β-adrenergic receptor

阿普洛尔（口服，50 mg/kg）可显着降低清醒肾高血压犬的血压，平均降低 20 mm Hg，并增加心率，平均 39 次/分钟（3 小时）[1]。 Alprenolol (ip, 5 mg/kg) 有效抑制吲哚美辛和伊沙匹隆的抗焦虑作用，同时对运动活动没有影响 吲哚美辛和伊沙匹隆的抗焦虑作用，但不会降低成年雄性 Swiss Webster 小鼠的运动活动[2 ]. 阿普洛尔（静脉注射，0.5或1.0 mg/kg）可使心率降低23次/分钟，舒张压降低10毫米汞柱，收缩压降低10毫米汞柱。猫的肝脏和心肌血流量在 1.0 mg/kg 剂量下分别轻微减少 15% 和 17%[3]。

在神志清醒的肾性高血压犬中，口服盐酸阿普洛尔（50 mg/kg）可显着降低血压，平均下降 20 mm Hg，心率增加每分钟 39 次（3 小时）[1]。在成年雄性 Swiss Webster 小鼠中，盐酸阿普洛尔（腹腔注射，5 mg/kg）不会降低运动活性，但能有效阻断吲哚美辛和伊沙匹隆的抗焦虑作用[2]。猫的心率每分钟下降23次，剂量为1.0mg/kg时，猫的心肌和肝脏血流量平均分别减少17%和15%。阿普拉洛尔（静脉注射，0.5 或 1.0 mg/kg）可使收缩压平均降低 10 mm Hg，舒张压平均降低 10 mm Hg）盐酸盐。

The effects of pindolol, 10 mg/kg, alprenolol, 50 mg/kg, and practolol, 50 mg/kg, given by mouth, on blood pressure and heart rate were investigated over a 24-hr period in 5 conscious renal hypertensive dogs, using a cross-over design. Pindolol and alprenolol caused significant falls in blood pressure which averaged 22 mm Hg (at 3-hr after p.o. administration) and 20 mm Hg (at 3-hr). However, practolol failed to produce any significant changes in blood pressure. Heart rate increased by 67 beats/min (at 1-hr) and 39 beats/min (at 3-hr) after pindolol and alprenolol, respectively, but did not show any significant increase when practolol was given orally. The pindolol-induced tachycardia and hypotension were not suppressed significantly by propranolol (1 mg/kg i.v.) which blocked completely the tachycardia and hypotension induced by isoprenaline (3 mg/kg p.o.). The hypotension and tachycardia observed after oral administration of D-32 (50 mg/kg) or after intravenous infusion of p-OH D-32 (1 mg/kg per min for 5 min) were also not modified significantly by propranolol (1 mg/kg i.v.). Based on these results and other published data, mechanisms pertaining to the hypotension exerted by beta-adrenoceptor blocking agents were discussed. [1]

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The systemic injection of diazepam (0.5 and 1.0 mg/kg), indorenate (5 and 10 mg/kg) and ipsapirone (2.5 and 5.0 mg/kg) reduced anxiety as tested in an exploratory avoidance model in mice. The injection of pindolol (2.0 mg/kg), alprenolol (5.0 mg/kg) or methiotepin (0.25 mg/kg) effectively prevented the anxiolytic action of indorenate and ipsapirone. The combined treatment of the antagonists with indorenate or ipsapirone did not reduce the motor activity, therefore suggesting that the inhibition of exploratory behaviour, after such combinations, was not mediated through a general motor impairment. Neither diazepam nor indorenate alone modified the motor activity; ipsapirone (5 and 2.5 mg/kg), however, reduced ambulation. This reduction was also prevented by administering pindolol, alprenolol or methiotepin. These observations suggest that the anxiolytic actions of indorenate and ipsapirone are mediated via stimulation of the 5-HT1A like receptor subtype. [2]

Metabolism / Metabolites
Hepatic. One of the active metabolites, 4-OH-alprenolol, is an active beta-blocker.

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Biological Half-Life
2-3 hours

Protein Binding
80-90%

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women LDLo oral 210 mg/kg Ugeskrift for Laeger. Doctor's Weekly., 139(2817), 1977 [PMID:595169]
mouse LD50 intraperitoneal 90 mg/kg European Journal of Medicinal Chemistry--Chimie Therapeutique., 18(151), 1983
mouse LD50 intravenous 20 mg/kg AUTONOMIC NERVOUS SYSTEM: SYMPATHOMIMETIC Arzneimittel-Forschung. Drug Research., 27(1022), 1977 [PMID:18157]
mammal (species unspecified) LD50 oral 184 mg/kg Pharmaceutical Chemistry Journal, 8(137), 1974
mammal (species unspecified) LD50 intraperitoneal 102 mg/kg Pharmaceutical Chemistry Journal, 8(137), 1974

[1]. Effects of beta-adrenoceptor blocking agents, pindolol, alprenolol and practolol on blood pressure and heart rate in conscious renal hypertensive dogs. Arch Int Pharmacodyn Ther. 1977 Jan;225(1):152-65.

[2]. Evidence for the involvement of the 5-HT1A receptor in the anxiolytic action of indorenate and ipsapirone. Psychopharmacology (Berl). 1990;101(3):354-8.

[3]. Myocardial and haemodynamic effects of the beta-adrenoceptor blocking drug alprenolol (H56/28) in anaesthetized cats. Br J Pharmacol. 1969 Oct;37(2):357-66.

C22H29NO4

371.47

371.20965

C, 71.13; H, 7.87; N, 3.77; O, 17.23

67824-72-0

67824-72-0 (benzoate); 15020-61-8; 13707-88-5 (HCl); 15020-61-8; 15020-61-8 (HCl R-isomer); 13707-88-5; 15132-12-4 (HCl S-isomer); 16768-36-8; 21378-88-1 (tartrate); 23846-72-2; 100897-05-0 (tartrate R-isomer); 23846-71-1; 16768-36-8 (tartrate S-isomer); 13655-52-2; 23846-72-2

9951320

Typically exists as solids at room temperature

O(C1C=CC=CC=1CC=C)CC(CNC(C)C)O.OC(C1C=CC=CC=1)=O

URFIUJMADXJBKL-UHFFFAOYSA-N

InChI=1S/C15H23NO2.C7H6O2/c1-4-7-13-8-5-6-9-15(13)18-11-14(17)10-16-12(2)3;8-7(9)6-4-2-1-3-5-6/h4-6,8-9,12,14,16-17H,1,7,10-11H2,2-3H3;1-5H,(H,8,9)

benzoic acid;1-(propan-2-ylamino)-3-(2-prop-2-enylphenoxy)propan-2-ol

Alprenolol benzoate; 67824-72-0; UNII-T3H696761C; T3H696761C; 1-(2-allylphenoxy)-3-(isopropylamino)propan-2-ol benzoate; SCHEMBL9267485; C07AA01; ALPRENOLOL BENZOATE [MART.];

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples

注意: 如下所列的是一些常用的体内动物实验溶解配方，主要用于溶解难溶或不溶于水的产品（水溶度<1 mg/mL）。 建议您先取少量样品进行尝试，如该配方可行，再根据实验需求增加样品量。

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注射用配方1: DMSO : Tween 80： Saline = 10 : 5 : 85 (如： 100 μL DMSO → 50 μL Tween 80 → 850 μL Saline)
*生理盐水/Saline的制备：将0.9g氯化钠/NaCl溶解在100 mL ddH ₂ O中，得到澄清溶液。
注射用配方 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (如： 100 μL DMSO → 400 μL PEG300 → 50 μL Tween 80 → 450 μL Saline)
注射用配方 3: DMSO : Corn oil = 10 : 90 (如： 100 μL DMSO → 900 μL Corn oil)
示例: 以注射用配方 3 (DMSO : Corn oil = 10 : 90) 为例说明, 如果要配制 1 mL 2.5 mg/mL的工作液, 您可以取 100 μL 25 mg/mL 澄清的 DMSO 储备液，加到 900 μL Corn oil/玉米油中, 混合均匀。

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注射用配方 4: DMSO : 20% SBE-β-CD in Saline = 10 : 90 [如：100 μL DMSO → 900 μL (20% SBE-β-CD in Saline)]
*20% SBE-β-CD in Saline的制备（4°C，储存1周）：将2g SBE-β-CD (磺丁基-β-环糊精) 溶解于10mL生理盐水中，得到澄清溶液。
注射用配方 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (如： 500 μL 2-Hydroxypropyl-β-cyclodextrin (羟丙基环胡精)→ 500 μL Saline)
注射用配方 6: DMSO : PEG300 : Castor oil : Saline = 5 : 10 : 20 : 65 (如： 50 μL DMSO → 100 μL PEG300 → 200 μL Castor oil → 650 μL Saline)
注射用配方 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (如： 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
注射用配方 8: 溶解于Cremophor/Ethanol (50 : 50), 然后用生理盐水稀释。
注射用配方 9: EtOH : Corn oil = 10 : 90 (如： 100 μL EtOH → 900 μL Corn oil)
注射用配方 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (如： 100 μL EtOH → 400 μL PEG300 → 50 μL Tween 80 → 450 μL Saline)

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口服配方 1: 悬浮于0.5% CMC Na (羧甲基纤维素钠)
口服配方 2: 悬浮于0.5% Carboxymethyl cellulose (羧甲基纤维素)
示例: 以口服配方 1 (悬浮于 0.5% CMC Na)为例说明, 如果要配制 100 mL 2.5 mg/mL 的工作液, 您可以先取0.5g CMC Na并将其溶解于100mL ddH2O中，得到0.5%CMC-Na澄清溶液；然后将250 mg待测化合物加到100 mL前述 0.5%CMC Na溶液中，得到悬浮液。

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口服配方 3: 溶解于 PEG400 (聚乙二醇400)
口服配方 4: 悬浮于0.2% Carboxymethyl cellulose (羧甲基纤维素)
口服配方 5: 溶解于0.25% Tween 80 and 0.5% Carboxymethyl cellulose (羧甲基纤维素)
口服配方 6: 做成粉末与食物混合

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注意: 以上为较为常见方法，仅供参考， InvivoChem并未独立验证这些配方的准确性。具体溶剂的选择首先应参照文献已报道溶解方法、配方或剂型，对于某些尚未有文献报道溶解方法的化合物，需通过前期实验来确定（建议先取少量样品进行尝试），包括产品的溶解情况、梯度设置、动物的耐受性等。

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请根据您的实验动物和给药方式选择适当的溶解配方/方案：
1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液));
2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方):
10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline);
假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL；
3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例;
4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶;
5、为保证最佳实验结果，工作液请现配现用！
6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们;
7、 以上所有助溶剂都可在 Invivochem.cn网站购买。