2937-01-1Relevant academic research and scientific papers
High affinity ligands and potent antagonists for the α1D- adrenergic receptor. Novel 3,8-disubstituted [1]benzothieno[3,2-d]pyrimidine derivatives
Romeo, Giuseppe,Salerno, Loredana,Pittalà, Valeria,Modica, Maria N.,Siracusa, Maria A.,Materia, Luisa,Buccioni, Michela,Marucci, Gabriella,Minneman, Kenneth P.
, p. 419 - 432 (2014/07/21)
A new series of high affinity ligands and antagonists for the α1D-adrenergic receptor (AR) has been discovered. New molecules present a [1]benzothieno[3,2-d]pyrimidin-2,4(1H,3H)-dione or a [1]benzothieno[3,2-d]pyrimidin-4(3H)-one scaffold and bear a 2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl moiety in the 3-position and various amide substituents in the 8-position. In binding assays at the three human cloned α1A-, α1B-, and α1D-AR subtypes, they showed high affinity values, particularly for the α1D-AR subtype. Compound 22 (RX18), N1-methyl-N 5-[3-[2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl]-2,4-dioxo-1,2,3, 4-tetrahydro[1]benzothieno[3,2-d]pyrimidin-8-yl]-N1-(phenylmethyl) pentanediamide, was the most interesting in the series displaying very high affinity (pKi = 10.25) and potent antagonism (pKb = 9.15) when tested in a functional assay at the α1D-AR.
Composition containing a penem or carbapenem antibiotic and the use of the same
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, (2008/06/13)
Administration of an N-acylated amino acid in association with a penem or carbapenem antibiotic relieves or eliminates the renal problems associated with administration of the antibiotic alone. The amino acid derivative and antibiotic may be formulated together as a composition or administered separately, either simultaneously or sequentially.
Composition containing a penem or carbapenem antibiotic
-
, (2008/06/13)
Administration of an N-acylated amino acid in association with a penem or carbapenem antibiotic relieves or eliminates the renal problems associated with administration of the antibiotic alone. The amino acid derivative and antibiotic may be formulated together as a composition or administered separately, either simultaneously or sequentially. The composition may be prepared by simple mixing.
