托肽品 Q
| 中文名称 | 托肽品 Q |
|---|---|
| 中文同义词 | 托肽品 Q;托肽品 QT;TERTIAPIN Q|||TERTIAPINQ;化合物 TERTIAPIN-Q |
| 英文名称 | Tertiapin Q |
| 英文同义词 | Teriapin Q;L-Lysinamide, L-alanyl-L-leucyl-L-cysteinyl-L-asparaginyl-L-cysteinyl-L-asparaginyl-L-arginyl-L-isoleucyl-L-isoleucyl-L-isoleucyl-L-prolyl-L-histidyl-L-glutaminyl-L-cysteinyl-L-tryptophyl-L-lysyl-L-lysyl-L-cysteinylglycyl-L-lysyl-, cyclic (3→14),(5→18)-bis(disulfide);Tertiapin-Q TFA |
| CAS号 | 910044-56-3 |
| 分子式 | C106H175N35O24S4 |
| 分子量 | 2452.01 |
| EINECS号 | |
| 相关类别 | 多肽中间体 |
| Mol文件 | 910044-56-3.mol |
| 结构式 |  |
托肽品 Q 性质
| 密度 | 1.51±0.1 g/cm3(Predicted) |
|---|---|
| 储存条件 | -20°C |
| 形态 | 固体 |
| 颜色 | 白色至米白色 |
| 水溶解性 | Soluble in water (2mg/ml) |
| 序列 | Ala-Leu-Cys-Asn-Cys-Asn-Arg-Ile-Ile-Ile-Pro-His-Gln-Cys-Trp-Lys-Lys-Cys-Gly-Lys-Lys-NH2 (Disulfide bridge: Cys3-Cys14, Cys5-Cys18) |
Potassium channel
Tertiapin-Q is a highly selective blocker of G protein-coupled inwardly rectifying potassium (GIRK1/4) heterodimer and renal outer medullary potassium channel (ROMK1, Kir 1.1 ). Tertiapin-Q is a potent and selective blocker for Kir 1.1 renal outer medullary potassium, Kir 3.1 -Kir 3.4 channels and calcium activated large conductance potassium channels (big potassium channels). The somatostatin (SS-14)-activated current is almost completely blocked (93.2±2.9%, n=5; P<0.01) by preincubation with the G protein-coupled inwardly rectifying potassium (GIRK) channel blocker Tertiapin-Q (TPN-Q).
Tertiapin-Q is a muscarinic acetylcholine receptor-operated K + current (I K,Ach ) blocker. After the cessation of rapid atrial pacing, the atrial effective refractory period (AERP) is unchanged during the experimental period in the rapid atrial pacing (RAP) rabbits (n=6). Bepridil (1 mg/kg, n=5 for each group), Amiodarone (10 mg/kg, n=5 for each group), Vernakalant (3 mg/kg, n=5 for each group), Ranolazine (10 mg/kg, n=6 for each group) or Tertiapin-Q (0.03 mg/kg, n=5 for each group) on the AERP in the control and RAP rabbits. Tertiapin-Q significantly prolongs the AERP at each pacing cycle length both in the control and RAP rabbits. The extents of prolonging effect of Tertiapin-Q on the AERP in the RAP rabbits are greater than those in the control animals.