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Chemical Compound Review:

Atussil 2-(2-diethylaminoethoxy)ethyl 1...

Synonyms: Pentoxiverin, Pentoxyverin, Pentoxiverina, Pentoxyverine, Pentoxiverinum, ...

Wallace, D.R. et al., Brown, C. et al., Domenici, M.R. et al., Tortella, F.C. et al., Klouz, A. et al., et al.

Brown, Fezoui, Selig, Schwartz, Ellis,

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Psychiatry related information on Pentoxyverine

The non-opioid antitussives dextromethorphan and carbetapentane, the active ingredients of several over-the-counter cough suppressants, provide a dose-related protection against maximal electroshock seizures in rats [1].

High impact information on Pentoxyverine

In this work, CE separation with end-column Ru(bpy)3(2+) ECL detection for the quantitative determination of pentoxyverine was firstly performed [2].
Identification of D3 and sigma receptors in the rat striatum and nucleus accumbens using (+/-)-7-hydroxy-N,N-di-n-[3H]propyl-2-aminotetralin and carbetapentane [3].
In transfected CCL1.3 mouse fibroblasts expressing the human D3 receptor, neither DTG nor carbetapentane (0.1 microM) displaced (+/-)-7-OH-[3H]DPAT binding [3].
Carbetapentane and R(-)-PPAP (0.1 microM) displaced approximately 20-50% of total (+/-)-7-OH-[3H]DPAT binding in striatum, nucleus accumbens, and olfactory tubercle in autoradiographic studies, with the nucleus accumbens shell subregion exhibiting the greatest displacement [3].
However, carbetapentane interacts at muscarinic binding sites as well, and it is not clear whether either of these receptor systems is involved in the mechanism(s) of action(s) of this drug [4].

Chemical compound and disease context of Pentoxyverine

DM, carbetapentane, and caramiphen also are efficacious anticonvulsant agents in the rat maximal electroshock seizures test, and DM enhances the anticonvulsant effects of phenytoin (PHT) [5].

Biological context of Pentoxyverine

Carbetapentane acted as a kappa-agonist and mu-antagonist (IC50 = 11.2) [6].

Anatomical context of Pentoxyverine

These sites were located on the outer mitochondrial membranes and displayed high affinity for other sigma(1) ligands namely, haloperidol, ifenprodil, carbetapentane or 1,3-di(2-tolyl)guanidine (DTG) [7].

Associations of Pentoxyverine with other chemical compounds

The nonopioid antitussives dextromethorphan (DM), carbetapentane and caramiphen are efficacious anticonvulsant agents in the rat MES test [8].
2. Intraperitoneal (i.p.) administration of DEX (30 mg kg(-1)) and the sigma-1 agonists SKF-10,047 (1-5 mg kg(-1)), Pre-084 (5 mg kg(-1)), and carbetapentane (1-5 mg kg(-1)) inhibited citric-acid-induced cough in guinea-pigs [9].
All 3 drugs significantly reduced the release of glutamate, with carbetapentane being the most potent (IC50 approximately 40 microM) [10].

Gene context of Pentoxyverine

1. The effects of the non-opioid antitussives caramiphen and carbetapentane and of the anticonvulsants 5,5-diphenylhydantoin and MK 801 were tested towards hypoxia-induced electrical changes in rat hippocampal slices [11].

References

Dextromethorphan and carbetapentane: centrally acting non-opioid antitussive agents with novel anticonvulsant properties. Tortella, F.C., Musacchio, J.M. Brain Res. (1986) [Pubmed]
Study on the enhancement of Ru(bpy)3(2+) electrochemiluminescence by nanogold and its application for pentoxyverine detection. Liu, Y., Pan, W., Liu, Q., Yao, S. Electrophoresis (2005) [Pubmed]
Identification of D3 and sigma receptors in the rat striatum and nucleus accumbens using (+/-)-7-hydroxy-N,N-di-n-[3H]propyl-2-aminotetralin and carbetapentane. Wallace, D.R., Booze, R.M. J. Neurochem. (1995) [Pubmed]
Novel 1-phenylcycloalkanecarboxylic acid derivatives are potent and selective sigma 1 ligands. Calderon, S.N., Izenwasser, S., Heller, B., Gutkind, J.S., Mattson, M.V., Su, T.P., Newman, A.H. J. Med. Chem. (1994) [Pubmed]
Dextromethorphan binding sites in the guinea pig brain. Musacchio, J.M., Klein, M. Cell. Mol. Neurobiol. (1988) [Pubmed]
Effects of sigma ligands on the cloned mu-, delta- and kappa-opioid receptors co-expressed with G-protein-activated K+ (GIRK) channel in Xenopus oocytes. Kobayashi, T., Ikeda, K., Ichikawa, T., Togashi, S., Kumanishi, T. Br. J. Pharmacol. (1996) [Pubmed]
Evidence for sigma-1-like receptors in isolated rat liver mitochondrial membranes. Klouz, A., Sapena, R., Liu, J., Maurice, T., Tillement, J.P., Papadopoulos, V., Morin, D. Br. J. Pharmacol. (2002) [Pubmed]
Allosteric modulation of dextromethorphan binding sites. Musacchio, J.M., Klein, M., Santiago, L.J. Neuropharmacology (1987) [Pubmed]
Antitussive activity of sigma-1 receptor agonists in the guinea-pig. Brown, C., Fezoui, M., Selig, W.M., Schwartz, C.E., Ellis, J.L. Br. J. Pharmacol. (2004) [Pubmed]
Non-opioid antitussives inhibit endogenous glutamate release from rabbit hippocampal slices. Annels, S.J., Ellis, Y., Davies, J.A. Brain Res. (1991) [Pubmed]
Effects of non-opioid antitussives on hypoxia-induced electrical changes in rat hippocampal slices: a comparative study with anticonvulsant drugs. Domenici, M.R., Sagratella, S., Frank, C., Scotti de Carolis, A. Gen. Pharmacol. (1993) [Pubmed]

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