Pentoxyverine-d8

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Pentoxyverine-d8 

Pentoxyverine-d8 是 Pentoxyverine 的氘代物。Pentoxyverine (Carbetapentane) 是 sigma-1 受体激动剂，在豚鼠脑膜上的 Ki 值为 75 nM。Pentoxyverine 是一种中枢性咳嗽抑制剂，具有抗毒蕈碱和抗惊厥作用。Pentoxyverine 可用于抑制支气管阻滞剂，减弱咳嗽反射，支气管平滑肌松弛和降低气道阻力。

Pentoxyverine-d8

Pentoxyverine-d8 Chemical Structure

CAS No. : 1329797-10-5

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生物活性

Pentoxyverine-d8 (Carbetapentane-d8) is the deuterium labeled Pentoxyverine. Pentoxyverine (Carbetapentane) is a sigma-1 receptor agonist, with a Ki of 75 nM on guinea-pig brain membranes. Pentoxyverine is a centrally-acting cough suppressant with antimuscarinic and anticonvulsant properties. Pentoxyverine can be used for inhibiting bronchial interceptor, weakening of cough reflex, bronchial smooth muscle relaxation and reduction of airway resistance[1][2][3][4].

体外研究
(In Vitro)

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

341.51

Formula

C20H23D8NO3
CAS 号

1329797-10-5
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.

    [2]. Mohamed SH, et, al. Extraction-free spectrophotometric assay of the antitussive drug pentoxyverine citrate using sulfonephthalein dyes. Spectrochim Acta A Mol Biomol Spectrosc. 2019 Nov 5;222:117186.

    [3]. Tortella FC, et, al. Dextromethorphan and carbetapentane: centrally acting non-opioid antitussive agents with novel anticonvulsant properties. Brain Res. 1986 Sep 24;383(1-2):314-8.

    [4]. Calderon SN, et, al. Novel 1-phenylcycloalkanecarboxylic acid derivatives are potent and selective sigma 1 ligands. J Med Chem. 1994 Jul 22;37(15):2285-91.

    [5]. Brown C, et, al. Antitussive activity of sigma-1 receptor agonists in the guinea-pig. Br J Pharmacol. 2004 Jan;141(2):233-40.

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