β2-adrenergic receptor ( IC50 = 8930 nM )
β2-adrenoceptor [3]

在分离的豚鼠慢肌（比目鱼肌）和快肌（趾长伸肌，EDL）骨骼肌中，硫酸沙丁胺醇（Salbutamol Sulfate，AH-3365；沙丁胺醇，Albuterol）（R,S-对映体）以浓度依赖方式增强不完全融合强直收缩的幅度。该效应在慢肌中更显著：1 μM使收缩幅度增加约25%，10 μM使收缩幅度增加约40%；在快肌中，10 μM仅使收缩幅度增加约20%。R-对映体是主要活性成分，S-对映体在浓度高达10 μM时仍无明显作用[1]

在年轻健康男性（18-30岁）中，口服硫酸沙丁胺醇（Salbutamol Sulfate，AH-3365；沙丁胺醇，Albuterol）（8 mg/天，分两次给药）连续7天，显著增加骨骼肌力量。与安慰剂相比，股四头肌最大等长收缩力增加约12%，等速收缩扭矩（60°/秒）增加约10%，未观察到肌肉质量的显著变化[3]
在健康男性受试者中，短期口服硫酸沙丁胺醇（Salbutamol Sulfate，AH-3365；沙丁胺醇，Albuterol）（4 mg/天，连续4天）改善运动耐力。在70%最大摄氧量（VO2max）的自行车功率计运动中，力竭时间增加约15%，股外侧肌糖原消耗速率降低。此外，它还增加运动期间的全身脂肪氧化（约20%），减少碳水化合物氧化（约12%）[2]

Guinea-pig skeletal muscle contraction assay: Adult guinea-pigs are sacrificed, and soleus (slow-twitch) and EDL (fast-twitch) muscles are dissected and mounted in organ baths containing oxygenated physiological saline at 37°C. Muscles are stimulated electrically with trains of pulses (20-50 Hz) to produce incompletely fused tetanic contractions. Salbutamol Sulfate (AH-3365; Albuterol) (0.1-10 μM) or its enantiomers are added to the bath, and contraction amplitude is recorded continuously for 30 minutes to assess dose-dependent effects [1]

Effects During Pregnancy and Lactation
◉ Summary of Use during Lactation
Although no published data exist on the use of albuterol by mouth or inhaler during lactation, data from the related drug, terbutaline, indicate that very little is expected to be excreted into breastmilk. The authors of several reviews and expert guidelines agree that use of inhaled bronchodilators is acceptable during breastfeeding because of the low bioavailability and maternal serum levels after use.
◉ Effects in Breastfed Infants
Relevant published information was not found as of the revision date.
◉ Effects on Lactation and Breastmilk
Relevant published information was not found as of the revision date.

[1]. Prior, C., M.B. Leonard, and J.R. McCullough, Effects of the enantiomers of R,S-salbutamol on incompletely fused tetanic contractions of slow- and fast-twitch skeletal muscles of the guinea-pig. Br J Pharmacol, 1998. 123(3): p. 558-64.

[2]. Effects of short-term oral salbutamol administration on exercise endurance and metabolism. J Appl Physiol (1985), 2000. 89(2): p. 430-6.

[3]. Salbutamol, a beta 2-adrenoceptor agonist, increases skeletal muscle strength in young men. Clin Sci (Lond), 1992. 83(5): p. 615-21.

Albuterol sulfate is an ethanolamine sulfate salt. It is functionally related to an albuterol.
Albuterol Sulfate is the sulfate salt of the short-acting sympathomimetic agent albuterol, a 1:1 racemic mixture of (R)-albuterol and (S)-albuterol with bronchodilator activity. Albuterol stimulates beta2-adrenergic receptors in the lungs, thereby activating the enzyme adenylate cyclase that catalyzes the conversion of ATP to cyclic-3',5'-adenosine monophosphate (cAMP). Increased cAMP concentrations relax bronchial smooth muscle, relieve bronchospasms, and reduce inflammatory cell mediator release, especially from mast cells. To a lesser extent albuterol stimulates beta1-adrenergic receptors, thereby increasing the force and rate of myocardial contraction.
A short-acting beta-2 adrenergic agonist that is primarily used as a bronchodilator agent to treat ASTHMA. Albuterol is prepared as a racemic mixture of R(-) and S(+) stereoisomers. The stereospecific preparation of R(-) isomer of albuterol is referred to as levalbuterol.
See also: Albuterol (broader); Albuterol sulfate; ipratropium bromide (component of); Albuterol sulfate; budesonide (component of).

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Salbutamol Sulfate (AH-3365; Albuterol) is a selective β2-adrenoceptor agonist with potent effects on skeletal muscle function [3]
Its mechanism of action involves activation of β2-adrenoceptors in skeletal muscle, leading to increased intracellular cAMP levels, which enhances muscle contraction force and modulates energy metabolism (promoting fat oxidation and sparing glycogen) [2][3]
The R-enantiomer (levalbuterol) is the pharmacologically active form, while the S-enantiomer has negligible β2-adrenoceptor activity [1]
It exhibits ergogenic effects in humans, including improved exercise endurance and increased skeletal muscle strength, without significant changes in muscle mass [2][3]

C13H23NO7S

337.39

576.271

C, 46.28; H, 6.87; N, 4.15; O, 33.19; S, 9.50

51022-70-9

Salbutamol; 18559-94-9

39859

White to off-white solid powder

419.2ºC at 760 mmHg

180 °C

250 °C

2.124

155.7

10

12

10

39

309

0

S(=O)(=O)(O[H])O[H].O([H])C([H])(C1C([H])=C([H])C(=C(C([H])([H])O[H])C=1[H])O[H])C([H])([H])N([H])C(C([H])([H])[H])(C([H])([H])[H])C([H])([H])[H].O([H])C([H])(C1C([H])=C([H])C(=C(C([H])([H])O[H])C=1[H])O[H])C([H])([H])N([H])C(C([H])([H])[H])(C([H])([H])[H])C([H])([H])[H]

OVICLFZZVQVVFT-UHFFFAOYSA-N

InChI=1S/C13H21NO3.H2O4S/c1-13(2,3)14-7-12(17)9-4-5-11(16)10(6-9)8-15;1-5(2,3)4/h4-6,12,14-17H,7-8H2,1-3H3;(H2,1,2,3,4)

4-[2-(tert-Butylamino)-1-hydroxyethyl]-2-(hydroxymethyl)phenol sulfuric acid salt

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)

配方 1 中的溶解度: 100 mg/mL (347.05 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。

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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。