Binding of dimemorfan to sigma-1 receptor and its anticonvulsant and locomotor effects in mice, compared with dextromethorphan and dextrorphan

Chou, Yueh‐Ching; Liao, Jyh‐Fei; Chang, Wei-Wen; Lin, Ming-Fang; Chen, Chieh-Fu

doi:10.1016/s0006-8993(99)01125-7

Cited by 63 publications

(55 citation statements)

References 17 publications

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“…It has been shown to bind to a series of receptors, including the N-methyl-D-aspartate (NMDA) glutamate receptors (Netzer et al, 1993, Chou et al, 1999, s-1 receptors (Chou et al, 1999), nicotinic (Glick et al, 2001), and serotonergic receptors (Meoni et al, 1997). This complex activity is believed to suppress cough by altering the threshold for cough initiation primarily via its effects as an NMDA antagonist at the level of antagonizing glutamate receptors in the nTS in the CNS (Ramsay et al, 2008).…”

Section: B Dextromethorphanmentioning

confidence: 99%

Antitussive Drugs—Past, Present, and Future

et al. 2014

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Section: B Dextromethorphanmentioning

confidence: 99%

Antitussive Drugs—Past, Present, and Future

et al. 2014

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“…Its other possible beneficial effects have been evaluated using diverse models of neurodegeneration. Interestingly, the evidence indicates that the recognition sites for DM and DF are identical or overlapping (55,91).…”

Section: Neuroprotective Potential Of Dfmentioning

confidence: 99%

“…Previous studies demonstrated that DF is a high-affinity ligand for the σ 1 receptor (K i = 151 nM) but not the PCP site (K i = 16798 nM) and has anticonvulsant properties (43,55,91). In addition, it has been reported to activate σ 1 receptors to attenuate scopolamine-and β-amyloid peptide-induced amnesia in mice (92), possibly through its enhancement of hippocampal acetylcholine release (93).…”

Section: Neuroprotective Potential Of Dfmentioning

confidence: 99%

Neuropsychotoxic and Neuroprotective Potentials of Dextromethorphan and Its Analogs

et al. 2011

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Abstract. Dextromethorphan (3-methoxy-17-methylmorphinan) has complex pharmacologic effects on the central nervous system. Although some of these effects are neuropsychotoxic, this review focuses on the neuroprotective effects of dextromethorphan and its analogs. Some of these analogs, particularly dimemorfan (3-methyl-17-methylmorphinan) and 3-hydroxymorphinan, have promising neuroprotective properties with negligible neuropsychotoxic effects. Their neuroprotective effects, the mechanisms underlying these effects, and their therapeutic potential for the treatment of diverse neurodegenerative disorders are discussed.

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“…It is an uncompetitive N-methyl-D-aspartate receptor (NMDA) receptor antagonist and μ-, δ-, and κ-opioid receptor agonist (Burns et al, 2013;Codd et al, 1995). Instead of acting as a direct antagonist of the NMDA receptor itself, dextromethorphan likely functions as a pro-drug to its nearly 10-fold more potent metabolite dextromethorphan, and this is the true mediator of its dissociative effects (Chou et al, 1999). (+)-3-methoxymorphinan, dextromethorphan's other major metabolite, plays role in its effects, but it is not entirely clear (Schmider et al, 1997).…”

Section: Introductionmentioning

confidence: 99%

Study of Interaction of Dextromethorphan Hydrobromide with Deoxyribonucleic Acid by Fluorescence Quenching

et al. 2016

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Interactions with many clinically active therapeutic agents with deoxyribonucleic acid (DNA) are well studied and it expedites deciphering the structure of DNA and to investigate the pathological implication of those molecules in a living organism. The interaction of dextromethorphan hydrobromide (DEX) with calf thymus DNA (ct DNA) was studied employing UV absorption and fluorescence spectroscopic techniques. The binding affinity of DEX to DNA was calculated at different temperatures and the stoichiometry of binding was characterized to be about 1 dextromethorphan molecule per nucleotide. Hypochromic effect was found in the absorption spectra of dextromethorphan, and its wavelength had no shift in the presence of DNA indicating external binding mode of dextromethorphan to DNA. Quenching constants 3532 L/ mol and 12446L/ mol at 298 K and 308 K respectively with correlation co-efficient of 0.974 and 0.976, using SternVolmer equation and the quenching mechanism was found to be dynamic. Fluorescence spectroscopic results showed the quenching of fluorescence intensity of DEX in the presence of DNA, indicating the interaction between DEX and DNA. Based on this, hydrophobic interaction were found to play the dominating role in DEX-DNA binding and those binding forces also indicate the binding site of dextromethorphan to be in the minor groove of DNA.

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Binding of dimemorfan to sigma-1 receptor and its anticonvulsant and locomotor effects in mice, compared with dextromethorphan and dextrorphan

Cited by 63 publications

References 17 publications

Antitussive Drugs—Past, Present, and Future

Antitussive Drugs—Past, Present, and Future

Neuropsychotoxic and Neuroprotective Potentials of Dextromethorphan and Its Analogs

Study of Interaction of Dextromethorphan Hydrobromide with Deoxyribonucleic Acid by Fluorescence Quenching

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