The effects of the tryptophan hydroxylase (TPH) inhibitor p-chlorophenylalanine (PCPA; 200 mg/kg; 3 days), and of the protein synthesis inhibitor cycloheximide (CXM, 2 mg/kg), on regional serotonin (5-HT) synthesis were studied using the α-[14C]methyl-l-tryptophan (α-[14C]MTrp) autoradiographi...
Tuberous sclerosis complex (TSC) is characterized by hamartomatous lesions in various organs and arises due to mutations in the TSC1 or TSC2 genes. TSC mutations lead to a range of neurological manifestations including epilepsy, cognitive impairment, autism spectrum disorders (ASD), and brain le...
11C-alpha-methyl-l-tryptophan ([11C]AMT), a tryptophan metabolism PET tracer, has successfully been employed for brain serotonin pathway and indoleamine 2,3-dioxygenase (IDO) pathway related tumor imaging. We here report a reliable, automated procedure for routine synthesis of [11C]AMT based on ...
This paper deals with the synthesis of Nα-(β-naphthylsulfonylaminoglycyl)-argininamide compounds and the results of a pharmacological study (in vitro and in vivo). No thrombin inhibition was obtained with Nα-arylsulfonyl-aminoalkyl-(4-amidinophenyl)-alaninamide compounds in which the 4-amidin...
NG-Acylated argininamides, covering a broad range of lipophilicity (calculated log D values: −1.8–12.5), were synthesized and investigated for NPY Y1 receptor (Y1R) antagonism, Y1R affinity and stability in buffer (NG-deacylation, yielding BIBP 3226). Broad structural variation of substituents ...
The trans-activating region (TAR) RNA-Tat protein interaction is important for activation of transciption in the human immunodeficiency virus (HIV). A model complex for this interaction composed of the two base bulge HIV-2 TAR and the amide derivative of arginine was studied by multidimensional ...
l-Arginine (Arg) is a widely used additive for suppressing protein aggregation during refolding. Systematic screening of Arg analogs provides superior additives that enhance the refolding yield more effectively than Arg. The refolding yield of hen egg lysozyme in the presence of 500 mM l-arginin...
Fluorescently labelled NPY Y1 receptor (Y1R) ligands were synthesized by connecting pyrylium and cyanine dyes with the argininamide-type Y1R antagonist core structure by linkers, covering a wide variety in length and chemical nature, attached to the guanidine group. The most promising fluorescen...
The structurally related peptides neuropeptide Y (NPY), peptide YY (PYY) and pancreatic polypeptide (PP) are endogenous agonists of the NPY receptor (YR) family, which in humans comprises four functionally expressed subtypes, designated Y1R, Y2R, Y4R and Y5R. Nonpeptide antagonists with high aff...
In this paper, we reported the synthesis of bifendate derivatives and evaluation of anti-inflammatory activity by detecting the production of the Nitric Oxide (NO) in the lipopolysaccharide(LPS)-stimulated RAW 264.7 cell lines. Among the newly derivatives, compound 7k was the most potent one and...
Cysteine is one of the more toxic amino acids, however the toxic agent associated with cysteine toxicity has not been identified. Recently it was shown that 2-methyl-2,4-thiazolidine dicarboxylate (MTD) was formed from cysteine by rat liver and would be toxic to the rat. This suggested that MTD ...
Reversible synthetic inhibitors are characterized for Astacus protease, a 22,614-Da zinc containing neutral endopeptidase from the digestive tract of crayfish. Effective inhibition was demonstrated for several simple thiol containing compounds and a series of amino acid hydroxamates. Both classe...
3-Arylsydnone-4-carbohydroximic acid chlorides (1) could react with N-arylmaleimides (3a–b) or 2-methyl-N-phenylmale-imide (3c) to give 3-(3-arylsydnon-4-yl)-5-aryl-3a,6a-dihydro-pyrrolo[3,4-d]isoxazole-4,6-diones (4a–h) or 6a-methyl-3-(3-arylsydnon-4-yl)-5-phenyl-3a,6a-dihydro-pyrrolo[3,4-d]i...
A series of N-alkylmaleimides varying in chainlength from N-methyl to N-octylmaleimide inclusive was shown to effectively inactivate sheep liver sorbitol dehydrogenase at pH 7.5 and 25°C. The apparent second-order rate constants for inactivation increased with increasing chainlength of the N-al...
A high-performance liquid chromatographic assay for penicillamine in plasma is described. The method is based on the derivatisation of penicillamine in acidified protein-free plasma supernatants with the sulphydryl-specific reagent N-[p-(2-benzoxazolyl)-phenyl] maleimide (BOPM) to give a stable ...
Basic hydrolysis (pyridine-water) of a 2,2,2-trifluoroethyl tyrosinyl 1-H-phosphonate diester affords predominantly a 2,2,2-trifluoroethyl 1-H-phosphonate mono-ester and tyrosine. The latter finding has been applied to the synthesis of a dipeptide consisting of a 1-H-phosphonylated serine and a ...
The lipase(PPL)-catalyzed peptide synthesis(Z-Phe-Phe-NH2) in aqueous water-miscible organic cosolvents was studied using Z-Phe-OEt as an ester substrate and Phe-NH2 as a nucleophile. It was found that peptide yield increased with an increase of the concentration of DMF. At a higher concentratio...
Ab initio molecular orbital calculations at the MINI 1 and 3–21G levels of theory have been used to optimise structures for α-substituted carbocations CH2Z+, CH3CHZ+, and (CH3)2 CZ+, and for the hydrocarbons CH3Z, CH3CH2Z and (CH3)2 CHZ where Z is NH2, PH2, AsH2, OH, SH and SeH. Energy differe...
Two libraries of hMC4R agonists, X-Y-DPhe7-Arg8-2-Nal9-Z-NH2 and X-Y-DPhe7-Arg8-Trp9-Z-NH2, totaling 185 peptides were prepared using Irori radiofrequency tagging technology and Argonaut Quest 210 Synthesizer, where X stands for N-caps, Y for His6 surrogates and Z for Gly10 surrogates. As a resu...
The design of novel efficient antimicrobial peptides (AMPs) faces several issues, such as cost of synthesis, proteolytic stability or cytotoxicity. The identification of key determinants involved in the activity of AMPs, such as cationicity and amphipathicity, allowed the synthesis of short pept...
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