PHARMACOLOGICAL STUDIES ON 4(OR 5)-AMINOIMIDAZOLE-5 (OR 4)-CARBOXAMIDE (AICA) DERIVATIVES

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Pharmacological studies on 4 (or 5)-aminoimidazole-5 (or 4)-carboxamide (AICA) derivatives.

In previous works from our laboratory (1-3) we reported that 4-diazoimidazole-5 carboxamide (diazo-ICA) and 4-(mono or di-substituted) triazenoimidazole-5-carboxamide (mono or dialkyl-TICA) showed marked inhibitory effects on the growth of tumors and bacterial cells. During examination of their toxicity in mice, behavioral sedation caused by these compounds was also observed (2). These observat...

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Glycogen-dependent effects of 5-aminoimidazole-4-carboxamide (AICA)-riboside on AMP-activated protein kinase and glycogen synthase activities in rat skeletal muscle.

5'-AMP-activated protein kinase (AMPK) functions as a metabolic switch in mammalian cells and can be artificially activated by 5-aminoimidazole-4-carboxamide (AICA)-riboside. AMPK activation during muscle contraction is dependent on muscle glycogen concentrations, but whether glycogen also modifies the activation of AMPK and its possible downstream effectors (glycogen synthase and glucose trans...

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5-aminoimidazole-4-carboxamide ribonucleoside (AICAR) inhibits insulin-stimulated glucose transport in 3T3-L1 adipocytes.

Incubation of skeletal muscle with 5-aminoimidazole-4carboxamide ribonucleoside (AICAR), a compound that activates 5'-AMP-activated protein kinase (AMPK), has been demonstrated to stimulate glucose transport and GLUT4 translocation to the plasma membrane. In this study, we characterized the AMPK cascade in 3T3-L1 adipocytes and the response of glucose transport to incubation with AICAR. Both is...

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Inhibition of 5-aminoimidazole-4-carboxamide ribotide transformylase, adenosine deaminase and 5'-adenylate deaminase by polyglutamates of methotrexate and oxidized folates and by 5-aminoimidazole-4-carboxamide riboside and ribotide.

With the use of a continuous spectrophotometric assay and initial rates determined by the method of Waley [Biochem. J. (1981) 193, 1009-1012] methotrexate was found to be a non-competitive inhibitor, with Ki(intercept) = 72 microM and Ki(slope) = 41 microM, of 5-aminoimidazole-4-carboxamide ribotide transformylase, whereas a polyglutamate of methotrexate containing three gamma-linked glutamate ...

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Role of 4-aminoimidazole-5-carboxamide in purine synthesis by Escherichia coli.

In a previous communication (1) it has been shown that the accumulation of 4-aminoimidazole-5-carboxamide (“amine”) in sulfadiazine-inhibited Escherichia coli is suppressed by the addition of methionine and catalytic quantities of p-aminobenzoic acid (PABA), and it was assumed that the “labile methyl” group of the sulfur-containing amino acid is used, with the help of PABA as carrier, for the c...

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ژورنال

عنوان ژورنال: Japanese Journal of Pharmacology

سال: 1967

ISSN: 0021-5198

DOI: 10.1016/s0021-5198(19)67519-0