beta-adrenergic receptors; 5-HT1A 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]

---

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.

---

Biological Half-Life
2-3 hours

Protein Binding
80-90%

---

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.

One of the ADRENERGIC BETA-ANTAGONISTS used as an antihypertensive, anti-anginal, and anti-arrhythmic agent.

C15H24CLNO2

285.8096

285.149

13707-88-5

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

66368

White to off-white solid powder

1.007g/cm3

383.4ºC at 760 mmHg

108ºC

185.7ºC

3.345

41.49

3

3

8

19

231

0

PAZJSJFMUHDSTF-UHFFFAOYSA-N

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

1-(propan-2-ylamino)-3-(2-prop-2-enylphenoxy)propan-2-ol

Gubernal; Regletin; Yobir; Alprenolol hydrochloride; 13707-88-5; Alprenolol HCl; Apllobal; Dimacor; Gubernal; Regletin; Aptine; Apllobal; Alfeprol; Alpheprol; Yobir; Alprenololum; Alpheprol; Aptin; Duriles; Aptin-Duriles; Aptina ; Aptin; Duriles; Aptine

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

注意： 请将本产品存放在密封且受保护的环境中，避免吸湿/受潮。

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

DMSO : ~100 mg/mL (~349.88 mM)
H2O : ~50 mg/mL (~174.94 mM)

配方 1 中的溶解度: 2.08 mg/mL (7.28 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (这些助溶剂从左到右依次添加，逐一添加), 悬浮液；超声助溶。
例如，若需制备1 mL的工作液，可将100 μL 20.8 mg/mL澄清DMSO储备液加入400 μL PEG300中，混匀；然后向上述溶液中加入50 μL Tween-80，混匀；加入450 μL生理盐水定容至1 mL。
*生理盐水的制备：将 0.9 g 氯化钠溶解在 100 mL ddH₂O中，得到澄清溶液。

---

配方 2 中的溶解度: ≥ 2.08 mg/mL (7.28 mM) (饱和度未知) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将 100 μL 20.8 mg/mL澄清DMSO储备液加入900 μL 20% SBE-β-CD生理盐水溶液中，混匀。
*20% SBE-β-CD 生理盐水溶液的制备（4°C，1 周）：将 2 g SBE-β-CD 溶解于 10 mL 生理盐水中，得到澄清溶液。

---

View More

配方 3 中的溶解度: ≥ 2.08 mg/mL (7.28 mM) (饱和度未知) in 10% DMSO + 90% Corn Oil (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将 100 μL 20.8 mg/mL 澄清 DMSO 储备液加入到 900 μL 玉米油中并混合均匀。

---

配方 4 中的溶解度: 11 mg/mL (38.49 mM) in PBS (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液; 超声助溶.

---

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。