CAS |
No.75695-93-1 |
中文名称 |
伊拉地平 |
英文名称 |
Isradipine |
别名 |
PN 200-110 |
分子式 |
C19H21N3O5 |
分子量 |
371.39 |
溶解性 |
Soluble in DMSO |
纯度 |
≥98% |
外观(性状) |
Solid |
储存条件 |
Powder:2-8℃,2 years;Insolvent(母液):-20℃,6 months;-80℃,1 year |
EC |
EINECS 630-420-5 |
MDL |
MFCD00153820 |
SMILES |
CC1=C(C(C(=C(N1)C)C(=O)OC(C)C)C2=CC=CC3=NON=C32)C(=O)OC |
InChIKey |
HMJIYCCIJYRONP-UHFFFAOYSA-N |
InChI |
InChI=1S/C19H21N3O5/c1-9(2)26-19(24)15-11(4)20-10(3)14(18(23)25-5)16(15)12-7-6-8-13-17(12)22-27-21-13/h6-9,16,20H,1-5H3 |
PubChem CID |
3784 |
靶点 |
Calcium Channel |
通路 |
Membrane Transporter&Ion Channel;Neuronal Signaling |
背景说明 |
Isradipine是一种L 型钙通道阻滞剂。 |
生物活性 |
Isradipine (PN 200-110) is an orally active L-type calcium channel blocker. Isradipine, as a powerful peripheral vasodilator, is a dihydropyridine calcium antagonist with selective actions on the heart as well as the peripheral circulation. Isradipine is a potentially viable neuroprotective agent for Parkinson's disease[1][2][3]. |
IC50 |
L-type calcium channel[1][2] |
In Vitro |
Isradipine has much higher (>40 fold) affinity for Cav1.3 channels as well as good brain bioavailability. Isradipine has nearly equal potency at Cav1.2 and Cav1.3 channels[1]. |
In Vivo |
Isradipine (0.1~3 mg/kg; p.o.) makes sodium excretion increase in a dose-dependent manner[3].Isradipine pre-treatment reduces 6-hydroxydopamine induced neurotoxicity at the striatal level. Protective effect of isradipine at the striatal level is dose-dependent as shown from 6 mice. Isradipine pre-treatment increases the number of surviving SNc DA cells after 6-hydroxydopamine induced degeneration. Isradipine is capable of protecting striatal dopaminergic terminals and SNc dopaminergic cell bodies against a slow, progressive insult created by intrastriatal injection of 6-hydroxydopamine[1]. |
数据来源文献 |
[1]. Ilijic E, et al. The L-type channel antagonist isradipine is neuroprotective in a mouse model of Parkinson's disease. Neurobiol Dis. 2011;43(2):364-371. [2]. Campbell CA, et al. Effects of isradipine, an L-type calcium channel blocker on permanent and transient focal cerebral ischemia in spontaneously hypertensive rats. Exp Neurol. 1997;148(1):45-50. [3]. Hof RP, et al. Selective effects of PN 200-110 (isradipine) on the peripheral circulation and the heart. Am J Cardiol. 1987;59(3):30B-36B. |
规格 |
1mg 5mg 10mg 50mg 100mg |
单位 |
瓶 |