Anipamil
(Synonyms: 阿尼帕米) 目录号 : GC32566
Anipamil是一种长效的calciumchannel阻滞剂，常用于心血管疾病研究。
Cas No.:83200-10-6
Sample solution is provided at 25 µL, 10mM.
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- Purity: >98.00%
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Animal experiment: | Preliminary studies are performed to determine the anipamil dose response. Anipamil is mixed with food to give a dose of 0.5, 2 or 5 mg/kg/day. One week after five-sixths nephrectomy, rats are paired according to renal function, blood pressure and body weight. Rats are then pair-fed and receive either the long-acting calcium channel blocker anipamil (2 mg/kg/day in food, n=20) or placebo (n=20). |
References: [1]. Pauletto P, et al. Anipamil prevents intimal thickening in the aorta of hypertensive rabbits through changes in smooth muscle cell phenotype. Am J Hypertens. 1996 Jul;9(7):687-94. | |
Anipamil is a long-acting calcium channel blocker, used for the treatment of cardiovascular disease.
Anipamil (40 mg, p.o.)-treated 2K-1C rabbits reveal absent or negligible intimal thickening and a decrease of postnatal-type SMC from the underlying media. Anipamil inhibits the growth of SMC accompanied by the expression of SM-MyHC in all SMC, ie, the appearance of a more differentiated cell phenotype compared to control cultures[1]. In the arrhythmic assay, anipamil (1.0 mg/kg + 0.10 mg/kg/min infusion, n=8 or 5.0 mg/kg + 0.50 mg/kg/min infusion, n=12) reduces VT but not VF[2]. In rats with subtotal (five-sixths) nephrectomy treated with anipamil (0.5 mg/kg/day, p.o.), the mortality is less, and the mean arterial blood pressure is also more well controlled, and the serum creatinine concentration is lower than control group. The anipamil (2 mg/kg/day)-treated group exhibits significantly greater protection of renal function than does the hydralazine-treated group for the same level of blood pressure control[3].
[1]. Pauletto P, et al. Anipamil prevents intimal thickening in the aorta of hypertensive rabbits through changes in smooth muscle cell phenotype. Am J Hypertens. 1996 Jul;9(7):687-94. [2]. Pugsley MK, et al. Effects of anipamil, a long acting analog of verapamil, in pigs subjected to myocardial ischemia. Life Sci. 1995;57(12):1219-31. [3]. Jarusiripipat C, et al. Effect of long-acting calcium entry blocker (anipamil) on blood pressure, renal function and survival of uremic rats. J Pharmacol Exp Ther. 1992 Jan;260(1):243-7.
| Cas No. | 83200-10-6 | SDF | |
| 别名 | 阿尼帕米 | ||
| Canonical SMILES | N#CC(CCCN(CCC1=CC=CC(OC)=C1)C)(CCCCCCCCCCCC)C2=CC=CC(OC)=C2 | ||
| 分子式 | C34H52N2O2 | 分子量 | 520.79 |
| 溶解度 | Soluble in DMSO | 储存条件 | Store at -20°C |
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.9202 mL | 9.6008 mL | 19.2016 mL |
| 5 mM | 0.384 mL | 1.9202 mL | 3.8403 mL |
| 10 mM | 0.192 mL | 0.9601 mL | 1.9202 mL |
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Anipamil prevents intimal thickening in the aorta of hypertensive rabbits through changes in smooth muscle cell phenotype
Am J Hypertens 1996 Jul;9(7):687-94.PMID:8806982DOI:10.1016/0895-7061(96)00032-5.
The aim of this study was to evaluate the effect of Anipamil, a phenyalkylamine-derived Ca(2+)-antagonist, on aortic intimal thickening and smooth muscle cell (SMC) phenotype in 2K-1C hypertensive rabbits. Monoclonal antimyosin antibodies [SM-E7, NM-G2, and NM-F6, which respectively, recognize smooth muscle (SM), A-type-, and B-type-like nonmuscle (NM) myosin heavy chains (MyHC)] identify different aortic SMC types: adult (SM-E7-positive), postnatal (SM-E7- and NM-G2-positive), and fetal (SM-E7-, NM-G2-, and NM-F6-positive). Twenty-four hypertensive rabbits were studied 2.5 months (n = 12) and 4 months (n = 12) after clipping. Six animals from each group were given Anipamil (40 mg orally, once daily) immediately after surgery. The remaining 2K-1C were given a daily oral placebo. Normotensive age-matched controls were also studied. Transverse cryosections of aorta were taken for computerized morphometry and immunocytochemical studies. Primary and secondary SMC cultures were used to define potential changes in cell phenotype after adding Anipamil to the culture medium. In untreated 2K-1C, intimal thickening, mainly composed of postnatal-type SMC, was found by 2.5 months after clipping. Morphometric and immunofluorescence studies in anipamil-treated 2K-1C rabbits revealed absent or negligible intimal thickening and a decrease of postnatal-type SMC from the underlying media. In culture experiments, growth inhibition of SMC by Anipamil was accompanied by the expression of SM-MyHC in all SMC, ie, the appearance of a more differentiated cell phenotype compared to control cultures. In conclusion, prevention of intimal thickening in anipamil-treated 2K-1C was achieved through selective reduction in the media of the postnatal-type SMC. This could be achieved by reducing NM-MyHC content or increasing synthesis of SM-MyHC expression. As blood pressure was not significantly lowered by Anipamil treatment, a direct and specific antiproliferative action of this drug on medial SMC is likely to take place.
Efficacy of Anipamil, a phenylalkylamine calcium antagonist, in treatment of angina pectoris
J Cardiovasc Pharmacol 1994 Nov;24(5):841-5.PMID:7532763DOI:10.1097/00005344-199424050-00020.
To evaluate the efficacy of Anipamil, a phenylalkylamine calcium antagonist, in treatment of stable angina pectoris, we performed a randomized, double blind placebo-controlled, cross-over study. Inclusion criteria were (a) stable angina pectoris for at least 2 months, (b) an exercise test with > or = 0.1-mV horizontal or downsloping ST-segment depression limited by angina, and (c) at least 10 attacks of angina pectoris in a single-blind 3-week run-in period. Nineteen patients were randomized to enter the study. In 3-week periods, they received either Anipamil 80 mg once daily (o.d.), Anipamil 160 mg o.d., or placebo. At the end of each period, an exercise test was performed. The number of angina pectoris attacks was significantly reduced during treatment with Anipamil 80 mg (p < 0.05) and Anipamil 160 mg (p < 0.001) as compared with placebo. Glycerol nitrate consumption was significantly reduced during treatment with Anipamil 80 mg (p < 0.01) and 160 mg (p < 0.001) as compared with placebo. During exercise testing, the load (W) at start of angina was significantly increased during treatment with Anipamil 80 mg (p < 0.01) and 160 mg (p < 0.05) as compared with placebo. Heart rate (HR) at 0.1 mV ST-segment depression was increased during treatment with Anipamil 80 mg (p < 0.001). Few adverse events were reported.
Antihypertensive, anticalcinotic, and antiarteriosclerotic properties of Anipamil, a long-acting new derivative of verapamil
J Cardiovasc Pharmacol 1989;13 Suppl 4:S23-8.PMID:2475679DOI:10.1097/00005344-198900134-00006.
The classical indication for calcium antagonists has for a long time been coronary heart disease. However, more recent experimental data as well as a host of clinical observations now encourage a broader use of these drugs also for antihypertensive purposes and for prevention of concomitant sclerotic vascular injury. Needless to say, for the treatment of hypertensive crises rapidly acting calcium antagonists are required, whereas for chronic therapy of hypertension calcium antagonists with a long duration of action on blood pressure are advantageous. In this context Anipamil seems to be particularly suited for long-term control of elevated blood pressure. Thus, Anipamil justifies good therapeutic expectations regarding the clinical management of essential or renal hypertension.
The antiarrhythmic efficacy of intravenous Anipamil against occlusion and reperfusion arrhythmias
Br J Pharmacol 1989 Dec;98(4):1165-72.PMID:2611487DOI:10.1111/j.1476-5381.1989.tb12661.x.
1. Anipamil, a long acting analogue of verapamil, was tested for its actions against arrhythmias induced by ischaemia and reperfusion in conscious and anaesthetized rats, as well as for effects on epicardial intracellular action potentials. 2. When given 15 min or 4 h before coronary occlusion, 1 and 5 mg kg-1 Anipamil reduced ischaemia-induced arrhythmias in conscious rats. The same doses also reduced arrhythmias when given 15 min before occlusion in acutely-prepared anaesthetized rats. ED50 values were between 1 and 5 mg kg-1. 3. The incidence of reperfusion arrhythmias depended upon the period of regional ischaemia prior to reperfusion such that the peak incidence occurred after 5-7 min of ischaemia. Anipamil (2.5 mg kg-1, i.v.) selectively abolished the reperfusion arrhythmias induced by short periods of ischaemia, although some antiarrhythmic effects were seen for all periods of ischaemia. 4. Anipamil slowed the rate of development of R-wave increases and S-T segment elevations induced by ischaemia, but did not reduce the maximum values they attained. 5. Anipamil (2.5 mg kg-1 i.v.) lacked Class I or III electrophysiological actions on intracellular action potentials recorded in vivo from the epicardium of rat hearts. 6. In conclusion, the antiarrhythmic actions of Anipamil appeared to depend upon calcium antagonism which may have reduced arrhythmias by a combination of anti-ischaemic and direct anti-arrhythmic actions. Presumed anti-ischaemic actions changed the relationship between the duration of preceding ischaemia and resulting reperfusion arrhythmias.
Effects of Anipamil on cardiovascular status and regional blood flow in anaesthetized rats
Br J Pharmacol 1989 Dec;98(4):1185-90.PMID:2611488DOI:10.1111/j.1476-5381.1989.tb12663.x.
1. Anipamil, a long-acting analogue of verapamil, was tested at 1, 2.5 and 5 mg kg-1 i.v. for its effects on cardiovascular status and blood flow in different organs and vascular beds in rats anaesthetized with pentobarbitone. 2. Blood flow was determined by microsphere (57Co or 113Sn) injection before, and 1 h after, administration of Anipamil at the above doses. 3. Anipamil produced a dose-dependent fall in blood pressure and heart rate. This was associated with a fall in peripheral resistance. At the highest dose there was, in addition, evidence of myocardial depression. 4. Both blood flow and conductance (flow corrected for blood pressure) were notably increased by Anipamil in heart, liver and skeletal muscle beds, but were decreased, especially at the high doses, in kidneys, intestine and spleen. 5. The profile of the actions of Anipamil on haemodynamic performance and flow was consistent with its proposed calcium antagonist actions. This profile was similar to that of verapamil.