Ketanserin

製品コードS2232 バッチS223201

印刷

化学情報

Chemical Structure Synonyms R41468, Ketanserinum Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C22H22FN3O3
分子量 395.43 CAS No. 74050-98-9
Solubility (25°C)* 体外 DMSO 2 mg/mL (5.05 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 Ketanserin (R41468, Ketanserinum) is a specific 5-HT2A serotonin receptor antagonist with Ki of 2.5 nM for rat and human 5-HT2A, used as an antihypertensive drug.
in vitro

Ketanserin causes a dose-dependent inhibition on the contractile responses to 5-hydroxytryptamine of isolated rat caudal artery, canine basilar, carotid, coronary and gastrosplenic arteries, canine gastrosplenic veins and canine saphenous veins. Ketanserin inhibits the contractions of rat caudal arteries and canine saphenous veins caused by postjunctional alpha adrenergic activation. Ketanserin depresses and in certain experiments reverses the vasoconstrictor response to 5-hydroxytryptamine in the perfused guinea-pig stomach. [1] Ketanserin is found to attenuate the excitatory responses produced by norepinephrine, an alpha 1-adrenoceptor-mediated response, in the lateral geniculate nucleus. Ketanserin potentiates rather than attenuates, the inhibitory effect of 5-HT in the lateral geniculate nucleus. [2] Ketanserin significantly prolongs action potential duration (APD) at 50% repolarization by 218% and APD at 90% repolarization by 256% with no significant effect on other action potential parameters in rat ventricular myocytes. Ketanserin results in a concentration- and time-dependent inhibition of charge area of Ito evaluated by integration with an EC50 of 8.3 μM. Ketanserin also blocks Ito and sustained current (ISus) in a dose-dependent manner with an EC50 of 11.2 μM and has no significant effect on both the inward rectifier potassium current and the L-type calcium current. [3]
in vivo

Ketanserin produces dose-dependent antinociception in the hot-plate and acetic acid-induced writhing tests with ED50 values (95% confidence limit) of 1.51 and 0.62 mg/kg, respectively, but is without any significant effect on the tail-flick test. [4]

プロトコル(参考用のみ)

カスタマーフィードバック

Data from [Data independently produced by , , Neurosignals, 2017, 25(1):39-53]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Serotonin-induced vascular permeability is mediated by transient receptor potential vanilloid 4 in the airways and upper gastrointestinal tract of mice [ Lab Invest, 2021, 1-14] PubMed: 33859334
Serotonin receptors 5-HTR2A and 5-HTR2B are involved in cigarette smoke-induced airway inflammation, mucus hypersecretion and airway remodeling in mice. [ Int Immunopharmacol, 2019, 10.1016/j.intimp.2019.106036] PubMed: 31787571
Antiproliferative activities of the second-generation antipsychotic drug sertindole against breast cancers with a potential application for treatment of breast-to-brain metastases. [ Sci Rep, 2018, 8(1):15753] PubMed: 30361678
Stimulation of Anxiety-Like Behavior via ERK Pathway by Competitive Serotonin Receptors 2A and 1A in Post-Traumatic Stress Disordered Mice. [ Neurosignals, 2017, 25(1):39-53] PubMed: 28977803

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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