A-119637 is a novel, selective and potent antagonist of the alpha1D adrenoceptor. A-119637 attenuated electrically induced contractions in isolated CC (-logIC(50); 8.12+/-0.15), and relaxed noradrenaline (NA)-contracted preparations by more than 90% at 10(-7) M. The inhibitory effects of A-322312 (10(-7) M) in electrically activated CC were 32.3+/-5.1%, whereas no effect on concentration-response curves for NA […]
A-304121, a piperazine amide, is a potent H3R antagonist. A-304121 potently antagonize native H3Rs by blocking histamine inhibition of potassium-evoked [3H]histamine release from rat brain cortical synaptosomes (pKb values = 8.6 and 9.3) and (R)-alpha-MeHA reversal of electric field-stimulated guinea pig ileum contractions (pA2 values = 7.1 and 8.3). A-304121 is also more efficacious inverse […]
SB-366791 analog is a novel, potent, competitive and selective cinnamide antagonist of the vanilloid receptor (VR1/TRPV1). TRPV1 is a non-selective cation channel, predominantly expressed by peripheral sensory neurones, which is known to play a key role in the detection of noxious painful stimuli, such as capsaicin, acid and heat. In a FLIPR-based Ca(2+)-assay, SB-366791 produced […]
A-315675, a pyrrolidine-based compound, is a novel and potent anti-infuenza agent. It acts as a neuramidase inhibitor and responds well to resistant strains. A-315675 can inhibit A and B strain influenza virus neuraminidases in enzyme assays and influenza virus replication in cell culture. A-315675 effectively inhibited influenza A N1, N2, and N9 and B strain […]
A 204 is a polycyclic antibiotic with a polyether monocarboxylic acid structure. It is originally isolated from fermentation of strain of Streptomyces albus as a crystalline. It has the potential to produce the acute reversible myopathy.
A-192621 is an antagonist of endothelin-B. Endothelins (ETs), 21-amino-acid peptides involved in the pathogenesis of various diseases, bind to ET(A) and ET(B) receptors to initiate their effects. A-192621 can markedly enhance MAP, TPR, and mesenteric, and the renal constrictor effects of ET-1. A-192621 was more effective than IRL-2500 in blocking IRL-1620-induced vasoconstriction, but both augmented […]
A-16316-C is a new water-soluble basic antibiotic isolated together with antibiotic A-396-I and hygromycin B from a streptomyces strain identified as Streptoverticullium eurocidicus. The properties of the antibiotic A-16316-C were similar to those of destomycin B. But it was found that the antibiotic A-16316-C was not identical with destomycin B on the basis of NMR […]
A25822B is an azasterol antifungal agent. It may decrease the ratio of unsaturated to saturated fatty acids. The A25822 antibiotic complex consists of seven biologically active factors. A comparative study of these factors determined that factor B possessed the greatest antifungal activity. The minimal inhibitory concentration of A25822B against isolates of Candida albicans was less […]
A 144 is a bioactive chemical with the name of 4-(((2-Naphthalenylamino)methyl)amino)butanoic acid.
A 31472 is a tetracyclic spiro amine which has previously been shown to have considerable affinity for dopamine D-2 receptors. It is important for defining the pharmacophore for D-2 antagonist activity due to its limited conformational freedom. This compound is important for defining the pharmacophore for D-2 antagonist activity due to their limited conformational freedom. […]