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Biomedical subjects

D Spalding

Publications and source records attributed to D Spalding.

8 recordsLinked to original sources

Indazolylamino quinazolines and pyridopyrimidines as inhibitors of the EGFr and C-erbB-2.

Described herein is the design and synthesis of indazolylaminopyridopyrimidines and quinazolines as inhibitors of the class 1 tyrosine kinase receptor family. Data is presented for N(4)-(1-benzyl-1H-indazol-5-yl)-N(6),N(6)-dimethylpyrido[3,4-d]pyrimidine-4,6-diamine 3B. This compound inhibited EGFr and c-erbB-2 enzymes selectively over other kinases. It inhibited the proliferation of a range of tumour cell lines in vitro and the growth of BT474 xenografts in SCID mice.

Animals↗

Modelling the muscles of the scapula morphometric and coordinate data and functional implications.

Modelling of the shoulder mechanism is dependent upon reliable data on the morphometry and points of attachment of the relevant muscles. In this paper, the authors present coordinate data which have been derived from the radiography of dissected cadavers. All of the coordinates have been normalised with respect to reference dimensions of the relevant segments (humerus, scapula, clavicle and trunk). Similarly the measurements of physiological cross-section area (PCSA) have been normalised with respect to that of deltoid. The measurements of PCSA have been shown to agree largely with the work of Veeger et al. [J. Biomechanics 24, 615-629 (1991)] and Karlsson and Peterson [J. Biomechanics 25, 189-199 (1992)]. While the majority of the descriptions of morphometry concur with accepted texts there are some notable disagreements, particularly concerning trapezius.

Anatomy, Cross-Sectional↗

Polymorphic formation of morphine from codeine in poor and extensive metabolizers of dextromethorphan: relationship to the presence of immunoidentified cytochrome P-450IID1.

We studied the oxidation capacity in liver biopsies of a series of extensive metabolizers (n = 10) and poor metabolizers (n = 2) as identified by in vivo phenotyping with dextromethorphan. Codeine and dextromethorphan were used as probe drugs in vitro. The data were compared with the contents of cytochrome P-450IID1 as quantitated by Western immunoblotting by use of a specific monoclonal antibody (MAb 114/2). The O-demethylation of codeine was highly correlated with the O-demethylation of dextromethorphan (r = 0.90). The N-demethylation of codeine was catalyzed at a considerably higher rate than the O-demethylation. The N-demethylation to O-demethylation ratio of codeine was 46 in the poor metabolizer and, on average, 6.2 (range, 2.6 to 11) in the extensive metabolizers, respectively. The band intensity in Western blots correlated with the rate of O-demethylation of codeine (r = 0.95) and of dextromethorphan (r = 0.88) in the extensive metabolizers. The comeasurement of the O-demethylation and N-demethylation of codeine may provide a tool with which to phenotype individuals in vitro with respect to the polymorphism of the cytochrome P-450IID1.

Antibodies, Monoclonal↗