Benzo[1,2-c:5,4-c']dipyrazoles: non-xanthine adenosine antagonists.
3,5-Dimethylbenzo[1,2-c:5,4-c']dipyrazoles, optionally substituted in the 1-, 7-, and 8-positions, were synthesized from resorcinols. These compounds display affinity for adenosine A1 (rat brain) and A2 (human platelet) receptors. In addition, these compounds reverse contractions of guinea pig tracheal cylindrical segments induced by potassium chloride, histamine, acetylcholine, and 5-hydroxytryptamine, as well as reverse bronchospasm induced by aerosolized histamine in the conscious guinea pig.
Peet
N P
NP
Merrell Dow Research Institute, Cincinnati, Ohio 45215.
Dickerson
G A
GA
Abdallah
A H
AH
Daly
J W
JW
Ukena
D
D
D000241:Adenosine / Q000037:antagonists & inhibitors*; D000818:Animals; D001980:Bronchi / Q000187:drug effects; D006168:Guinea Pigs; D006801:Humans; D009119:Muscle Contraction / Q000187:drug effects; D011720:Pyrazoles / Q000494:pharmacology*; D051381:Rats; D011983:Receptors, Purinergic / Q000378:metabolism; D013329:Structure-Activity Relationship
D011720:Pyrazoles; D011983:Receptors, Purinergic; D000241:Adenosine