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。
货号:ajcx32552
CAS:77-23-6
分子式:C20H31NO3
分子量：333.47
溶解度:DMSO : 250 mg/mL (749.69 mM)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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].

Pentoxyverine competitive binds to [3H]-pentazocine-labelled sites on guinea-pig brain membranes, with a Ki of 75 nM[4].

Pentoxyverine (1-5 mg/kg; a single i.p.) inhibits citric-acid-induced cough in guinea-pigs[4].

参考文献:
[1]. 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.
[2]. 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.
[3]. 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.
[4]. Brown C, et, al. Antitussive activity of sigma-1 receptor agonists in the guinea-pig. Br J Pharmacol. 2004 Jan;141(2):233-40.