Title of article :
Potent, selective, water-soluble benzodiazepine-based CCKB receptor antagonists that contain lipophilic carboxylate surrogates
Author/Authors :
Mark S. Chambers، نويسنده , , Sarah C. Hobbs، نويسنده , , Michael I. Graham، نويسنده , , Alan P. Watt، نويسنده , , Stephen R. Fletcher، نويسنده , , Raymond Baker، نويسنده , , Stephen B. Freedman، نويسنده , , Smita Patel، نويسنده , , Alison J. Smith، نويسنده , , Victor G. Matassa، نويسنده ,
Abstract :
Acylsulphonamide analogues of the meta-tolylurea L-708,474 have been synthesised and evaluated as CCKB receptor antagonists. Such derivatives retain very high affinity and subtype selectivity for the CCKB receptor, and have good aqueous solubility. The ortho-tolyl acylsulphonamide L-736,309 is orally bioavailable and brain penetrant in rat.
