TYR-PRO-TRP-PHE-NH2

生物活性靶点体外研究体内研究 TYR-PRO-TRP-PHE-NH2 试剂级价格

TYR-PRO-TRP-PHE-NH2

CAS号:189388-22-5
英文名:ENDOMORPHIN-1
中文名:TYR-PRO-TRP-PHE-NH2
CBNumber:CB1684104
分子式:C34H38N6O5
分子量:610.7
MOL File:189388-22-5.mol

TYR-PRO-TRP-PHE-NH2化学性质

熔点 :144-146℃
沸点 :1052.8±65.0 °C(Predicted)
密度 :1.343±0.06 g/cm3(Predicted)
RTECS号 :SQ7316800
储存条件 :−20°C
溶解度 :≥14.9 mg/mL in H2O; ≥30.55 mg/mL in DMSO; ≥47 mg/mL in EtOH
酸度系数(pKa) :9.86±0.15(Predicted)
形态 :Solid
颜色 :White to off-white
水溶解性 :Soluble in water
CAS 数据库 :189388-22-5(CAS DataBase Reference)

安全信息

WGK Germany :3

TYR-PRO-TRP-PHE-NH2性质、用途与生产工艺

生物活性 Endomorphin 1，一种高度选择性的高亲和力μ-opioid受体激动剂，对kappa3结合位点具有高亲和力，Ki为 20 到 30 nM 之间。
靶点

Ki: 20-30 nM (kappa ₃ opioid receptor)
体外研究

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.
体内研究

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.