Carβpentane citrate is a selective inhibitor ofmAchR with Ki value of 76nM, also binds to serotonin 5-HT3 with Ki value of 7.9 nM and works as an agonist of the sigma-1 receptor (Ki = 10.4 nM).
Carbetapentane citrate, a non-opioid centrally-acting antitussive drug, is a common treatment for cough associated with other diseases such as common cold and respiratory tract infections. Its mode of action is very close to that of atropine; since it acts at the level of the peripheral parasympathetic nerve endings. The drug reaches its maximum plasma concentration (Cmax) 2h after administration, and it has a plasma half-life of 2.3h in case of oral administration[3]. Carbetapentane exhibited dose-dependent spinal blockade with a more sensory-selective action over motor blockade. Carbetapentane showed a much stronger frequency-dependence of block than lidocaine: with high frequency stimulation (3.33 Hz), 50 µM lidocaine produced an additional 30% blockade, while the same concentration of carbetapentane produced 70% more block[4]. Carbetapentane had an anticonvulsant action without protecting against NMDA-induced lethality[5]. Carbetapentane pretreatment also significantly attenuated the KA-induced (kainic acid) increase in Fos-related antigen immunoreactivity in the hippocampus. Carbetapentane provides neuroprotection against KA insult via sigma-1 receptor modulation[6].
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