Dicentrine was found to be a potent alpha 1-adrenoceptor blocking agent in rat thoracic aorta as revealed by its competitive antagonism of noradrenaline- (pA2 = 8.19 +/- 0.09) or phenylephrine (pA2 = 9.01 +/- 0.10)-induced vasoconstriction. These effects still persisted in denuded aorta. Dicentrine inhibited platelet aggregation and release reaction through the suppression of thromboxane formation and elevation of adenosine 3': S'-cyclic monophosphate. (A15323) d-Dicentrine significantly inhibits the growth of human hepatoma cell line HuH-7 by delaying its doubling time in tissue culture. An in vitro colony forming assay showed that d-dicentrine decreased the colony formation efficiency in both hepatoma cell lines, HuH-7 and MS-G2. An MTT assay in 21 tumor cell lines also revealed that d-dicentrine was most cytotoxic to esophageal carcinoma HCE-6, lymphoma cell lines Molt-4 and CESS, leukemia cell lines HL60 and K562, and hepatoma cell line MS-G2. (A15341) Dicentrine is also a selective α1-adrenoceptor antagonist with potent antiarrhythmic and antihypertensive activities. (A15324)
| Target Name |
Mechanism of Action |
References |
Alpha-1 adrenergic receptor
Cyclin-dependent kinase 2
|
|
20097066
20622045
1686739
|
