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Submit Review(E)-Capsaicin is a prototypic vanilloid receptor agonist (pEC50 values are 7.97 and 7.10 at rat and human VR1 receptors respectively). Excites a subset of primary afferent sensory neurons, with subsequent antinociceptive and anti-inflammatory effects. Reversibly inhibits aggregation of platelets.
分子量 | 305.42 |
公式 | C18H27NO3 |
储存 | Store at RT |
纯度 | ≥98% (HPLC) |
CAS Number | 404-86-4 |
PubChem ID | 1548943 |
InChI Key | YKPUWZUDDOIDPM-SOFGYWHQSA-N |
Smiles | COC1=C(O)C=CC(CNC(=O)CCCC\C=C\C(C)C)=C1 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 15.27 | 50 | |
ethanol | 15.27 | 50 |
以下数据基于产品分子量 305.42。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
0.5 mM | 6.55 mL | 32.74 mL | 65.48 mL |
2.5 mM | 1.31 mL | 6.55 mL | 13.1 mL |
5 mM | 0.65 mL | 3.27 mL | 6.55 mL |
25 mM | 0.13 mL | 0.65 mL | 1.31 mL |
参考文献是支持产品生物活性的出版物。
Bevan and Szolcsani (1990) Sensory neuron-specific actions of capsaicin: mechanisms and application. TiPS 11 330 PMID: 2203194
Hogaboam and Wallace (1991) Inhibition of platelet aggregation by capsaicin. An effect unrelated to actions on sensory afferent neurons. Eur.J.Pharmacol. 202 129 PMID: 1786800
Holzer (1991) Capsaicin-cellular targets, mechanism of actions, and selectivity for thin sensory neurons. Pharmacol.Rev. 43 143 PMID: 1852779
Ralevic et al (2001) Cannabinoid activation of recombinant and endogenous vanilloid receptors. Eur.J.Pharmacol. 424 211 PMID: 11672565
If you know of a relevant reference for (E)-Capsaicin, please let us know.
关键词: (E)-Capsaicin, (E)-Capsaicin supplier, Prototypic, vanilloid, receptor, agonists, Vanillioid, Receptors, VR1, TRPV, TRP, Channels, Transient, Receptor, Potential, 0462, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 (E)-Capsaicin 的部分引用包括:
Fairless et al (2013) Membrane potential measurements of isolated neurons using a voltage-sensitive dye. PLoS One 8 e58260 PMID: 23516458
Bhaskaran and Smith (2010) Effects of TRPV1 activation on synaptic excitation in the dentate gyrus of a mouse model of temporal lobe epilepsy. World J Gastroenterol 223 529 PMID: 20144892
Ahern et al (2005) Extracellular cations sensitize and gate capsaicin receptor TRPV1 modulating pain signaling. J Neurosci 25 5109 PMID: 15917451
Buznikov et al (2010) A putative 'pre-nervous' endocannabinoid system in early echinoderm development. Dev Neurosci 32 1 PMID: 19907129
Pitcher et al (2007) Spinal NKCC1 blockade inhibits TRPV1-dependent referred allodynia. J Pharmacol Exp Ther 3 17 PMID: 17603899
Diniz et al (2019) Dual mechanism of TRKB activation by anandamide through CB1 and TRPV1 receptors. PeerJ 7 e6493 PMID: 30809460
Chen et al (2016) Spatial Distribution of the Cannabinoid Type 1 and Capsaicin Receptors May Contribute to the Complexity of Their Crosstalk. Sci Rep 6 33307 PMID: 27653550
Khatibi et al (2011) Capsaicin pre-treatment provides neurovascular protection against neonatal hypoxic-ischemic brain injury in rats. Mol Pain 111 225 PMID: 21725760
Martínez-García et al (2011) Increase of capsaicin-induced trigeminal Fos-like immunoreactivity by 5-HT(7) receptors. Cardiovasc Res 51 1511 PMID: 22082421
Zsombok et al (2011) Functional plasticity of central TRPV1 receptors in brainstem dorsal vagal complex circuits of streptozotocin-treated hyperglycemic mice. Exp Neurol 31 14024 PMID: 21957263
Westlund et al (2010) Impact of central and peripheral TRPV1 and ROS levels on proinflammatory mediators and nociceptive behavior. Proc Natl Acad Sci U S A 6 46 PMID: 20691059
Ma et al (2015) Experimental evidence for alleviating nociceptive hypersensitivity by single application of capsaicin. Mol Pain 11 22 PMID: 25896608
Chiu et al (2013) Bacteria activate sensory neurons that modulate pain and inflammation. World J Gastroenterol 501 52 PMID: 23965627
Shabir et al (2013) Functional expression of purinergic P2 receptors and transient receptor potential channels by the human urothelium. Diabetes 305 F396 PMID: 23720349
Gao et al (2012) Transient receptor potential vanilloid type 1-dependent regulation of liver-related neurons in the paraventricular nucleus of the hypothalamus diminished in the type 1 diabetic mouse. Acta Neurochir Suppl 61 1381 PMID: 22492526
Rossi et al (2014) Interleukin-1β causes excitotoxic neurodegeneration and multiple sclerosis disease progression by activating the apoptotic protein p53. Mol Neurodegener 9 56 PMID: 25495224
Wang et al (2014) Innervation of enteric mast cells by primary spinal afferents in guinea pig and human small intestine. Am J Physiol Gastrointest Liver Physiol 307 G719 PMID: 25147231
Nguyen et al (2014) Transient receptor potential vanilloid type 1 channel may modulate opioid reward. Neuropsychopharmacology 39 2414 PMID: 24732880
Gibson et al (2008) TRPV1 channels mediate long-term depression at synapses on hippocampal interneurons. Neuron 57 746 PMID: 18341994
Balleza-Tapia et al (2018) TrpV1 receptor activation rescues neuronal function and network gamma oscillations from Aβ-induced impairment in mouse hippocampus in vitro. Elife 7 PMID: 30417826
Hartley et al (2013) Development and experimental application of an HPLC procedure for the determination of capsaicin and dihydrocapsaicin in serum samples from human subjects. Indian J Clin Biochem 28 329 PMID: 24426233
Nesuashvili et al (2013) Sensory nerve terminal mitochondrial dysfunction activates airway sensory nerves via transient receptor potential (TRP) channels. Mol Pharmacol 83 1007 PMID: 23444014
Benninger et al (2008) Control of excitatory synaptic transmission by capsaicin is unaltered in TRPV1 vanilloid receptor knockout mice. Br J Pharmacol 52 89 PMID: 17651868
Chen et al (2014) Antinociceptive effects of novel melatonin receptor agonists in mouse models of abdominal pain. Mol Pain 20 1298 PMID: 24574803
Nash et al (2012) 7-tert-Butyl-6-(4-chloro-phenyl)-2-thioxo-2,3-dihydro-1H-pyrido[2,3-d]pyrimidin-4-one, a classic polymodal inhibitor of transient receptor potential vanilloid type 1 with a reduced liability for hyperthermia, is analgesic and ameliorates visceral hypersen J Pharmacol Exp Ther 342 389 PMID: 22566669
Smart et al (2002) 'Entourage' effects of N-acyl ethanolamines at human vanilloid receptors. Comparison of effects upon anandamide-induced vanilloid receptor activation and upon anandamide metabolism. Headache 136 452 PMID: 12023948
Izzo et al (2001) Effect of vanilloid drugs on gastrointestinal transit in mice. Br J Pharmacol 132 1411 PMID: 11264233
Craib et al (2001) A possible role of lipoxygenase in the activation of vanilloid receptors by anandamide in the guinea-pig bronchus. Neurochem Int 134 42581 PMID: 11522594
Shi et al (2015) Alterations in serotonin, transient receptor potential channels and protease-activated receptors in rats with irritable bowel syndrome attenuated by Shugan decoction. Front Cell Neurosci 21 4852 PMID: 25944998
Zakharov et al (2015) Hunting for origins of migraine pain: cluster analysis of spontaneous and capsaicin-induced firing in meningeal trigeminal nerve fibers. J Transl Med 9 287 PMID: 26283923
Wang et al (2015) Mother root of Aconitum carmichaelii Debeaux exerts antinociceptive effect in Complet Freund's Adjuvant-induced mice: roles of dynorpin/κ-opioid system and transient receptor potential vanilloid type-1 ion channel. PLoS One 13 284 PMID: 26320055
Chen et al (2015) Berberine Improves Intestinal Motility and Visceral Pain in the Mouse Models Mimicking Diarrhea-Predominant Irritable Bowel Syndrome (IBS-D) Symptoms in an Opioid-Receptor Dependent Manner. Nature 10 e0145556 PMID: 26700862
Stanley et al (2015) Cannabidiol causes endothelium-dependent vasorelaxation of human mesenteric arteries via CB1 activation. Neuropsychopharmacology 107 568 PMID: 26092099
Cobellis et al (2010) A gradient of 2-arachidonoylglycerol regulates mouse epididymal sperm cell start-up. Biol Reprod 82 451 PMID: 19812302
Bautista et al (2005) Pungent products from garlic activate the sensory ion channel TRPA1. Br J Pharmacol 102 12248 PMID: 16103371
Bang et al (2004) Neurokinin-1 receptor antagonists protect mice from CD95- and tumor necrosis factor-α-mediated apoptotic liver damage. J Neurosci 308 1174 PMID: 14617692
Melis et al (2004) Endocannabinoids mediate presynaptic inhibition of glutamatergic transmission in rat ventral tegmental area DA neurons through activation of CB1 receptors. J Neurosci 24 53 PMID: 14715937
Yissachar et al (2017) An Intestinal Organ Culture System Uncovers a Role for the Nervous System in Microbe-Immune Crosstalk. Cell 168 1135 PMID: 28262351
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