TRH-like peptides were synthesized in which the critical N-terminus residue L-pGlu was replaced with various heteroaromatic rings, and the central residue histidine with 1-alkyl-L-histidines. All synthesized TRH-like peptides were evaluated in vitro as agonists in HEK mTRH-R1 and HEK mTRH-R2 cell lines, an expressing receptor binding assay (IC50), and cell signaling assay (EC50). The analeptic ...

Histiocytic sarcoma (HS) spontaneously arises in the liver in mice ; however, the cellular origins of hepatic HS have not been fully clarified. In this study, we immunohistochemically analyzed 18 cases of hepatic HS from the archives of our previous experiments. In all cases, the tumor cells showed positive reactions for the macrophage-specific markers F4/80 and CD68. The cells were negative fo...

BACKGROUND Protection against disease or colonization from serotypes related to those in pneumococcal conjugate vaccines (i.e. cross-protection) vary by serotype; the basis for this variation is not understood. The 13-valent pneumococcal conjugate vaccine (PCV13) replaced 7-valent conjugate (PCV7) in the USA in 2010 allowing assessment of PCV7 and PCV13 immunogenicity and functional cross-prote...

Five series of tetrahydrobenzothieno[2,3-d]pyrimidine and tetrahydrobenzothienotriazolopyrimidine derivatives have been synthesized namely: 4-(substituted amino)-5,6,7,8-tetrahydro[1]benzothieno[2,3-d]pyrimidines 4a–d, 4-substituted (methylidenehydrazino)-5,6,7,8-tetrahydro[1]benzothieno[2,3-d]pyrimidines 6a–c, 4-(3,5-disubstituted pyrazol-1-yl)-5,6,7,8-tetrahydro[1]benzothieno[2,3-d]pyrimidine...

BACKGROUND & AIMS Endothelins are expressed in many enteric neurons of the gut. Because activation of endothelin ET(A) and ET(B) receptors is known to alter intestinal muscle activity, the effect of ET(A) and ET(B) receptor agonists and antagonists on propulsive peristalsis was examined. METHODS Repetitive peristalsis in fluid-perfused segments of the guinea pig isolated small intestine was e...

New analogues of nifedipine, as a known calcium channel blocker, were synthesized by replacing the orthonitrophenyl group on position 4 with 1-(4-Nitrobenzyl)-5-imidazolyl or 2-methylthio-1-(4-Nitrobenzyl)-5-imidazolyl substituent. Effects of the new synthesized compounds on blood pressure were studied at 15, 30 and 60 min after administration by indirect tail-cuff method and compared with nife...

New analogues of nifedipine, as a known calcium channel blocker, were synthesized by replacing the orthonitrophenyl group on position 4 with 1-(4-Nitrobenzyl)-5-imidazolyl or 2-methylthio-1-(4-Nitrobenzyl)-5-imidazolyl substituent. Effects of the new synthesized compounds on blood pressure were studied at 15, 30 and 60 min after administration by indirect tail-cuff method and compared with nife...