Senazodan (MCI 154) (hydrochloride), as a Ca sensitiser, shows inhibition effect on PDE III.
IC50&Target
PDE III
体外研究
Senazodan (hydrochloride) seems to affect directly the actin-myosin crossbridge kinetics, and increases myosin ATPase activity. Senazodan (hydrochloride) produces a concentration-dependent increase in tension development. Senazodan (hydrochloride) enhances Ca binding to myofilaments and to purified cardiac troponin C. Senazodan (hydrochloride) also enhances contractility in guinea-pig papillary muscles by inhibiting PDE III.Senazodan (0.1 nM~0.1 mM) (hydrochloride) shows that the contractile response of superior mesenteric arterie (SMA) to norepinephrine (NE) after hemorrhagic shock is significantly decreased as compared with the normal control group. Senazodan (0.01 mM) (hydrochloride) pretreatment prevents the effects of Ang II, and the concentration-response curve of Ca is shifted to the right as compared with Ang II-alone group.
体内研究
Senazodan (0.1~2.0 mg/kg; left femoral vein catheterization infusion) (hydrochloride) decreases the pressor effect of norepinephrine (NE).
Senazodan (0.1 mg/kg; i.v.) (hydrochloride) makes LVSP, IP, MC, and Lo all increased significantly, while heart rate is not obviously changed and left ventricular end-diastolic pressure (LVEDP) is reduced remarkably.
Animal Model:
Wistar rats (200~250 g)
Dosage:
0.1~2.0 mg/kg
Administration:
Left femoral vein catheterization infusion
Result:
Decreased the pressor effect of norepinephrine (NE).
Animal Model:
Rabbits
Dosage:
0.1 mg/kg
Administration:
I.v.
Result:
LVSP, IP, MC, and Lo all were increased significantly while heart rate was not obviously changed and left ventricular end-diastolic pressure (LVEDP) was reduced remarkably.
分子式
C15H15ClN4O
分子量
302.76
CAS号
98326-33-1
中文名称
司那佐旦(盐酸盐)
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, sealed storage, away from moisture and light
*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
溶解性数据
In Vitro:
DMSO : 50 mg/mL (165.15 mM; Need ultrasonic)
配制储备液
浓度溶剂体积质量
1 mg
5 mg
10 mg
1 mM
3.3029 mL
16.5147 mL
33.0295 mL
5 mM
0.6606 mL
3.3029 mL
6.6059 mL
10 mM
0.3303 mL
1.6515 mL
3.3029 mL
*
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
In Vivo:
请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂: