We have determined the binding affinities of the novel alpha-2 adrenoceptor antagonist radioligand [3H]-MK912 for the cloned human alpha-2A, alpha-2B and alpha-2C adrenoceptors. The KD-values were 1.25 nM, 1.36 nM and 0.086 nM for the al... S Uhlén,AC Porter,RR Neubig - 《Journal ...
Synthesis of Novel α-C-Glycosylamino Acids and Reverse Regioselectivity in Larock's Heteroannulation for the Synthesis of the Indole Nucleus and Isobe, M., Synthesis of novel -C-glycosylamino acids and reverse regioselec- tivity in Larock's heteroannulation for the synthesis of the indole nu....
Novel method for preparing alpha-glycosylceramides, novel alpha-glycosylceramide derivatives and their uses The invention relates to new derivatives α - glycosylceramide corresponding to the general formula (s) - (i), a process for their preparation and pharmaceutical compositions containing them and ...
Novel asymmetric thioethers of the formula <IMAGE> (I) in which the general symbols have the following meanings: a is an integer of from 1 to 7, Ro represents hydrogen or C1-7-alkanoyl, R1 represents C1-3-alkyl which may be substituted at the terminal carbon atom by a free or acylated...
Purpose To investigate the potential of a novel lipid carrier, comprising beads of alpha-cyclodextrin and soybean oil, for topical drug delivery. Adapalene was chosen as a model drug to explore the ability of the beads to encapsulate and release a highly lipophilic compound. Materials and Methods...
A novel one-pot procedure for the stereoselective synthesis of alpha-hydroxy esters from ortho esters was developed. Key steps were multi-heteroatom Cope rearrangements of O-acylated N-hydroxy-l-tert-leucinol-derived oxazoline N-oxides leading to alpha-acyloxy oxazolines and, after methanolysis, to...
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In this project, we describe the design and characterization of novel melanoma-targeting peptide analogs for use in diagnostic imaging of both primary and metastatic melanoma lesions. Novel alpha-MSH peptide conjugates were designed to target the melanocortin-1 receptor present and over-expressed on ...
Positive PC18C5 mAb-ir signals in brain areas that did not match with previously identified C-terminal amide–peptide immunoreactivity, were considered as potential brain areas expressing putative novel valine amide neuropeptides. Positive Val-CONH2-ir signals detected in subtracted brain regions were ...
Novel Site on Sodium Channel α-Subunit Responsible for the Differential Sensitivity of Grayanotoxin in Skeletal and Cardiac Muscle We searched for sites on the alpha-subunit of the fast Na(+) channel responsible for the difference in GTX (grayanotoxin) sensitivity of the skeletal- and ... T...