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4-Aminophenyl acetamides and propanamides as potent transient receptor potential vanilloid 1 (TRPV1) ligands.
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A series of 2-(3,5-substituted 4-aminophenyl)acetamide and propanamide derivatives were investigated as human TRPV1 antagonists. The analysis of the structure-activity relationship indicated that 2-(3,5-dihalo 4-aminophenyl)acetamide analogues displayed excellent antagonism of hTRPV1 activation by
Repeated administration of vanilloid receptor TRPV1 antagonists attenuates hyperthermia elicited by TRPV1 blockade.
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Capsaicin, the active ingredient in some pain-relieving creams, is an agonist of a nonselective cation channel known as the transient receptor potential vanilloid type 1 (TRPV1). The pain-relieving mechanism of capsaicin includes desensitization of the channel, suggesting that TRPV1 antagonism may
Acute agranular CD4-positive natural killer cell leukemia. Comprehensive clinicopathologic studies including virologic and in vitro culture with inducing agents.
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BACKGROUND
A 63-year-old male presented with fever, a subcutaneous nodule, gingival hypertrophy, lacrimal gland enlargement, and no lymphadenopathy or hepatosplenomegaly, but had anemia, thrombocytopenia, and peripheral blood (PB) plus bone marrow (BM) involvement by leukemic cells. There was
Identification of chloramphenicol in human hair leading to a diagnosis of factitious disorder.
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Introduction: Chloramphenicol (2,2-dichloro-N-[1,3-dihydroxy-1-(4-nitrophenyl)porpan-2-yl]acetamide) is a bacteriostatic antibiotic of the phenicolated family, used in the past to treat meningitis, plague, cholera, or typhoid fever. Treatment with chloramphenicol can have life threatening
Spectroscopic monitoring of local conformational changes during the intramolecular domain-domain interaction of the ryanodine receptor.
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The amino (N)-terminal and central regions of the ryanodine receptor (RyR) containing most mutation sites of malignant hyperthermia (MH) and central core disease (CCD) seem to be involved in the Ca(2+) channel regulation. Our recent peptide probe study (Yamamoto, T., El-Hayek, R., and Ikemoto, N.
Functional effects of systemically administered agonists and antagonists of mu, delta, and kappa opioid receptor subtypes on body temperature in mice.
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We have investigated the roles of peripheral and central mu, delta, and kappa opioid receptors and their subtypes in opioid-induced hypothermia in mice. Measuring rectal temperature after i.p. injection, opioid agonists [morphine, fentanyl, SNC80
A novel colchicine-based microtubule inhibitor exhibits potent antitumor activity by inducing mitochondrial mediated apoptosis in MIA PaCa-2 pancreatic cancer cells.
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Colchicine, an antimitotic alkaloid isolated from Colchicum autumnale, is a classical drug for treatment of gout and familial Mediterranean fever. It causes antiproliferative effects through the inhibition of microtubule formation, which leads to mitotic arrest and cell death by apoptosis. Here, we
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