Cicloprolol hydrochloride
(Synonyms: 盐酸环丙洛尔) 目录号 : GC32542
Cicloprolol是部分β1-肾上腺素能受体(β1-adrenoceptor)激动剂。
Cas No.:63686-79-3
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Cicloprolol is a partial β 1-adrenoceptor agonist .
Cicloprolol is a partial β1-adrenoceptor agonist considered for the treatment of patients with coronary artery disease and impaired left ventricular function[1]. The new β-adrenoceptor partial agonist Cicloprolol acts as a β-agonist at normal levels and as a β-antagonist at high levels of adrenergic discharge. Treatment with Cicloprolol should protect the heart against excessive stimulation, while providing a baseline level of sympathetic drive. Cicloprolol has a weak β1-agonistic effect at normal levels of adrenergic discharge and acts as an antagonist at high levels of discharge[2].
[1]. Weber S, et al. Pharmacodynamic without pharmacokinetic interaction between cicloprolol, a partial beta 1-adrenoceptor agonist, and digoxin in healthy subjects. Br J Clin Pharmacol. 1990 Sep;30(3):411-6 [2]. Cocco G, et al. An evaluation of the safety of the beta-modulator cicloprolol in chronic heart failure. Clin Cardiol. 1992 Jan;15(1):38-42.
| Cas No. | 63686-79-3 | SDF | |
| 别名 | 盐酸环丙洛尔 | ||
| Canonical SMILES | OC(CNC(C)C)COC1=CC=C(OCCOCC2CC2)C=C1.[H]Cl | ||
| 分子式 | C18H30ClNO4 | 分子量 | 359.89 |
| 溶解度 | Soluble in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.7786 mL | 13.8931 mL | 27.7863 mL |
| 5 mM | 0.5557 mL | 2.7786 mL | 5.5573 mL |
| 10 mM | 0.2779 mL | 1.3893 mL | 2.7786 mL |
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| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
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1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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Pharmacodynamic without pharmacokinetic interaction between Cicloprolol, a partial beta 1-adrenoceptor agonist, and digoxin in healthy subjects
Br J Clin Pharmacol 1990 Sep;30(3):411-6.PMID:1977438DOI:10.1111/j.1365-2125.1990.tb03792.x.
1. Cicloprolol is a partial beta 1-adrenoceptor agonist considered for the treatment of patients with coronary artery disease and impaired left ventricular function. In such patients, digoxin remains in widespread use. 2. We assessed the pharmacokinetic and pharmacodynamic interaction between oral Cicloprolol 50 mg day-1 and oral digoxin 0.25 mg day-1 in 10 healthy male volunteers, using a double-blind, randomised protocol, during three 8 day periods. Digoxin was given alone during the first period to reach steady state; then digoxin was given with Cicloprolol or placebo during the second and third periods, according to a cross-over design. 3. No significant adverse effects were observed. 4. The pharmacokinetics of digoxin were not different significantly at the end of the placebo-digoxin and cicloprolol-digoxin periods. 5. A significant increase in minimum heart rate and mean nocturnal heart rate, assessed by 24 h Holter recordings, was observed at the end of the cicloprolol-digoxin period as compared with the placebo-digoxin period (means +/- s.e. mean, 57.1 +/- 3.2 beats min-1 vs 52.2 +/- 3.1 beats min-1, P less than 0.01; and 65.6 +/- 3.8 beats min-1 vs 59.9 +/- 3.9 beats min-1, P less than 0.01, respectively). 6. A significant increase in left ventricular ejection fraction and shortening fraction, assessed by echocardiography, was noted at the end of the cicloprolol-digoxin period as compared with the placebo-digoxin period (means +/- s.e. mean, 66.4 +/- 1.4% vs 61.3 +/- 1.2%, P less than 0.05; and 37.0 +/- 1.1% vs 33.3 +/- 0.9%, P less than 0.05, respectively).(ABSTRACT TRUNCATED AT 250 WORDS)
Comparative analysis of beta-1 adrenoceptor agonist and antagonist potency and selectivity of Cicloprolol, xamoterol and pindolol
J Pharmacol Exp Ther 1987 Sep;242(3):1025-34.PMID:2888869doi
The partial beta adrenoceptor agonist properties of Cicloprolol, xamoterol and pindolol have been compared in vivo (anesthetized catecholamine-depleted or pithed rats) and in vitro (guinea pig or rat right atria and guinea pig tracheal muscle preparations) conditions. All three compounds increased heart rate in the former preparations, and their intrinsic activities relative to isoproterenol were 0.7, 0.65 and 0.45, respectively. The positive chronotropic effects of Cicloprolol or xamoterol were competitively antagonized by betaxolol or propranolol; however, part of those induced by pindolol were resistant to these beta adrenoceptor antagonists. None of these compounds increased the spontaneous beating rate of isolated guinea pig atria; however, xamoterol only increased heart rate in isolated rat atria, and its intrinsic activity with respect to isoproterenol was 0.4. Pindolol, xamoterol and Cicloprolol behaved as competitive beta-1 adrenoceptor antagonists against isoproterenol-induced tachycardia in a pithed rat model. In order to mimic the intrinsic effects of the partial agonist drugs, control dose-response curves for isoproterenol were determined in pithed rats in which the base-line heart rate was elevated by thoracic spinal cord stimulation. In this in vivo preparation, xamoterol and pindolol were more potent beta-1 adrenoceptor antagonists than Cicloprolol; however, Cicloprolol and xamoterol, in contrast to pindolol, were selective for beta-1 adrenoceptors. In isolated spontaneously beating guinea pig right atria, Cicloprolol and xamoterol were equipotent beta-1 adrenoceptor antagonists but were about 50 times less potent than pindolol. In isolated rat atria, the beta-1 adrenoceptor antagonist potency of xamoterol was greater (pA2 = 8.7) than in guinea pig atria (pA2 = 7.8). The potencies of Cicloprolol and pindolol did not vary between these species. In catecholamine-depleted rats, high i.v. doses of Cicloprolol had vasodilator activity that was partly mediated by beta-2 adrenoceptors. In carbachol-contracted guinea pig trachea, Cicloprolol and xamoterol, in contrast to pindolol, were relatively inactive against isoproterenol-induced relaxation. In conclusion, Cicloprolol and xamoterol, similarly to pindolol, behave as agonists and antagonists of beta-1 adrenoceptors. However, only Cicloprolol and xamoterol show an elevated degree of selectivity toward the beta-1 adrenoceptor subtype.
Studies of the agonist and antagonist activity of Cicloprolol in man
Eur J Clin Pharmacol 1988;34(6):569-75.PMID:3169110DOI:10.1007/BF00615219.
To assess the partial agonist activity of Cicloprolol in man, four studies were carried out in normal male volunteers. I and II. Open dose escalating studies of the effects of oral doses of the drug on exercise tachycardia and sleeping heart rate. III and IV. Double-blind randomized studies of the effects of placebo, Cicloprolol 25 mg, Cicloprolol 50 mg, Cicloprolol 100 mg, atenolol 50 mg, pindolol 10 mg, salbutamol 8 mg and prenalterol 50 mg on sleeping heart rate, resting supine heart rate, blood pressure, forearm blood flow, finger tremor and exercise tachycardia. All doses of Cicloprolol above 2.5 mg reduced an exercise tachycardia but there was no increase in effect above a dose of 50 mg. Cicloprolol caused a dose dependent increase in sleeping heart rate up to 200 mg. Cicloprolol increased resting supine heart rate, systolic blood pressure, forearm blood flow and finger tremor. None of the drugs affected quality of sleep. Cicloprolol has significant partial agonist activity at the beta 1-adrenoceptor as indicated by increases in heart rate and systolic blood pressure. The increases in finger tremor and forearm blood flow suggest that Cicloprolol has some partial agonist activity at the beta 2-adrenoceptor.
An evaluation of the safety of the beta-modulator Cicloprolol in chronic heart failure
Clin Cardiol 1992 Jan;15(1):38-42.PMID:1347258DOI:10.1002/clc.4960150109.
The new beta-adrenoceptor partial agonist Cicloprolol acts as a beta-agonist at normal levels and as a beta-antagonist at high levels of adrenergic discharge. Treatment with Cicloprolol should protect the heart against excessive stimulation, while providing a baseline level of sympathetic drive. The clinical interest of such a profile is, however, not yet established in heart failure. Accordingly this study examined the safety of oral Cicloprolol, a step necessary before undertaking efficacy comparison with other compounds recently proposed to treat heart failure. Twenty-five patients were studied. Cicloprolol was given once a day for 2 weeks in a crossover double-blind placebo-controlled design. Follow-ups were obtained at baseline and at the end of each period. At baseline all patients had clear evidence of heart failure. Cicloprolol did not affect resting heart rate and blood pressure, but it reduced significantly peak exercise heart rate and peak rate-pressure product. The effect was especially significant in patients with sinus rhythm. The drug did not induce bradycardia or arrhythmias. Resting and exercise ejection rate were not affected. Cicloprolol improved the quality of life and the work capacity of 5 of 12 patients with congestive failure due to ischemic etiology. Side effects were few and similar with placebo and Cicloprolol. Thus, short-term administration of Cicloprolol is safe in moderate heart failure.
Effect of Cicloprolol in intraocular pressure in healthy volunteers
Br J Clin Pharmacol 1988 Jul;26(1):89-91.PMID:2904826DOI:10.1111/j.1365-2125.1988.tb03368.x.
Two oral doses of Cicloprolol (50 mg and 100 mg), a beta 1-adrenoceptor partial agonist, were administered to nine healthy volunteers in a double-blind placebo-controlled study. Intraocular pressure (IOP) and exercise heart rate were reduced while the resting heart rate and blood pressure remained unchanged. The responses to the two different doses of Cicloprolol were similar.