Tiotropium is an antagonist that binds to M1, M2, and M3 muscarinic acetylcholine receptors (Kds = 0.43, 0.54, and 0.69 nM, respectively, for human receptors). It decreases acetylcholine-induced contraction of isolated guinea pig trachea in a concentration-dependent manner. In vivo, tiotropium (1 g/L inhaled...

Venturicidin A is a macrolide antibiotic isolated from strains of Streptomyces. It is active against fungi in the genus Venturia which cause apple scab, as well as other fungi, but not against higher plants. Venturicidin A is also cytotoxic against trypanosomes (IC50 = 120-540 ng/ml) while being more than 25,000...

Nicardipine is a dihydropyridine L-type calcium channel antagonist that displays antihypertensive and antianginal activity. It is reported to inhibit adenosine A1, A2A, and A3 receptors with Ki values of 19.6, 63.8, and 3.25 µM, respectively, and can inhibit cytochrome P450 3A4 catalytic activity with an IC50 value...

NF-kappaB p65 is a ubiquitously expressed transcription factor that is a subunit of the NF-kappaB complex and is encoded by the RELA gene in humans. It is composed of an N-terminal Rel homology domain, which contains the nuclear localization signal (NLS), and mediates dimerization, nuclear localization, and DNA and...

Aminoacetone is a threonine and glycine catabolite that can be converted to methylglyoxal by amine oxidases. It has been identified as one of several endogenous sources of methylglyoxal found in the plasma of diabetes patients. As a pro-oxidant, 0.10-5 mM aminoacetone can induce cell death in RINm5f pancreatic...