D2343
目录号 : GC30665
D2343是一种β2肾上腺素能受体激动剂，也是一种α1-肾上腺素能受体抑制剂。
Cas No.:72734-63-5
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
D2343 is a β2-adrenoceptor agonist and also is an α1- adrenoceptor inhibitor.
D2343 is a compound with about the same beta 2-adrenoceptor-agonist effect as Terbutaline and exhibiting in addition an alpha 1-receptor inhibitory activity[1]. The beta 2-agonistic and alpha 1-antagonistic drug D2343 inhibits the evoked contractions in a concentration related fashion with 50% effect at 9.6 μM[2].
D2343 has been compared to the beta 2-agonist Terbutaline on oestrogenized uterine preparations from rat and rabbit and in myometrial strips from homo. D2343 has shown an ability to relax the uterine muscles to the same degree as Terbutaline or even more, especially when the two drugs are compared in preparations from rabbit and rat[1].
[1]. Olsson OA, et al. The effects in myometrial preparations of D2343, a beta 2-adrenoceptor agonist possessing alpha 1-receptor blocking qualities. Acta Pharmacol Toxicol (Copenh). 1984 Nov;55(5):391-7. [2]. Olsson OA, et al. The effect of D2343 in transmurally stimulated rabbit isthmus muscle. Acta Pharmacol Toxicol (Copenh). 1985 May;56(5):427-30.
| Cas No. | 72734-63-5 | SDF | |
| Canonical SMILES | OC(C1=CC=C(O)C=C1)CNC(C)(C)CCC2=C(C=CC=C2)OC | ||
| 分子式 | C20H27NO3 | 分子量 | 329.43 |
| 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 | 3.0355 mL | 15.1777 mL | 30.3555 mL |
| 5 mM | 0.6071 mL | 3.0355 mL | 6.0711 mL |
| 10 mM | 0.3036 mL | 1.5178 mL | 3.0355 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。
Effects of D2343, a new beta-mimetic drug, and terbutaline on spontaneous term labor
The effects of an intravenous bolus injection of D2343 (0.75 or 1 mg) or terbutaline (0.25 mg) on spontaneous term labor were studied. The uterine activity was recorded by a transducer-tipped intrauterine catheter and calculated electronically by an uterine activity integrator module built in a conventional fetal monitor. After drug administration the uterine activity was reduced to a similar extent with D2343 and terbutaline but the contractions were abolished for a longer time with terbutaline injection (mean of 9.3-9.8 min compared with 17.0 min). Maternal blood pressure was unaffected in both groups but the increase in pulse rate was slightly higher in the D2343 groups. D2343 seems to have an effect ratio between uterine inhibitory capacity and cardiovascular side effects similar to terbutaline.
A new beta 2-adrenoceptor agonist--D 2343--with long duration. Inhalation comparison with terbutaline in asthmatics
A new beta 2-adrenoceptor agonist D2343 has been shown in a human i.v. study to be less potent than terbutaline. Animal experiments showed an increased affinity to lung tissue and a longer bronchodilating effect than terbutaline when inhaled. In a randomized single-blind, crossover comparison, 2.5 and 5 mg D2343 and 5 mg terbutaline were inhaled by eight asthma patients. We found that 5 mg of D2343 was equipotent to 5 mg terbutaline in bronchodilatory effect measured with FEV1. The duration was longer with an increased bronchodilation (P less than 0.01) 6 h after D2343 inhalation compared with terbutaline. The mean fall in FEV1 3-6 h after inhalation was significantly greater with terbutaline than with D2343 (P less than 0.05). Thus, this study shows that inhaled D2343 has a longer bronchodilating effect than terbutaline.
The effects in myometrial preparations of D2343, a beta 2-adrenoceptor agonist possessing alpha 1-receptor blocking qualities
D2343 is a compound with about the same beta 2-adrenoceptor-agonist effect as terbutaline and exhibiting in addition an alpha 1-receptor inhibitory activity. D2343 has been compared to the beta 2-agonist terbutaline on oestrogenized uterine preparations from rat and rabbit (in vitro and in vivo) and in myometrial strips from homo. Generally, D2343 has shown an ability to relax the uterine muscles to the same degree as terbutaline or even more, especially when the two drugs were compared in vitro in preparations from rabbit and rat.
The effect of D2343 in transmurally stimulated rabbit isthmus muscle
In in vitro experiments spirally cut isthmic preparations from oestrogenized rabbits have been contracted by transmural stimulation. The beta 2-agonistic and alpha 1-antagonistic drug D2343 (for chemical structure, see fig. 1 in Olsson et al. 1984) inhibits the evoked contractions in a concentration related fashion with 50% effect at 9.6 X 10(-6) mol/l. The alpha 1-antagonist prazosin has an inhibiting action in the same concentration range (EC50 = 14.0 X 10(-6) mol/l). To inhibit the contractile response to the same degree by the beta 2-agonist terbutaline the concentration has to be greater than 10(-3) mol/l. From received results the beta (beta 2)-adrenoceptor mediated effects seem to be of minor importance compared to the alpha (alpha 1)-receptor dominance in the isthmus muscle during oestrus.
On the predictive value of experiments in vitro in the evaluation of the effect duration of bronchodilator drugs for local administration
Six bronchodilating beta-adrenoceptor agonists, clinically documented with respect to the duration of action after inhalation, were included in this study in vitro on the guinea-pig trachea. Relaxation of carbachol contracted trachea strip preparations and inhibition of contraction of a vagus nerve-tracheal tube preparation were measured. The relaxing effects of salbutamol and fenoterol (both with relatively short duration in man) were rapid in onset and easily reversed by washing in a drug-free medium. The relaxation by salmeterol (long duration) and D2343 (intermediate duration) developed more slowly, resisted washing but was reversed by propranolol. Formoterol (long duration) and salmefamol (intermediate duration) showed properties between these two extremes. All test compounds inhibited the vagally-induced contractions of tracheal concentration dependently. The EC50 values for the hydrophilic compounds salbutamol and fenoterol were higher with intra- as compared with extratracheal administration. For the more lipophilic compounds formoterol, salmefamol, salmeterol and D2343, this difference was less pronounced. A high lipophilicity and a retention by the tissue in vitro of a beta-adrenoceptor agonist may be factors contributing to a long effect duration after inhalation but a further selection has to be made in vivo since metabolic and circulatory effects may influence the effect kinetics.