Synthesis and in Vitro Evaluation of Oxindole Derivatives as Potential Radioligands for 5-HT(7) Receptor Imaging With PET.

Synthesis and In Vitro Evaluation of Oxindole Derivatives as Potential Radioligands for 5-HT(7) Receptor Imaging with PET.

Filed under: Drug and Alcohol Rehabilitation

ACS Chem Neurosci. 2012 Dec 19; 3(12): 1002-7
Herth MM, Volk B, Pallagi K, Kofoed Bech L, Antoni FA, Knudsen GM, Kristensen JL

The most recently discovered serotonin (5-HT) receptor subtype, 5-HT(7), is considered to be associated with several CNS disorders. Noninvasive in vivo positron emission tomography (PET) studies of cerebral 5-HT(7) receptors could provide a significant advance in the understanding of the neurobiology and eventual dysfunctions of the 5-HT(7) receptor. To date, no appropriate 5-HT(7) receptor PET ligand has been developed. Here, we modified known 5-HT(7) selective phenylpiperazinyl-butyloxindole derivatives so that they may be labeled either with carbon-11 or fluorine-18. A set of potential 5-HT(7) ligands for PET molecular imaging was successfully synthesized. Two compounds (10 and 14) were tested against a range of targets. Both compounds display a promising in vitro profile with respect to PET imaging of the 5-HT(7) receptor in thalamic regions.
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ACS Chemical Neuroscience and Neuroscience Drug Discovery as 2012 Comes to a Close.

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ACS Chem Neurosci. 2012 Dec 19; 3(12): 988
Lindsley CW

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Epimedium koreanum Nakai Water Extract Exhibits Antiviral Activity against Porcine Epidermic Diarrhea Virus In Vitro and In Vivo.

Filed under: Drug and Alcohol Rehabilitation

Evid Based Complement Alternat Med. 2012; 2012: 985151
Cho WK, Kim H, Choi YJ, Yim NH, Yang HJ, Ma JY

Porcine epidemic diarrhea virus (PEDV) causes diarrhea of pigs age-independently and death of young piglets, resulting in economic loss of porcine industry. We have screened 333 natural oriental herbal medicines to search for new antiviral candidates against PEDV. We found that two herbal extracts, KIOM 198 and KIOM 124, contain significant anti-PED viral effect. KIOM 198 and KIOM 124 were identified as Epimedium koreanum Nakai and Lonicera japonica Thunberg, respectively. The further plaque and CPE inhibition assay in vitro showed that KIOM 198 has much stronger antiviral activity than KIOM 124. Additionally, KIOM 198 exhibited a similar extent of antiviral effect against other subtypes of Corona virus such as sm98 and TGE viruses. Cytotoxicity results showed that KIOM 198 is nontoxic on the cells and suggest that it can be delivered safely for therapy. Furthermore, when we orally administered KIOM 198 to piglets and then infected them with PEDV, the piglets did not show any disease symptoms like diarrhea and biopsy results showed clean intestine, whereas control pigs without KIOM 198 treatment exhibited PED-related severe symptoms. These results imply that KIOM 198 contains strong antiviral activity and has a potential to be developed as an antiviral phytomedicine to treat PEDV-related diseases in pigs.
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