| Bioactivity | 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]. | ||||||||||||
| Target | Ki: 75 nM (sigma-1 receptor) | ||||||||||||
| Invitro | Pentoxyverine competitive binds to [3H]-pentazocine-labelled sites on guinea-pig brain membranes, with a Ki of 75 nM[4]. | ||||||||||||
| In Vivo | Pentoxyverine (1-5 mg/kg; a single i.p.) inhibits citric-acid-induced cough in guinea-pigs[4]. | ||||||||||||
| Name | Pentoxyverine | ||||||||||||
| CAS | 77-23-6 | ||||||||||||
| Formula | C20H31NO3 | ||||||||||||
| Molar Mass | 333.47 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. |