Chemistry is traditionally divided into organic and inorganic chemistry. The former is the study of compounds containing at least one carbon-hydrogen bonds. 16153-81-4, Name is 4-(4-Methylpiperazin-1-yl)phenylamine, molecular formula is C11H17N3, belongs to piperazines compound, is a common compound. In a patnet, author is Baptista-Hon, Daniel T., once mentioned the new application about 16153-81-4, Quality Control of 4-(4-Methylpiperazin-1-yl)phenylamine.
Activation of mu-opioid receptors by MT-45 (1-cyclohexyl-4-(1,2-diphenylethyl)piperazine) and its fluorinated derivatives
Background and Purpose A fluorinated derivative (2F-MT-45) of the synthetic mu-opioid receptor agonist MT-45 (1-cyclohexyl-4-(1,2-diphenylethyl)piperazine) was recently identified in a seized illicit tablet. While MT-45 is a Class A drug, banned in a number of countries, nothing is known about the pharmacology of 2F-MT-45. This study compares the pharmacology of MT-45, its fluorinated derivatives and two of its metabolites. Experimental Approach We used a beta-arrestin2 recruitment assay in CHO cells stably expressing mu receptors to quantify the apparent potencies and efficacies of known (MT-45, morphine, fentanyl and DAMGO) and potential agonists. In addition, the GloSensor protein was transiently expressed to quantify changes in cAMP levels. We measured Ca2+ to investigate whether MT-45 and its metabolites have effects on GluN1/N2A NMDA receptors stably expressed in Ltk- cells. Key Results The fluorinated MT-45 derivatives have higher apparent potencies (2F-MT-45: 42 nM) than MT-45 (1.3 mu M) for inhibition of cAMP accumulation and beta-arrestin2 recruitment (2F-MT-45: 196 nM; MT-45: 23.1 mu M). While MT-45 and 2F-MT-45 are poor recruiters of beta-arrestin2, they have similar efficacies for reducing cAMP levels as DAMGO. Two MT-45 metabolites displayed negligible potencies as mu receptor agonists, but one, 1,2-diphenylethylpiperazine, inhibited the NMDA receptor with an IC50 of 29 mu M. Conclusion and Implications Fluorinated derivatives of MT-45 are potent mu receptor agonists and this may pose a danger to illicit opioid users. Inhibition of NMDA receptors by a metabolite of MT-45 may contribute to the reported dissociative effects.
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Reference:
Piperazine – Wikipedia,
,Piperazines – an overview | ScienceDirect Topics