|3-异丙基5-甲基 4-(苯并[c][1,2,5]恶二唑-4-基)-2,6-二甲基-1,4-二氢吡啶-3,5-二羧酸盐|CsnPharm

CAS No.: 75695-93-1

依拉地平 Catalog No. CSN11235

Synonyms: PN 200-110;DynaCirc;Prescal

Isradipine is a potent L-type calcium channel selective blocker with an IC50 of 34±8 μM.

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描述sradipine is a calcium antagonist with marked vascular selectivity and, in practical terms, is devoid of cardiac effects. Both when used as single drug treatment and in combination with other agents, particularly beta-blockers, isradipine is well tolerated, does not cause metabolic disturbances and, apart from the typical dihydropyridine-type vascular adverse effects, e.g. flushing and ankle oedema, it does not cause any specific side effect^[3]. The confirmation of its antihypertensive efficacy, along with its favourable haemodynamic profile and reversal of left ventricular hypertrophy, minimal effect on glucose and lipid metabolism, preservation of quality of life and good tolerability, makes isradipine a suitable drug for the treatment of most patients with mild to moderate hypertension^[4]. Isradipine-induced acceleration of the Ca(v)1.2 current decay reflects enhanced fast voltage-dependent inactivation and not open channel block^[2]. Isradipine in vitro attenuates beta amyloid oligomer toxicity by suppressing calcium influx into cytoplasm and by suppressing Ca(v)1.2 expression. Isradipine became bioavailable, lowered tau burden, and improved autophagy function in the brain^[5]. Chronic isradipine treatment remodeled SNc DA neurons in a way that should not only diminish their vulnerability to mitochondrial challenges, but to autophagic stress as well^[6].
临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT03538262	-	-	Enrolling by invitation	January 31, 2023	United States, New York ... more >> CHeT Telemedicine (Site 363) Rochester, New York, United States, 14642 Collapse <<
NCT00684489	Hypertension	Not Applicable	Completed	-	-
NCT01587742	-	-	Completed	-	-

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参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.6926 mL
- 13.4630 mL
- 26.9261 mL
- 5 mM
- 0.5385 mL
- 2.6926 mL
- 5.3852 mL
- 10 mM
- 0.2693 mL
- 1.3463 mL
- 2.6926 mL

技术信息

CAS号

75695-93-1

储存条件

粉末: Sealed in dry,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C19H21N3O5

运输

蓝冰

分子量

371.39

别名

PN 200-110;DynaCirc;Prescal;Lomir;PN-205-033;PN-205-034

溶解度

DMSO	74.0 mg/mL (199.3 mM)
Water	Insoluble
Ethanol	74.0 mg/mL (199.3 mM) warming

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NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点

NCT03538262	-	-	Enrolling by invitation	January 31, 2023	United States, New York ... more >> CHeT Telemedicine (Site 363) Rochester, New York, United States, 14642 Collapse <<
NCT00684489	Hypertension	Not Applicable	Completed	-	-
NCT01587742	-	-	Completed	-	-
NCT00733239	Opioid Dependence	Phase 1	Completed	-	United States, Arkansas ... more >> University of Arkansas for Medical Sciences Little Rock, Arkansas, United States, 72205 Collapse <<
NCT01007994	Hypertension Secondary to Kidn... more >>ey Transplant Collapse <<	Phase 2 Phase 3	Active, not recruiting	December 2018	United States, New York ... more >> Cohen Children's Medical Center of NY New Hyde Park, New York, United States, 11040 United States, Pennsylvania Children's Hospital of Philadelphia Philadelphia, Pennsylvania, United States, 19104 Collapse <<
NCT02136823	Chronic Spinal Cord Injury	Not Applicable	Unknown	-	-
NCT00909545	Parkinson Disease	Phase 2	Completed	-	United States, California ... more >> Parkinson Institute Sunnyvale, California, United States, 94805 United States, Connecticut Institute for Neurodegenerative Disorders New Haven, Connecticut, United States, 06510 United States, Florida Mayo Clinic Jacksonville Jacksonville, Florida, United States, 32224 University of Miami Miami, Florida, United States, 33136 University of South Flordia Tampa, Florida, United States, 33606 United States, Georgia Emory University School of Medicine Atlanta, Georgia, United States, 30329 United States, Hawaii Pacific Health Institute Honolulu, Hawaii, United States, 96817 United States, Illinois Northwestern University Chicago, Illinois, United States, 60611 Rush University Medical Center Chicago, Illinois, United States, 60612 United States, Massachusetts Boston University Boston, Massachusetts, United States, 02118 United States, Michigan Michigan State University East Lansing, Michigan, United States, 48824 United States, Minnesota Park Nicolet Clinic Golden Valley, Minnesota, United States, 55427 University of Minnesota Minneapolis, Minnesota, United States, 55455 United States, Missouri Washington University St. Louis, Missouri, United States, 63110 United States, New York University of Rochester Rochester, New York, United States, 14618 United States, Ohio University of Cincinnati Cincinnati, Ohio, United States, 45219 United States, Pennsylvania University of Pittsburgh Pittsburgh, Pennsylvania, United States, 15213 United States, Tennessee University of Tennessee Memphis, Tennessee, United States, 38104 Canada, Ontario Ottowa Hospital Civic Site Ottawa, Ontario, Canada, K1Y 4E9 Toronto Western Hospital Toronto, Ontario, Canada, M5T 2S8 Collapse <<
NCT03083353	Nicotine Dependence	Early Phase 1	Suspended(The study is being m... more >>odified to address low recruitment.) Collapse <<	January 2022	United States, Texas ... more >> University of Texas at Austin Austin, Texas, United States, 78712 Collapse <<
NCT00593463	Drug Dependence	Phase 1	Completed	-	United States, Arkansas ... more >> University of Arkansas for Medical Sciences Little Rock, Arkansas, United States, 72205 Collapse <<
NCT01895270	Opioid Dependence	Phase 1 Phase 2	Completed	-	United States, Arkansas ... more >> UAMS Psychiatric Research Institute Little Rock, Arkansas, United States, 72205 Collapse <<
NCT00909545	-	-	Completed	-	-
NCT01895270	-	-	Completed	-	-
NCT01658150	-	-	Completed	-	-
NCT00753636	-	-	Completed	-	-
NCT01784666	Bipolar Disorder	Phase 2	Terminated(Lack of Enrollment)	-	United States, Massachusetts ... more >> Massachusetts General Hospital Boston, Massachusetts, United States, 02114 Collapse <<
NCT01658150	Schizophrenia ... more >> Schizoaffective Disorder Collapse <<	Not Applicable	Completed	-	United States, New York ... more >> Icahn School of Medicine at Mount Sinai New York, New York, United States, 10029 Collapse <<
NCT01784666	-	-	Terminated(Lack of Enrollment)	-	-
NCT00753636	Parkinson's Disease	Phase 2	Completed	-	United States, Illinois ... more >> 710 N. Lake Shore Dr. Chicago, Illinois, United States, 60610 Collapse <<
NCT02168842	Parkinson Disease	Phase 3	Active, not recruiting	March 2019	-

依拉地平 Catalog No. CSN11235

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