TYR-PRO-TRP-PHE-NH2
中文名稱 | TYR-PRO-TRP-PHE-NH2 |
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中文同義詞 | 內(nèi)嗎啡 1;內(nèi)嗎啡肽 1;內(nèi)嗎啡肽 1、ENDOMORPHIN 1;內(nèi)啡肽-1(醋酸鹽);ENDOMORPHIN-1,MU激動(dòng)劑 |
英文名稱 | ENDOMORPHIN-1 |
英文同義詞 | L-Tyrosyl-L-prolyl-L-tryptophyl-L-phenylalaninamide;H-TYR-PRO-TRP-PHE-NH2;ENDOMORPHIN-1;ENDOMORPHIN-1 (HUMAN, BOVINE);TYR-PRO-TRP-PHE-NH2;YPWF-NH2;L-Phenylalaninamide,L-tyrosyl-L-prolyl-L-tryptophyl-;(2S)-1-[(2S)-2-amino-3-(4-hydroxyphenyl)propanoyl]-N-[(1S)-1-[[(1S)-1-carbamoyl-2-phenyl-ethyl]carbamoyl]-2-(1H-indol-3-yl)ethyl]pyrrolidine-2-carboxamide |
CAS號(hào) | 189388-22-5 |
分子式 | C34H38N6O5 |
分子量 | 610.7 |
EINECS號(hào) | |
相關(guān)類別 | 生物活性小分子;細(xì)胞生物學(xué);多肽;細(xì)胞信號(hào)和神經(jīng)生物學(xué);SignalTransduction;Other Opioid Peptides;Other Opioid PeptidesPeptides for Cell Biology;Opioid receptor and opioid-like receptor;Peptide;Neuropeptides;Opioid Peptides |
Mol文件 | 189388-22-5.mol |
結(jié)構(gòu)式 |
TYR-PRO-TRP-PHE-NH2 性質(zhì)
熔點(diǎn) | 144-146℃ |
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沸點(diǎn) | 1052.8±65.0 °C(Predicted) |
密度 | 1.343±0.06 g/cm3(Predicted) |
RTECS號(hào) | SQ7316800 |
儲(chǔ)存條件 | −20°C |
溶解度 | 水中≥14.9 mg/mL; DMSO 中≥30.55 mg/mL;乙醇中≥47 mg/mL |
酸度系數(shù)(pKa) | 9.86±0.15(Predicted) |
形態(tài) | 固體 |
顏色 | 白色至類白色 |
水溶解性 | Soluble in water |
CAS 數(shù)據(jù)庫(kù) | 189388-22-5(CAS DataBase Reference) |
Ki: 20-30 nM (kappa 3 opioid receptor)
Endomorphin 1 (EM-1) is an endogenous opioid peptide and one of the two Endomorphins. It is a high affinity, highly selective agonist of the μ-opioid receptor, and along with Endomorphin 2 (EM-2). The two Endomorphins display reasonable affinities for kappa 3 binding sites, with K i values between 20 and 30 nM. Endomorphin 1 and Endomorphin 2 compete both μ 1 and μ 2 receptor sites quite potently. Endomorphins have little appreciable affinity for either delta or kappa 1 binding sites, with K i values greater than 500 nM.
Both Endomorphin 1 and Endomorphin 2 are potent analgesics with peak effects seen at 10 and 15 min, respectively. All subsequent studies are performed at peak effect. Both compounds are fully active supraspinally and spinally, with no indication of ceiling effects. Endomorphin 1 is significantly more potent spinally than supraspinally and, at the spinal level, it is significantly more potent than Endomorphin 2. The response of both agents are readily reversed by naloxone. β-FNA, a highly selective μ antagonist, effectively reverses the actions of both Endomorphins. Both Endomorphin 1 and Endomorphin 2 display a profile similar to morphine. Neither compound have analgesic activity in CXBK mice at a dose which produced over 70% analgesia in control CD-1 mice.
安全信息
WGK Germany | 3 |
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提供商 | 語(yǔ)言 |
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英文
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更新日期 | 產(chǎn)品編號(hào) | 產(chǎn)品名稱 | CAS號(hào) | 包裝 | 價(jià)格 |
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2024/11/08 | HY-P0185 | TYR-PRO-TRP-PHE-NH2 Endomorphin 1 | 189388-22-5 | 5mg | 500元 |
2024/11/08 | HY-P0185 | TYR-PRO-TRP-PHE-NH2 Endomorphin 1 | 189388-22-5 | 10mM * 1mLin Water | 672元 |