[CAS NO. 77-23-6]??Pentoxyverine
PRODUCTS SPECIFICATIONS [77-23-6]
DESCRIPTION [77-23-6]
Overview
| MDL | MFCD00209899 |
|---|---|
| Molecular Weight | 333.47 |
| Molecular Formula | C20H31NO3 |
| SMILES | O=C(C1(C2=CC=CC=C2)CCCC1)OCCOCCN(CC)CC |
Summary
Pentoxyverine (Carbetapentane) is a sigma-1 receptor agonist, with a K i 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] .
IC50 & Target
Ki: 75 nM (sigma-1 receptor) [4]
In Vitro
Pentoxyverine competitive binds to [
3
H]-pentazocine-labelled sites on guinea-pig brain membranes, with a K
i
of 75 nM
[4]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Pentoxyverine (1-5 mg/kg; a single i.p.) inhibits citric-acid-induced cough in guinea-pigs [4] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT02183649 | Boehringer Ingelheim |
Healthy
|
November 2009 | Phase 1 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 250 mg/mL ( 749.69 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.9988 mL | 14.9939 mL | 29.9877 mL |
| 5 mM | 0.5998 mL | 2.9988 mL | 5.9975 mL |
| 10 mM | 0.2999 mL | 1.4994 mL | 2.9988 mL |
References
- [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.
Synonyms