Pamatolol
(Synonyms: 氨甲酯心定) 目录号 : GC32532
Pamatolol是一种心选择性的beta-adrenoceptor拮抗剂，没有拟交感活性。
Cas No.:59110-35-9
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
Animal experiment: | Three male Sprague-Dawley rats weighing 200-250 g are given pamatolol-sulphate dissolved in water at a dose of 50 mg/kg (10 μCi/mg) by means of a stomach tube. The rats are housed in metabolic cages that allows for separate collection of urine and feces for a 24 hr period. They are given a commercial pellet diet and drinking water ad libitum. |
References: [1]. Hoffmann KJ, et al. Species differences in the metabolism of pamatolol, a cardioselective beta--adrenoceptor antagonist. Eur J Drug Metab Pharmacokinet. 1979;4(3):163-73. | |
Pamatolol is a cardioselective beta-adrenoceptor antagonist without sympathomimetic activity.
Pamatolol is well absorbed in the gastro-intestinal tract and excreted in the urine of man, dogs, rats and mice after oral administration, mainly in unchanged form, within 24 hrs[1].
[1]. Hoffmann KJ, et al. Species differences in the metabolism of pamatolol, a cardioselective beta--adrenoceptor antagonist. Eur J Drug Metab Pharmacokinet. 1979;4(3):163-73.
| Cas No. | 59110-35-9 | SDF | |
| 别名 | 氨甲酯心定 | ||
| Canonical SMILES | O=C(OC)NCCC1=CC=C(OCC(O)CNC(C)C)C=C1 | ||
| 分子式 | C16H26N2O4 | 分子量 | 310.39 |
| 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 | 3.2218 mL | 16.1088 mL | 32.2175 mL |
| 5 mM | 0.6444 mL | 3.2218 mL | 6.4435 mL |
| 10 mM | 0.3222 mL | 1.6109 mL | 3.2218 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。
Pamatolol: phase I evaluation of the pharmacodynamics of a cardioselective beta adrenoceptor blocking drug
Clin Pharmacol Ther 1978 Aug;24(2):168-74.PMID:28193DOI:10.1002/cpt1978242168.
A Phase I evaluation of a new adrenoceptor blocker, Pamatolol, was performed in 10 healthy male volunteers. Minor reductions in standing and exercise and isoproterenol-induced increases in heart rate were observed with the 10-mg oral dose and appeared maximal with the 400-600 mg dose. The rate of decline of effect averaged 1.5% of the exercise heart rate/hr. Neither resting systolic time intervals nor post-exercise pulmonary function was affected by this dose range of Pamatolol. Based on the latter responses and the isoproterenol dose response curve, we tentatively conclude that Pamatolol is relatively cardioselective in man.
Species differences in the metabolism of Pamatolol, a cardioselective beta--adrenoceptor antagonist
Eur J Drug Metab Pharmacokinet 1979;4(3):163-73.PMID:43252DOI:10.1007/BF03189420.
The metabolism of Pamatolol was studied in man, dogs, rats and mice after oral administration of a single dose. The drug was well absorbed in the gastro-intestinal tract and excreted in the urine, mainly in unchanged form, within 24 hrs. Four urinary metabolites were identified by gas chromatographic-mass spectrometric techniques. The metabolic data, in man, dog and mouse was found to be similar, both qualitatively and quantitatively. One metabolism route, involving aliphatic hydroxylation and subsequent oxidation, was found, to a significant extent only in the rat. The species variation between the mouse and the rat with regard to long-term toxicity of Pamatolol is discussed. Artefact formation during trace analysis was observed.
Effects of atenolol, metroprolol, and Pamatolol on cardiac and vascular beta-adrenoceptors in the rat
J Cardiovasc Pharmacol 1979 May-Jun;1(3):287-98.PMID:94397DOI:10.1097/00005344-197905000-00002.
Three beta-adrenoceptor antagonists--atenolol (A), metoprolol (M), and Pamatolol (P)--were examined with respect to their effects on isoproterenol responses of isolated right atria and portal veins from rats. With all three blockers at concentrations of 10(-7), 10(-6), and 10(-5) M, the chronotropic atrial responses indicated a linear relation with slope of 1 for log (dose ratio - 1) versus log[blocker]. The following pA2 values were obtained: A = 7.14, M = 7.51, P = 7.56. Inhibition of spontaneous contractions in portal veins by isoproterenol was studied after alpha-adrenoceptor blockade by phenoxybenzamine. The beta-adrenoceptor antagonists were used at 10(-6), 10(-5), and 10(-4) M in these experiments. Only with P did the relation log (dose ratio-1) versus log[blocker] show a slope near unity, whereas A and M gave slopes significantly less than 1. Intercepts of the regression lines with the abscissa corresponded to pA2 values of A = 6.01, M = 6.51, P = 5.54. The results indicate that all three substances are "cardioselective" beta-adrenoceptor antagonists devoid of intrinsic beta-stimulatory action. A and M show a comparable degree of cardioselectivity, whereas P is more selective.
Kinetics of Pamatolol, a cardioselective beta adrenoreceptor blocker
Clin Pharmacol Ther 1979 Dec;26(6):682-5.PMID:40725DOI:10.1002/cpt1979266682.
The systemic bioavailability, elimination half-life (t1/2), and plasma concentration--response relationships of Pamatolol, a relatively cardioselective beta adrenoceptor blocker, have been measured in healthy subjects. Pamatolol is rapidly and completely absorbed after oral dosing. Elimination t1/2 ranged from 2.9 to 4.6 hr after oral doses and from 2.2 to 5.6 hr after intravenous doses. There was a clear relationship between log plasma Pamatolol concentration and sympathetic blockade assessed by reduction of exercise heart rate. Concentration-response curves were essentially identical after oral and intravenous doses. There is no evidence of a first-pass effect, nor is there any evidence of metabolite activity.
Characteristics of the lipolytic beta-adrenergic receptors in hamster adipocytes
Biochim Biophys Acta 1982 Oct 14;713(1):80-5.PMID:6128033DOI:10.1016/0005-2760(82)90169-2.
Hamster adipocyte beta-adrenergic receptors were characterized by the effect on the lipolysis rate of several selective beta-adrenergic agonists and antagonists. Prenalterol and procaterol, selective beta 1- and beta 2-agonists, respectively, both stimulated the lipolysis rate half-maximally at 1-2 microM, a concentration approximately 100-fold higher than that needed for half-maximal stimulation by isoprenaline. The maximal procaterol effect was similar to that of isoprenaline, while the effect of prenalterol was 40% lower. Submaximally isoprenaline-stimulated lipolysis was half-maximally inhibited by propranolol at 0.2 microM and by atenolol and H 35/25, selective beta 1- and beta 2-antagonists, at 23 and 6 microM concentration, respectively. Highly specific beta 1 and beta 2 stimulation was induced by incubation with prenalterol or procaterol, with simultaneous maximal selective beta 2 or beta 1 inhibition, respectively. The maximal beta 2 stimulation was approximately twice the corresponding beta 1 effect under these conditions, the sum of both effects closely approaching that of maximal nonselective beta-adrenergic stimulation with isoprenaline. Similar results were obtained with the selective beta 2-antagonist, ICI 118,551, or the beta 1-antagonists, Pamatolol and practolol. The findings are most easily explained by the existence of a heterogeneous beta 1- and beta 2-adrenergic receptor population on hamster adipocytes.