Arbutamine
(Synonyms: (R)-4-[1-羟基-2-[[4-(4-羟基苯基)丁基]氨基]乙基]-1,2-苯二醇) 目录号 : GC60593
Arbutamine是一种短效的，非选择性β-肾上腺素受体(β-adrenoceptor)激动剂，可增加心率，心脏收缩力和收缩压。Arbutamine是一种用于儿科心脏应激因子的儿茶酚胺。
Cas No.:128470-16-6
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Arbutamine is a short-acting, potent and nonselective β-adrenoceptor agonist that increases heart rate, cardiac contractility, and systolic blood pressure[1]. Arbutamine is a catecholamine for a pharmacological cardiac stress agen[2].
Arbutamine (i.v.; 5, 10, 50, 100, and 250 ng/kg/min) increases mean heart rate, peak positive left ventricular pressure and its first time-derivative, and normal-zone myocardial thickening in 8 open-chest dogs (mean weight, 26.91 kg).
[1]. Ruiz M, et al. Arbutamine stress perfusion imaging in dogs with critical coronary artery stenoses: (99m)Tc-sestamibi versus (201)Tl. J Nucl Med. 2002 May;43(5):664-70. [2]. Nagarajan R, et al. A novel catecholamine, arbutamine, for a pharmacological cardiac stress agent. Cardiovasc Drugs Ther. 1996 Mar;10(1):31-8.
| Cas No. | 128470-16-6 | SDF | |
| 别名 | (R)-4-[1-羟基-2-[[4-(4-羟基苯基)丁基]氨基]乙基]-1,2-苯二醇 | ||
| Canonical SMILES | OC1=CC=C([C@@H](O)CNCCCCC2=CC=C(O)C=C2)C=C1O | ||
| 分子式 | C18H23NO4 | 分子量 | 317.38 |
| 溶解度 | 储存条件 | Store at -20°C, protect from light, stored under nitrogen | |
| 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 | 3.1508 mL | 15.754 mL | 31.508 mL |
| 5 mM | 0.6302 mL | 3.1508 mL | 6.3016 mL |
| 10 mM | 0.3151 mL | 1.5754 mL | 3.1508 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 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 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
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，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
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。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Arbutamine stress echocardiography
Eur Heart J 1997 Jun;18 Suppl D:D24-30.PMID:9183607DOI:10.1093/eurheartj/18.suppl_d.24.
Arbutamine, a new potent non-selective beta-adrenoceptor agonist with mild alpha 1-sympathomimetic activity, has been developed specifically for pharmacological stress testing. The drug acts like physical exercise, increasing both heart rate and myocardial contractility. Sensitivity, specificity and accuracy in detecting significant stenotic coronary artery disease are 76%, 96%, and 82%, respectively, again similar to those of exercise echocardiography. The drug is delivered by a computerized drug delivery and monitoring device (GenESA) which adjusts the infusion rate according to the patient's heart rate data feedback. The drug is generally well tolerated and has an acceptable safety profile. This article describes recent clinical experience with Arbutamine and presents preliminary results of a multicentre multinational study which evaluates the clinical utility and safety of the GenESA system in diagnosing coronary artery disease.
Arbutamine stress perfusion imaging in dogs with critical coronary artery stenoses: (99m)Tc-sestamibi versus (201)Tl
J Nucl Med 2002 May;43(5):664-70.PMID:11994532doi
Having previously shown that dobutamine reduces (99m)Tc-methoxyisobutylisonitrile (sestamibi [MIBI]) uptake in normal myocardium by elevating intracellular calcium, we hypothesized that Arbutamine, which has less inotropic effect than dobutamine, might cause less reduction in MIBI uptake, thereby improving defect contrast. In this study using a canine model, we compared the effects of Arbutamine stress on myocardial blood flow, myocardial MIBI uptake, and systolic thickening in the presence of a coronary artery stenosis. Methods: Arbutamine was infused (0.5-250 ng/kg/min) in 8 open-chest dogs with critical coronary stenoses that abolished flow reserve. At the time of peak Arbutamine effect, MIBI (296 MBq), (201)Tl (27.75 MBq), and microspheres were coinjected. The dogs were killed 5 min later, and myocardial tracer activities and flow were quantified by well counting. Ex vivo imaging of heart slices was also performed. Results: Arbutamine increased mean heart rate, peak positive left ventricular pressure and its first time-derivative, and normal-zone myocardial thickening. Stenotic zone flow and thickening did not increase during Arbutamine infusion. MIBI uptake versus flow was significantly lower than (201)Tl uptake at the same flow values. By imaging, defect magnitude (stenotic/normal) was greater for (201)Tl than MIBI (0.57 vs. 0.77; P < 0.001) [corrected]. Conclusion: In the presence of coronary stenoses that abolished regional flow reserve, myocardial uptake of MIBI, compared with (201)Tl, significantly underestimated the arbutamine-induced flow heterogeneity. The attenuation of MIBI uptake and diminished defect contrast during Arbutamine stress were comparable with those previously reported for dobutamine stress.
Arbutamine vs. exercise stress testing in patients with coronary artery disease: evaluation by echocardiography and electrocardiography
Int J Cardiol 1996 Nov 15;57(1):81-9.PMID:8960948DOI:10.1016/s0167-5273(96)02765-9.
Arbutamine is a new beta-adrenergic agonist with potent chronotropic and inotropic properties developed to pharmacologically induce stress. A prospective trial was conducted in five centers with a total enrolment of 45 patients with angiographically documented coronary artery disease. The primary purpose of the trial was to compare the efficacy of Arbutamine with symptom-limited exercise in provoking clinical (angina), electrocardiographic (> or = 0.1 mV ST depression) and echocardiographic (induced wall motion abnormality) evidence of transient stress-induced ischemia. The secondary purpose was to assess the safety of Arbutamine in patients with coronary artery disease. Ischemia was induced at a lower heart rate, systolic blood pressure and pressure-rate product during Arbutamine infusion than during exercise. Using angina and/or electrocardiographic evidence of ischemia, Arbutamine was more sensitive than exercise in detecting myocardial ischemia (77 vs. 58%, P = 0.021). Using echocardiography, the sensitivity for inducing wall motion abnormalities was 88% with Arbutamine and 79% with exercise (P = not significant). Echocardiography in combination with angina and/or electrocardiographic evidence increased the sensitivity to 94% using Arbutamine and to 88% with exercise. For the patients with multivessel disease, the sensitivity was 97% and 91%, respectively. No serious adverse events, either cardiac or noncardiac, were associated with Arbutamine, and no patient had prolonged ischemia. Although exercise is the preferred method of stress for patients who are able to exercise adequately, Arbutamine is at least as sensitive as exercise for the diagnosis of myocardial ischemia, and appears to be a safe and effective alternative to exercise testing in patients unable to exercise adequately.
Arbutamine stimulation detects viable myocardium 4 weeks after coronary occlusion
J Am Soc Echocardiogr 2001 Feb;14(2):138-48.PMID:11174448DOI:10.1067/mje.2001.108932.
At low doses, dobutamine has potent inotropic, but limited chronotropic, effects-properties that may be necessary for detection of hibernating myocardium. The efficacy of other catecholamines, which have more closely coupled inotropic and chronotropic effects, for the detection of viable myocardium is unknown. This study evaluated the efficacy of Arbutamine, a catecholamine with potent chrono-tropic effects, for the detection of viable myocardium in a canine model of hibernating myocardium. Contractile reserve was assessed during stepwise Arbutamine infusion (dosages of 2.5, 5, 10, 50, and 100 ng/kg/min) at 3 days (early) and 4 weeks (late) after coronary ligation. Segment shortening, wall thickening, and segmental wall motion were assessed by sonomicrometry and echocardiography. After 4 weeks of occlusion, functional recovery was assessed after revascularization. During the early Arbutamine study, the sensitivity for predicting functional recovery was highest at a dosage of 50 ng/kg/min, which also produced tachycardia. The sensitivity was 50% for segment shortening, 20% for wall thickening, and 75% for wall motion score. The late Arbutamine study had improved sensitivity. The sensitivity was 100% for segment shortening, 80% for wall thickening, and 90% for wall motion score at a dosage of 50 ng/kg/min. At the late Arbutamine study, myocardial perfusion reserve in the ischemic zone of dogs with functional recovery was only mildly reduced (2.0 versus 2.6 in nonischemic zones, P =.53). After coronary occlusion, viable myocardium can be detected with high doses of Arbutamine that produce tachycardia. However, the sensitivity of Arbutamine stimulation for predicting functional recovery is low early after occlusion, but it is improved by 4 weeks after occlusion with adequate perfusion reserve.
Pharmacologic stress echocardiography. Dobutamine and Arbutamine stress testing
Cardiol Clin 1999 Aug;17(3):461-79, viii.PMID:10453293DOI:10.1016/s0733-8651(05)70091-6.
Pharmacologic stress testing is an important noninvasive method for evaluating patients with known or suspected coronary artery disease who are unable to adequately exercise. Pharmacologic stress echocardiography using dobutamine has been developed over the last 10 to 15 years as an alternative to vasodilator stress testing using nuclear perfusion imaging. As experience has grown, digital subtraction echocardiogram has been shown to be a safe, convenient, and reliable method for stress testing in a variety of patient populations. Digital subtraction echocardiogram has comparable sensitivity, specificity, and accuracy when compared to other stress testing methods which employ cardiac imaging and is superior to the exercise echocardiogram. It has certain advantages over nuclear perfusion imaging in terms of cost and convenience. The recent addition of Arbutamine echocardiography (which has been shown to be comparable to digital subtraction echocardiogram) provides another alternative method for pharmacologic stress testing. Continued improvement in echocardiographic image quality and the development of new technologies such as tissue harmonic imaging and contrast echocardiography will hopefully improve the echocardiographic evaluation of wall motion therefore increasing the diagnostic accuracy of echocardiographic stress testing.