5-HT_1A 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]。

阿普洛尔（口服，50 mg/kg）可使清醒的肾高血压犬的血压显着下降，平均下降 20 mm Hg（3 小时），心率增加 39 次/分钟（3 小时）。 1]。阿普洛尔（腹腔注射，5 mg/kg）可有效阻断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）可使收缩压平均降低 10 mm Hg，舒张压平均降低 10 mm Hg），心率降低 23 次/分，并轻微降低心肌收缩力。剂量为 1.0 mg/kg 时，猫的肝脏血流量平均分别减少 17% 和 15%[3]。

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.

Alprenolol is a secondary alcohol that is propan-2-ol substituted by a 2-allylphenoxy group at position 1 and an isopropylamino group at position 3. It is a beta-adrenergic antagonist used as a antihypertensive, anti-arrhythmia and a sympatholytic agent. It has a role as an anti-arrhythmia drug, an antihypertensive agent, a beta-adrenergic antagonist and a sympatholytic agent. It is a secondary alcohol and a secondary amino compound.
One of the adrenergic beta-antagonists used as an antihypertensive, anti-anginal, and anti-arrhythmic agent. Alprenolol is no longer marketed by AstraZeneca, but may still be available in generic varieties.
One of the ADRENERGIC BETA-ANTAGONISTS used as an antihypertensive, anti-anginal, and anti-arrhythmic agent.

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Drug Indication
For the treatment of hypertension, angina, and arrhythmia

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Mechanism of Action
Alprenolol non-selectively blocks beta-1 adrenergic receptors mainly in the heart, inhibiting the effects of epinephrine and norepinephrine resulting in a decrease in heart rate and blood pressure. Also, with a more minor effect, by binding beta-2 receptors in the juxtaglomerular apparatus, alprenolol inhibits the production of renin, thereby inhibiting angiotensin II and aldosterone production and therefore inhibits the vasoconstriction and water retention due to angiotensin II and aldosterone, respectively.

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Pharmacodynamics
Alprenolol is a non-selective beta-blocker used in the treatment of hypertension, edema, ventricular tachycardias, and atrial fibrillation. Alprenolol impairs AV node conduction and decreases sinus rate and may also increase plasma triglycerides and decrease HDL-cholesterol levels. Alprenolol is nonpolar and hydrophobic, with low to moderate lipid solubility. Alprenolol has little to no intrinsic sympathomimetic activity and, unlike some other beta-adrenergic blocking agents, alprenolol has little direct myocardial depressant activity and does not have an anesthetic-like membrane-stabilizing action.

C₁₅H₂₃NO₂

249.35

249.173

C, 72.25; H, 9.30; N, 5.62; O, 12.83

13655-52-2

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

2119

White to off-white solid powder

1.007g/cm3

383.4ºC at 760mmHg

57.5°C

185.7ºC

1.46E-06mmHg at 25°C

1.5250 (estimate)

2.543

41.49

2

3

8

18

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

(RS)-Alprenolol; dl-Alprenolol; alprenolol; 13655-52-2; Alpheprol; Alfeprol; Alprenololum; Alfeprol [Russian]; Alprenololum [INN-Latin]; Alprenolol [INN:BAN]; Alprenolol

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

注意： 该产品在溶液状态不稳定，请现配现用。

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 (~401.4 mM)
H2O: ~0.7 mg/mL (~2.7 mM)

配方 1 中的溶解度: ≥ 2.5 mg/mL (10.03 mM) (饱和度未知) 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), 澄清溶液。
例如，若需制备1 mL的工作液，可将100 μL 25.0 mg/mL澄清DMSO储备液加入到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。

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配方 2 中的溶解度: ≥ 2.5 mg/mL (10.03 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 25.0 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。

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配方 3 中的溶解度: ≥ 2.5 mg/mL (10.03 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 25.0 mg/mL 澄清 DMSO 储备液加入到 900 μL 玉米油中并混合均匀。

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配方 4 中的溶解度: 4 mg/mL (16.04 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 (<60°C).

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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。