture of bovine articular chondrocytes with SP or with the related mammalian tachykinins neurokinin A or B (NKA or NKB) produced no effect on prostaglandin E2 (PGE2) or collagenase production. However, the C-terminal fragment of SP, SP-(7-11), increased PGE2 and collagenase production at concentrations greater than 1 microM. The N-terminal fragments SP-(1-4) and SP-(1-6) had no effect on PGE2 or collagenase production. In addition, SP-(7-11), but not intact SP, SP-(1-4), SP-(1-6), SP-(8-11) or SP-(9-11), nor the tachykinins NKA and NKB, caused an increase in the intracellular calcium concentration as measured by the fluorescent dye Fura-2. The maximal change in intra-cellular calcium induced by 10 microM SP-(7-11) was 140 +/- 30 nM. We postulate that cleavage of SP by neutral endopeptidases which are present in the synovial fluid and which yield SP-(7-11) may be of biological importance in chondrocyte-mediated cartilage pathology.
Anxiogenic effects of Substance P and its 7-11 C terminal, but not the 1-7 N terminal, injected into the dorsal periaqueductal gray
Peptides 1999 Dec;20(12):1437-43.PMID:10698119DOI:10.1016/s0196-9781(99)00154-0.
The dorsal periaqueductal gray matter (DPAG) is one of the main output regions of the brainstem for the expression of defense reaction. Recent findings implicating neurokinins in the expression of fear or anxiety-like behaviors, have stimulated interest in the participation of these neuropeptides in the generation of aversive states in the dorsal periaqueductal gray matter. Analyses of traditional measures of the behavior of rats submitted to the elevated plus-maze test in this laboratory have shown that microinjections of Substance P (SP) into the DPAG produce anxiogenic-like effects. The present study employs an ethological analysis of the behavior of animals in this test to investigate the involvement of Substance P (SP) and its C- and N- fragments (7-11 and 1-7) in the expression of the different aspects of fear upon injection into the DPAG. To this end, rats were implanted with a cannula in the DPAG and injected one week later with 35 and 70 pmol of either Substance P, or C- or N- SP fragments and tested immediately afterwards in the elevated plus-maze. The results show that SP and its C terminal fragment, produced increases in scanning, stretched attend posture, head dipping and flat-back approach, whereas the fragment N terminal produced only an increase in rearing. Therefore, the effects of SP and its C terminal fragment were associated to risk assessment behavior, whereas those of N terminal fragment were related to vertical exploratory activity. The results indicate that SP produces anxiogenic effects through activation of neural substrates of aversion in the DPAG and that this effect is probably related to its C terminal fragment.
GR 73,632 and [Glu(OBzl)11]substance P are selective agonists for the septide-sensitive tachykinin NK1 receptor in the rat urinary bladder
Neuropeptides 1995 Feb;28(2):99-106.PMID:7538205DOI:10.1016/0143-4179(95)90081-0.
The existence of a septide-sensitive subtype of the tachykinin NK1 receptor has been recently proposed. In the rat isolated urinary bladder, the non-peptide NK1 receptor antagonist RP 67,580 exhibits a higher affinity towards septide (pKB 7.57) than towards [Sar9]substance P sulfone (pKB 7.00). In this study we have investigated the pharmacological profile of the non-mammalian tachykinin physalaemin, of the synthetic NK1 receptor agonist GR 73,632 (delta-aminovaleryl[LPro9,NMeLeu10]Substance P(7-11)) and of [Glu(OBzl)11]substance P in relation to the putative existence of a septide-sensitive receptor. The activity of [Glu(OBzl)11]substance P at the NK1, NK2 and NK3 receptor was assayed in the guinea-pig ileum NK1 receptor assay (EC50 26 nM), in the rabbit pulmonary artery NK2 receptor assay (weak agonist activity) and in the rat portal vein NK3 receptor assays (no appreciable activity up to 1 microM). GR 73,632, [Glu(OBzl)11]substance P and physalaemin, all produced concentration-dependent contractions of the rat isolated urinary bladder, with EC50 values of 17, 79, and 9 nM, respectively. The responses to the three agonists were very slightly or not modified by the NK2 receptor antagonist SR 48,968 (1 microM). RP 67,580 (0.3-3 microM) produced a concentration-dependent rightward shift of the curve to GR 73,632, [Glu(OBzl)11]substance P and physalaemin without producing depression of their maximal response. Schild plot analysis indicated the competitive nature of the antagonism. The affinity (pKB) of RP 67,580 towards physalaemin, GR 73,632 and [Glu(OBzl)11]substance P was 7.12, 7.56 and 7.95, respectively.(ABSTRACT TRUNCATED AT 250 WORDS)
Ava[L-Pro9,N-MeLeu10] Substance P(7-11) (GR 73632) and Sar9, Met(O2)11 increase distention-induced peristalsis through activation of neurokinin-1 receptors on smooth muscle and interstitial cells of cajal
J Pharmacol Exp Ther 2006 Apr;317(1):439-45.PMID:16330493DOI:10.1124/jpet.105.094920.
Substance P is generally considered an excitatory neurotransmitter related to gut motor activity, although an inhibitory influence of neurokinin-1 (NK1) receptor activation on peristalsis has also been reported. With an optimized in vitro method to assess distention-induced peristalsis, our aim was to clarify the effect of NK1 receptor activation on peristaltic activity and to reveal the mechanisms by which NK1 activation alters peristalsis. Distention of the small intestine of the mouse and guinea pig induced periodic occurrence of rhythmic waves of propagating rings of circular muscle contraction, associated with slow waves and superimposed action potentials, that propelled intestinal contents aborally. Activation of NK1 receptors by Ava[l-Pro(9),N-MeLeu10] Substance P(7-11) (GR 73632) and Sar(9), Met(O(2))(11) on smooth muscle cells resulted in prolongation of the activity periods and increased action potential generation occurring superimposed on the intestinal slow wave activity. Activation of NK1 receptors on interstitial cells of Cajal resulted in an increase in slow wave frequency. Slow wave amplitude increased, likely by increased cell-to-cell coupling. The NK1 antagonist (S)-1-(2-[3-(3,4-dichlorophenyl)-1-(3-isopropoxyphenylacetyl)piperidin-3-yl]ethyl)-4-phenyl-1-azoniabicyclo[2.2.2]octane chloride (SR 140333) induced a decrease in the slow wave frequency and duration of the activity periods evoked by distention, which makes it likely that NK1 receptor activation plays a role in the normal physiological distention-induced generation of peristaltic motor patterns. In summary, NK1 receptors play a role in normal development of peristalsis and NK1 receptor activation markedly increases propulsive peristaltic contractile activity.
High affinity binding of [3H]propionyl-[Met(O2)11]Substance P(7-11), a tritiated septide-like peptide, in Chinese hamster ovary cells expressing human neurokinin-1 receptors and in rat submandibular glands
Mol Pharmacol 1997 Jul;52(1):120-7.PMID:9224821DOI:10.1124/mol.52.1.120.
Propionyl-[Met(O2)11]Substance P(7-11) [ALIE-124 or propionyl-[Met(O2)11]SP(7-11)] has been designed as a septide-like ligand adequate for tritiation and, therefore, adequate for binding studies. In Chinese hamster ovary (CHO) cells expressing human tachykinin neurokinin (NK)-1 receptors, ALIE-124 displaced [3H][Pro9]substance P (SP) from its binding site at micromolar concentrations. However, ALIE-124 stimulated phosphatidylinositol hydrolysis, as previously shown for septide-like peptides. With [3H]ALIE-124 (95 Ci/mmol), we have been able to reveal a high affinity binding site in CHO cells (Kd = 6.6 +/- 1.0 nM), with a low maximal binding capacity. [3H]ALIE-124 specific maximal binding represented only 15-20% of that observed with [3H][Pro9]SP in CHO cells. Septide-like peptides, including septide and NKA, were potent competitors (in the nanomolar range) of [3H]ALIE-124 specific binding site. Interestingly, SP and [Pro9]SP were also potent competitors, with 10-fold greater potency for sites labeled with [3H]ALIE-124 than for sites labeled with [3H][Pro9]SP. The NK-1 antagonist RP 67580 also showed a higher potency for [3H]ALIE-124 than for [3H][Pro9]SP-specific binding sites. NKB and [Lys5,methyl-Leu9,Nle10]NKA(4-10) displaced [3H]ALIE-124 binding but with lower potency, whereas senktide had no affinity. The existence of [3H]ALIE-124 specific binding sites was also demonstrated in rat submandibular gland. In this tissue, [3H]ALIE-124 specific maximal binding was higher, reaching 40-50% of that achieved with [3H][Pro9]SP.