Nicardipine HCl

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Chemical Structure| 54527-84-3 同义名 : YC-93; Nicardipine (hydrochloride); RS 69216; Nicardipine hydrochloride
CAS号 : 54527-84-3
货号 : A570738
分子式 : C26H30ClN3O6
纯度 : 99%
分子量 : 515.99
MDL号 : MFCD00057327
存储条件:

Pure form Keep in dark place, inert atmosphere, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月

溶解度 : -
动物实验配方:
生物活性
描述 Nicardipine hydrochloride (NC-HCl), a calcium channel blocker for the treatment of chronic stable angina and hypertension, seems to be a potential therapeutic transdermal system candidate, mainly due to its low dose, short half-life, and high first-pass metabolism[3]. Uterine activity was inhibited by all treatment regimens, but the most significant inhibition was achieved by the higher dose of nicardipine, which nearly abolished all uterine activity in pregnant rabbit during induced preterm uterine contractions[4]. The L-type voltage-dependent Ca(2+) channels (L-VDCC) blocker, nicardipine, significantly inhibited ACh- (acetylcholine) and Ca(2+)-enhanced BSM (bronchial smooth muscles) contractions in guinea pigs infused with HCl[5]. In patients with moyamoya disease, nicardipine may have a beneficial effect on cerebral hemodynamics and may prevent ischemic sequelae by optimizing existing collateral circulation[6]. In rabbit, nicardipine-HCl decreased the spontaneous rate of the sinoatrial (SA) node and prolonged sinus recovery time, dose-dependently. The effective refractory period (ERP) and functional refractory period (FRP) of the atrioventricular (AV) node and AV conduction time (A-H interval) were also prolonged by nicardipine-HCl in a dose-dependent manner[7].
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
NCT02286089 Age-related Macular Degenerati... 展开 >>on 收起 << Phase 1 Phase 2 Recruiting December 2019 United States, California ... 展开 >> Retina Vitreous Associates Medical Group Recruiting Los Angeles, California, United States, 900211 Contact: Janet Kurokouchi, B.Sc.    310-289-2478 ext 1243    JKurokouchi@laretina.com    Contact: Gerard Aquino, B.Sc.    310-289-2478 ext 1225    GAquino@laretina.com    Principal Investigator: David Boyer, MD          Byers Eye Institute, Stanford School of Medicine Recruiting Palo Alto, California, United States, 94303 Contact: Lisa Greer, MBA    650-725-9184    lgreer7@stanford.edu    Principal Investigator: Diana Do, Prof.          Retinal Consultants Medical Group Recruiting Sacramento, California, United States, 95819 Contact: Erin Nickerman    916-453-5429    nickermane@retinalMD.com    Contact: Whitney Lewis    916-453-5429    lewisw@retinalmd.com    Principal Investigator: David Telander, MD          West Coast Retina Medical Group, Inc Recruiting San Francisco, California, United States, 94109 Contact: Kaitlin E. Miani, BA    415-972-4607    kmiani@westcoastretina.com    Contact: C.          Principal Investigator: Richard McDonald, MD          Israel Hadassah Ein Kerem University Hospital Recruiting Jerusalem, Israel, 91120 Contact: Devora Marks Ohana    972-2-6776324    dryamdstudy@gmail.com    Principal Investigator: Tareq Jaouni, MD          Rabin Medical Center Recruiting Petah Tikva, Israel Contact: Vivi Dagan    972-3-9377199    eyeclinic@clalit.org.il    Principal Investigator: Rita Ehrlich, MD          Kaplan Medical Center Recruiting Rehovot, Israel Contact: Michal Scwartzberg    972-8-9441691    kaplaneye1@gmail.com    Principal Investigator: Haia Morori-Katz, MD          Tel Aviv Souraski Medical Center Recruiting Tel Aviv, Israel, 91121 Contact: Sagit Bechor    03-6974361    sagitba@tlvmc.gov.il    Principal Investigator: Adiel Barak, MD, Prof. 收起 <<
NCT02725840 - Recruiting April 2021 United States, Florida ... 展开 >> Department of Radiation Oncology Davis Cancer Pavilion Recruiting Gainesville, Florida, United States, 32611 Contact: John M Lybarger, MPH    352-265-0680 ext 87829    lybarj@shands.ufl.edu    Principal Investigator: Walter O'Dell, PhD          Sub-Investigator: Karen Daily, DO          Sub-Investigator: Coy Heldermon, MD, PhD          Sub-Investigator: David Wymer, MD          Sub-Investigator: Fei Zou, PhD          Sub-Investigator: Paul Okunieff, MD          Sub-Investigator: Jorge Lascano, MD          University of Florida Health Proton Therapy Institute Recruiting Jacksonville, Florida, United States, 32206 Contact: Julie Bradley, MD    904-588-1800    jbradley@floridaproton.org    Sub-Investigator: Nancy Mendenhall, MD          Sub-Investigator: Christopher Klassen, MD, PhD          Sub-Investigator: Michael Rutenberg, MD          Sub-Investigator: Roi Dagan, MD, MS          Principal Investigator: Julie Bradley 收起 <<
NCT01893307 Head And Neck Cancer Phase 2 Phase 3 Recruiting August 2023 United States, Arizona ... 展开 >> Mayo Clinic - Arizona Recruiting Scottsdale, Arizona, United States, 85259 United States, California University of California at San Diego Recruiting La Jolla, California, United States, 92093 Contact: Loren Mell, MD          United States, Florida Florida Health Protocol Institute Recruiting West Palm Beach, Florida, United States, 33407 Contact: Roi Dagan, MD          United States, Illinois Northwestern Memorial Hospital Recruiting Chicago, Illinois, United States, 60611 Contact: John H. Han-Chang, MD          United States, Maryland University of Maryland Recruiting College Park, Maryland, United States, 20742 Contact: William Regine, MD          Contact: Charles Simone, MD          United States, Massachusetts Massachusetts General Hospital Recruiting Boston, Massachusetts, United States, 02114 Contact: Paul Busse, MD          United States, Minnesota Mayo Clinic Recruiting Rochester, Minnesota, United States, 55905 Contact: Robert Foote, MD          United States, New York Memorial-Sloan Kettering Cancer Center Recruiting New York, New York, United States, 10065 Contact: Nancy Y. Lee, MD          United States, Pennsylvania University of Pennsylvania Health System Recruiting Philadelphia, Pennsylvania, United States, 19104 Contact: Alexander Lin, MD          United States, Texas University of Texas MD Anderson Cancer Center Recruiting Houston, Texas, United States, 77030 United States, Washington University of Washington Recruiting Seattle, Washington, United States, 98105 Contact: Upendra Parvathaneni, MD 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.94mL

0.39mL

0.19mL

9.69mL

1.94mL

0.97mL

19.38mL

3.88mL

1.94mL

参考文献

[1]Huang BR, Chang PC, et al. Anti-neuroinflammatory effects of the calcium channel blocker nicardipine on microglial cells: implications for neuroprotection. PLoS One. 2014 Mar 12;9(3):e91167.

[2]Gasior M, Kamiński R, et al. Influence of nicardipine, nimodipine and flunarizine on the anticonvulsant efficacy of antiepileptics against pentylenetetrazol in mice. J Neural Transm (Vienna). 1996;103(7):819-31.

[3]Aboofazeli R, Zia H, Needham TE. Transdermal delivery of nicardipine: an approach to in vitro permeation enhancement. Drug Deliv. 2002;9(4):239‐247

[4]Holbrook RH Jr, Lirette M, Katz M. Cardiovascular and tocolytic effects of nicardipine HCl in the pregnant rabbit: comparison with ritodrine HCl. Obstet Gynecol. 1987;69(1):83‐87

[5]Cheng YM, Cao AL, Zheng JP, et al. Airway hyperresponsiveness induced by repeated esophageal infusion of HCl in guinea pigs. Am J Respir Cell Mol Biol. 2014;51(5):701‐708

[6]Hosain SA, Hughes JT, Forem SL, Wisoff J, Fish I. Use of a calcium channel blocker (nicardipine HCl) in the treatment of childhood moyamoya disease. J Child Neurol. 1994;9(4):378‐380

[7]Tamamura T, Konishi T, Matsuda H, Kadoya M, Yokoyama S, Kawai C. Electrophysiological effects of nicardipine hydrochloride on the isolated sinoatrial and atrioventricular nodes of the rabbit. Jpn Circ J. 1983;47(7):817‐823