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최성운,David R. Elmaleh 한국과학수사학회 2010 과학수사학회지 Vol.4 No.2
Agents which prevent binding of cocaine to the dopamine transporter (DAT) weakly inhibit the reuptake of DA and act as antagonists at DA/ serotonin (5-HT) receptors might be useful drugs for treating cocaine addiction by assisting cocaine addicts in maintaining abstinence. To determine the structural requirements necessary for this dual activity at DAT and DA/5-HT receptor sites, a series of (bisarylmethoxy)butylpiperazine derivatives was prepared and evaluated in vitro and in vivo. These hybrid ligands were constructed by combining pharmacophores for the DAT and the DA/5-HT receptor. The initial series was evaluated in vitro as DAT and DA/5-HT receptor ligands and selected target compounds were tested in vivo for effects on cocaine-induced hyper-locomotor activity (LMA). Most of the new compounds demonstrated high to moderate affinity (4 to 175 nM) at the DAT. Compound 18exhibited the highest discrimination ratio (DR) of 144. These derivatives displayed modest affinity for and antagonistic activity at D 2 /D 3 DA receptors. Compounds 10 and 18 stimulated LMA whereas compound 16 suppressed the response. Cocaine-induced hyperlocomotion was attenuated by compounds 16 and 18. The results of this study demonstrate that (bisarylmethoxy)butylpiperazine derivatives may be of value in the development of therapeutics for treating cocaine abuse/addiction and in the further pharmacological and biological characterization of the DAT.
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주혜림,Pachhapure, Shailashree,Mufida, Amila,김아련,Elmaleh, David R.,최성운,장병철 계명대학교 의과대학 2022 계명의대학술지 Vol.41 No.2
Inflammation is a common link in the pathophysiology of many neurological illnesses, including Alzheimer’s disease. Activated glial cells contribute to neuroinflammation by producing pro-inflammatory mediators. Naproxen and ibuprofen are nonsteroidal anti-inflammatory drugs with 2-aryl(s) propionic acid as a common pharmacophore. Here we designed a small series of naproxen and ibuprofen amide dimers and tested their effects on the expression of inducible nitric oxide synthase (iNOS), a neuroinflammatory enzyme in lipopolysaccharide (LPS)-stimulated BV2 mouse microglial cells. Of note, treatment with CNU 019, 020, 021, 023, 024, and 027 at 10 M markedly inhibited the LPS-induced iNOS expression in BV2 cells. CNU 024 was tested further at different concentrations to regulate the LPS-induced iNOS expression in BV2 cells. Treatment with CNU 024 at 5, 10, or 20 M dose-dependently suppressed the LPS-induced iNOS protein and mRNA expression levels in BV2 cells, in which maximal inhibition was seen at 20 M. CNU 024 treatment at doses tested further led to a concentration-dependent inhibition of the LPS-induced phosphorylation (activation) of p38 mitogen-activated protein kinase (MAPK) without influencing its total protein expression in BV2 cells, but it did not affect the LPS-induced activation of c-jun N-terminal kinase-1/2 and extracellular signal-regulated kinases-1/2 in these cells. In summary, our results demonstrate that CNU 024 inhibits the LPS-induced iNOS expression in BV2 cells, partly mediated by the inhibition of p38 MAPK. This work shows that CNU 024 could be a valuable ligand for further development as a potential drug candidate for treating neuroinflammatory pathologies.
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