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ID1930 盐酸地尔硫卓 跨膜转运/离子通道 索莱宝

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  • 北京
  • ID1930
  • 2025年07月23日
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    • 详细信息
    • 文献和实验
    • 技术资料
    • 保存条件

      Powder:2-8℃,2 years;Insolvent(母液):-20℃,6 months;-80℃,1 year

    • 保质期

      Powder:2-8℃,2 years;Insolvent(母液):-20℃,6 months;-80℃,1 year

    • 英文名

      Diltiazem Hydrochloride

    • 库存

      现询

    • 供应商

      北京索莱宝科技有限公司

    • CAS号

      33286-22-5

    • 规格

      100mg

    基本信息
    CASNo.33286-22-5
    中文名称盐酸地尔硫卓
    英文名称Diltiazem Hydrochloride
    别名CRD-401;Diltiazem HCl;RG 83606 HCl
    分子式C22H27ClN2O4S
    分子量450.98
    溶解性Soluble in Water ≥5mg/mL
    纯度≥98%
    外观(性状)White to off-white Solid
    储存条件Powder:2-8℃,2 years;Insolvent(母液):-20℃,6 months;-80℃,1 year
    ECEINECS 251-443-3
    MDLMFCD00069252
    SMILESCN(C)CCN1C2=CC=CC=C2S[C@@H](C3=CC=C(OC)C=C3)[C@@H](OC(C)=O)C1=O.Cl
    InChIKeyHDRXZJPWHTXQRI-BHDTVMLSSA-N
    InChIInChI=1S/C22H26N2O4S.ClH/c1-15(25)28-20-21(16-9-11-17(27-4)12-10-16)29-19-8-6-5-7-18(19)24(22(20)26)14-13-23(2)3;/h5-12,20-21H,13-14H2,1-4H3;1H/t20-,21+;/m1./s1
    PubChem CID62920
    靶点Calcium Channel
    通路Membrane Transporter&Ion Channel;Neuronal Signaling
    背景说明是钙离子流入抑制剂。
    生物活性Diltiazem hydrochloride is a Ca2+ influx inhibitor (slow channel blocker or calcium antagonist).[1-5]
    In VitroWe investigated the contribution of individual IIIS6 amino acid residues for diltiazem sensitivity by employing alanine scanning mutagenesis in a benzothiazepine-sensitive alpha1 subunit chimera (ALDIL) expressed in Xenopus laevis oocytes.The most dramatic decrease of block by 100 microM diltiazem (ALDIL 45 +/- 4.8% inhibition) during trains of 100-ms pulses (0.1 Hz, -80 mV holding potential) was found after mutation of adjacent IIIS6 residues Phe1164(21 +/- 3%) and Val1165 (8.5 +/- 1.4%). Diltiazem delayed current recovery by promoting a slowly recovering current component. This effect was similar in ALDIL and F1164A but largely prevented in V1165A. Both mutations slowed inactivation kinetics during a pulse. The reduced diltiazem block can therefore be explained by slowing of inactivation kinetics (F1164A and V1165A) and accelerated recovery from drug block (V1165A).The bulkier diltiazem derivative benziazem still efficiently blocked V1165A. From these functional and from additional radioligand binding studies with the dihydropyridine (+)-[3H]isradipine we propose a model in which Val1165 controls dissociation of the bound diltiazem molecule, and where bulky substituents on the basic nitrogen of diltiazem protrude toward the adjacent dihydropyridine binding domain.[1]。
    细胞实验In conscious and anesthetized normotensive rats, intravenous administration of diltiazem (0.1--3 mg/kg) produced a dose - related decrease in blood pressure. Administration of diltiazem (1--50 mg/kg) into the duodenum of anesthetized rats also reduced the blood pressure in a dose related manner. In parallel with the change in blood pressure, the heart rate increased in conscious rats and decreased in anesthetized animals. Such an increase in the heart rate was suppressed by pretreatment with propranolol.[5]。
    数据来源文献[1]. Kraus RL, et al. Molecular mechanism of diltiazem interaction with L-type Ca2+ channels. J Biol Chem. 1998 Oct 16;273(42):27205-12.
    [2]. van Breemen C, et al. The mechanism of inhibitory action of diltiazem on vascular smooth muscle contractility. J Pharmacol Exp Ther. 1981 Aug;218(2):459-63.
    [3]. Chiesi M, et al. Stereospecific action of diltiazem on the mitochondrial Na-Ca exchange system and on sarcolemmal Ca-channels. Biochem Pharmacol. 1987 Sep 1;36(17):2735-40.
    [4]. Freitas F, et al. Cardiac microvascular rarefaction in hyperthyroid rats is reversed by losartan, diltiazem, and propranolol. Fundam Clin Pharmacol. 2015 Feb;29(1):31-40.
    [5]. Sato M, et al. Hypotensive effects of diltiazem hydrochloride in the normotensive, spontaneously hypertensive and renal hypertensive rats (authors transl). Nihon Yakurigaku Zasshi. 1979 Mar;75(2):99-106.
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