Pentoxyverine (citrate)

Pentoxyverine (Carbetapentane) citrate is an orally active sigma-1 receptor agonist, with Kis of 41 nM, 894 nM and 75 nM for σ1, σ2 and guinea-pig brain membrane σ1, respectively. Pentoxyverine citrate is a muscarinic antagonist. Pentoxyverine citrate is a potent antitussive, anticonvulsant, and spasmolytic agent. Pentoxyverine citrate can be used for inhibiting bronchial interceptor, weakening of cough reflex, bronchial smooth muscle relaxation and reduction of airway resistance[1][2][3][4].

Product Specifications

CAS Number

[23142-01-0]

Product Name Alternative

Carbetapentane (citrate)

UNSPSC

12352005

Hazard Statement

H302, H312, H315, H319, H332, H335

Target

MAChR; Sigma Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein; Neuronal Signaling

Applications

COVID-19-immunoregulation

Field of Research

Inflammation/Immunology; Neurological Disease

Assay Protocol

https://www.medchemexpress.com/pentoxyverine-citrate.html

Purity

99.57

Solubility

DMSO : ≥ 36 mg/mL

Smiles

O=C(C1(C2=CC=CC=C2)CCCC1)OCCOCCN(CC)CC.O=C(CC(C(O)=O)(O)CC(O)=O)O

Molecular Formula

C26H39NO10

Molecular Weight

525.59

Precautions

H302, H312, H315, H319, H332, H335

References & Citations

[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]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.|[3]Brown C, et, al. Antitussive activity of sigma-1 receptor agonists in the guinea-pig. Br J Pharmacol. 2004 Jan;141 (2) :233-40.|[4]J M Entrena, et al. Sigma-1 Receptor Agonism Promotes Mechanical Allodynia After Priming the Nociceptive System with Capsaicin. Sci Rep. 2016 Nov 25:6:37835. doi: 10.1038/srep37835.|[5]Yuebin Ge, et al. In Vivo Evaluation of the Antiasthmatic, Antitussive, and Expectorant Activities and Chemical Components of Three Elaeagnus Leaves. Evid Based Complement Alternat Med. 2015:2015:428208.