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Restrict the search for
adenosine
to a specific field?
Status:
Other
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
First synthesized in 2004 by the group of Peter G. Schultz, reversine is a 2,6- diamino substituted purine showing a potent inhibition on Aurora B, a protein kinase overexpressed in a variety of solid tumors. Due to its relevance in the cell cycle regulation, Aurora B represents a good target for anti-cancer drug development, so that reversine can be used as a promising lead compound for new potential antitumor agents. Reversine is a potent human A3 adenosine receptor antagonist with Ki of 0.66 μM, and a pan-aurora A/B/C kinase inhibitor with IC50 of 12 nM/13 nM/20 nM, respectively. Reversine also inhibits Mps1. Reversine is effective in inhibiting the growth of thyroid cancer cells by cell cycle arrest or apoptosis, especially with the more aggressive ATC and PDTC. Apoptosis was induced by the mitochondria-independent pathway. Reversine is being under investigation in clinical therapeutics.
Status:
Other
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
2-Phenylaminoadenosine (CV-1808) is an adenosine A2 receptor agonist. CV-1808 is a coronary vasodilator, antihypertensive and antipsychotic following systemic administration in vivo. CV-1808 appeared to be effective for salvaging ischemic myocardium. The effect might be related to improvement of coronary circulation and inhibition of release of vasoactive substances, including TXA2, from the ischemic myocardium. Development of CV-1808 has been discontinued in the United States.
2-Fluoroadenosine (F-Ado) was developed at Southern Research Institute in 1957 as a potential anticancer drug. 2-Fluoroadenosine is not deaminated by adenosine deaminase but metabolized to triphosphate as shown in vitro. The drug was also shown to be a potent inhibitor of lymphocyte-mediated cytolysis.
Status:
Other
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
1,3-Dipropylxanthine is an A1 and A2 adenosine receptors inhibitor. It is selective for the A1 receptors. 1,3-Dipropylxanthine was about 2- to 3-fold more potent than theophylline at A2 receptors, while being 5- to 6-fold more potent at A1 receptors.
Status:
Other
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
GR79236 is an adenosine A1 receptor agonist, which possesses cardiovascular and antilipolytic properties. GR79236 was studied in model animals for the treatment of diabetic ketoacidosis and in patients for pain relief. However, these studies were discontinued. In addition, analgesic efficacy of GR79236 was investigated in the dental pain model. Nevertheless, there was no evidence of efficacy of GR79236. A higher dose of GR79236 might have been effective or that was suggested, that intravenous administration of that drug did not achieve appropriate concentrations in the brain or peripheral nerves.
Status:
Other
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Strophanthidin is a cardiotonic steroid that decreases the potassium content and raises the sodium content in rabbit renal cortex slices. In addition, strophanthidin induced two different types of membrane depolarization: a small, reversible depolarization with a peak amplitude of 4 +/- 2.6 mV or a prolonged depolarization of large amplitude (48.6 +/- 9.0 mV) with or without a decrease in apparent rat membrane resistance.
