Fenoterol
(Synonyms: Phenoterol) 目录号 : GC25412Fenoterol (Phenoterol) is a β2 adrenoreceptor agonist with bronchodilator activity.
Cas No.:13392-18-2
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
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- Purity: >98.00%
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- Datasheet
Fenoterol (Phenoterol) is a β2 adrenoreceptor agonist with bronchodilator activity.
[1] Svedmyr N, et al. Pharmacotherapy. 1985, 5(3):109-26.
| Cas No. | 13392-18-2 | SDF | Download SDF |
| 别名 | Phenoterol | ||
| 分子式 | C17H21NO4 | 分子量 | 303.35 |
| 溶解度 | 储存条件 | Store at 2-8°C,protect from light | |
| 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 | 3.2965 mL | 16.4826 mL | 32.9652 mL |
| 5 mM | 0.6593 mL | 3.2965 mL | 6.593 mL |
| 10 mM | 0.3297 mL | 1.6483 mL | 3.2965 mL |
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| 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 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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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，
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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。
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Fenoterol: a review of its pharmacological properties and therapeutic efficacy in asthma
Drugs 1978 Jan;15(1):3-32.PMID:342228DOI:10.2165/00003495-197815010-00002.
Fenoterol, the 4-hydroxyphenyl derivative of orciprenaline, is a resorcinol derivative with relatively high selectivity for beta2-adrenoceptors. It is active in man after inhalation or oral administration and is indicated in the treatment of bronchospasm associated with asthma, bronchitis and other obstructive airway diseases. Clinical experience has shown that Fenoterol is an effective bronchodilator with negligible effects on the cardiovascular system following aerosol administration of usual therapeutic doses. In children, inhaled Fenoterol is effective in preventing exercise-induced asthma and administration of the aerosol in young children has been successfully used to terminate acute asthma attacks. In trials in adults, inhaled Fenoterol was superior to placebo. In other controlled studies, it showed a tendency to cause a slightly greater maximum improvement in airway function as assessed spirometrically, and to have a longer duration of action than inhaled orciprenaline, salbutamol or terbutaline, although in these trials statistically significant differences were often not found. The onset of maximum effect is less rapid than with isoprenaline but is longer lasting. About 60% of the eventual maximum response to Fenoterol is reached in the first few minutes after inhalation. Oral Fenoterol is more effective than placebo, ephedrine or orciprenaline, and probably similar to salbutamol and terbutaline. Following usual aerosol doses, side-effects are minimal. Oral administration is associated with a higher incidence of side-effects than inhalation, including fine muscle tremor and tachycardia.
Validation of Fenoterol to Study β2-Adrenoceptor Function in the Rat Urinary Bladder
Pharmacology 2022;107(1-2):116-121.PMID:34781292DOI:10.1159/000519720.
Fenoterol is a β2-adrenoceptor (AR)-selective agonist that is commonly used to investigate relaxation responses mediated by β2-AR in smooth muscle preparations. Some data have questioned this because Fenoterol had low potency in the rat urinary bladder when a muscarinic agonist was used as a pre-contraction agent and because some investigators proposed that Fenoterol may act in part via β3-AR. We designed the present study to investigate whether Fenoterol is a proper pharmacological tool to study β2-AR-mediated relaxation responses in the rat urinary bladder. Firstly, we have compared the effect of pre-contraction agents on Fenoterol potency and found that Fenoterol potency was about 1.5 log units greater against KCl than carbachol (pEC50 7.19 ± 0.66 and 5.62 ± 1.09 of KCl and of carbachol, respectively). To test the selectivity of Fenoterol, we have determined the effects of the β2-AR antagonist ICI 118,551 and the β3-AR antagonist L 748,337 on relaxation responses to Fenoterol. While 300 nM L 748,337 had little effect on the potency of Fenoterol (pEC50 6.56 ± 0.25 and 6.33 ± 0.61 in the absence and presence of L 748,337, respectively), the relaxation curve for Fenoterol was right-shifted in the presence 300 nM ICI 118,551 (pEC50 5.03 ± 0.18). Thus, we conclude that Fenoterol is a proper pharmacological tool to assess β2-AR-mediated responses in the rat urinary bladder and most likely in other smooth-muscle preparations containing multiple subtypes of the β-AR.
Fenoterol: a beta2-adrenergic agonist for use in asthma. Pharmacology, pharmacokinetics, clinical efficacy and adverse effects
Pharmacotherapy 1985 May-Jun;5(3):109-26.PMID:2991865DOI:10.1002/j.1875-9114.1985.tb03409.x.
Fenoterol (hydroxyphenylorciprenaline) is chemically closely related to metaproterenol (orciprenaline). It has a higher bronchodilating potency than metaproterenol, albuterol (salbutamol in Europe) or terbutaline. The beta 2 selectivity of Fenoterol at normal oral and inhaled doses is the same as for albuterol and terbutaline. Its pharmacodynamic effects are similar to those of other selective beta 2-adrenoceptor agonists. It has a high first-pass metabolism. The long half-life previously reported in the literature (7 hours) is mainly the half-life of inactive Fenoterol metabolites. The duration of action at equipotent bronchodilating doses seems to be the same as for albuterol and terbutaline, and not longer, as previously reported. Inhalation of beta-adrenoceptor agonists is the superior route of administration. Side effects do not usually occur at normal therapeutic doses. One puff of Fenoterol (200 micrograms) is about equipotent to 2 puffs of albuterol (2 X 100 micrograms) or 2 puffs of terbutaline (2 X 250 micrograms) with the same duration of effect. In patients who overdose with the metered-dose inhaler (MDI), side effects occur at half the number of puffs with Fenoterol. Dosage for an acute attack in children is 1 puff (200 micrograms), repeated within 5 minutes if necessary; in adults 1-3 puffs can be given. For maintenance therapy, the dose in adults is 1-2 puffs 2-4 times daily, while in children 1 puff at night and 1 in the morning may be sufficient. The usual oral dosage has been 5-10 mg 3 times daily.
Pharmacokinetic/pharmacodynamic characteristics of the beta-2-agonists terbutaline, salbutamol and Fenoterol
Int J Clin Pharmacol Ther Toxicol 1992 Sep;30(9):342-62.PMID:1358833doi
The clinical pharmacokinetics and pharmacokinetic/dynamic properties of the beta-adrenergic drugs Fenoterol, salbutamol and terbutaline are reviewed. Sulfate conjugates are the main metabolites in man. The protein binding of these derivatives is rather weak with most pronounced binding observed e.g. Fenoterol (40%). Disposition after parenteral administration shows a multi-exponential behavior for all the substances with linear but also stereo-selective pharmacokinetics. After parenteral administration, the drugs are mainly eliminated by renal processes while after oral administration a pronounced metabolic clearance (high first pass effect) is responsible for a low bioavailability, especially for Fenoterol (2%). The total clearance for Fenoterol is about twice that of salbutamol and terbutaline. Seven to 15% of the delivered aerosol reach typically the systemic circulation. In patients with respiratory disorders, pulmonary absorption is however highly dependent on the disease state. Pharmacokinetics in children do not significantly differ from adults when expressed per kg body weight. Patients with renal failure but not asthmatics show changed pharmacokinetic profiles. Only insignificant interactions with other drugs have been found. Pharmacokinetic/dynamic modeling approaches indicated that Fenoterol is 25 times more active at the site of action than salbutamol and terbutaline, but all three drugs show similar bronchopulmonary selectivities. When the overall clinical activity, determined by pharmacokinetic and dynamic properties is compared, the activity gap is reduced: Fenoterol (8) greater than salbutamol (2) greater than terbutaline (1). Differences in the first pass effect even inverse the pattern after oral administration. PK/PD modeling quantified the pulmonary effect after inhalation and suggested that the higher incidence of side effects for Fenoterol might be linked to an overdosing problem. The application of PK/PD principles may improve the clinical usage and therapy of beta-2-adrenergic drugs.
Effect of Fenoterol stereochemistry on the β2 adrenergic receptor system: ligand-directed chiral recognition
Chirality 2011;23 Suppl 1(Suppl 1):E1-6.PMID:21618615DOI:10.1002/chir.20963.
The β(2) adrenergic receptor (β(2)-AR) is a model system for studying the ligand recognition process in G protein-coupled receptors. Fenoterol (FEN) is a β(2)-AR selective agonist that has two centers of chirality and exists as four stereoisomers. Radioligand binding studies determined that stereochemistry greatly influences the binding affinity. Subsequent Van't Hoff analysis shows very different thermodynamics of binding depending on the stereoconfiguration of the molecule. The binding of (S,x')-isomers is almost entirely enthalpy controlled whereas binding of (R,x')-isomers is purely entropy driven. Stereochemistry of FEN molecule also affects the coupling of the receptor to different G proteins. In a rat cardiomyocyte contractility model, (R,R')-FEN was shown to selectively activate G(s) protein signaling while the (S,R')-isomer activated both G(i) and G(s) protein. The overall data demonstrate that the chirality at the two chiral centers of the FEN molecule influences the magnitude of binding affinity, thermodynamics of local interactions within the binding site, and the global mechanism of β(2)-AR activation. Differences in thermodynamic parameters and nonuniform G-protein coupling suggest a mechanism of chiral recognition in which observed enantioselectivities arise from the interaction of the (R,x')-FEN stereoisomers with a different receptor conformation than the one with which the (S,x')-isomer interacts.