STRUCTURE-ACTIVITY-RELATIONSHIPS OF 8-STYRYLXANTHINES AS A(2)-SELECTIVE ADENOSINE ANTAGONISTS

• Published in: Journal of medicinal chemistry Vol. 36; no. 10; pp. 1333 - 1342
• Main Authors: JACOBSON, KA, GALLORODRIGUEZ, C, MELMAN, N, FISCHER, B, MAILLARD, M, VANBERGEN, A, VANGALEN, PJM, KARTON, Y
• Format: Journal Article
• Language: English
• Published: WASHINGTON Amer Chemical Soc 14.05.1993
• Subjects: Chemistry, Medicinal; Life Sciences & Biomedicine; Pharmacology & Pharmacy; Science & Technology; SUBSTITUTION; POTENT; AFFINITY; ANALOGS; SPECIES-DIFFERENCES; RAT-BRAIN; INHIBITORS; BINDING-SITES; AGONISTS; A1-ADENOSINE RECEPTORS

A series of substituted 8-styryl derivatives of 1,3,7-alkylxanthines was synthesized as potential A2-selective adenosine receptor antagonists, and the potency at rat brain A1- and A2-receptors was studied in radioligand binding experiments. At the xanthine 7-position, only small hydrophobic substitu...