8 products were found matching "Cay16470"!

Promethazine is a first-generation histamine H1 receptor antagonist (Ki = 0.98 nM for the human receptor). It is selective for histamine H1 over H3 and H4 receptors (Kis = >100 and 77.6 µM, respectively, for the human receptors). Promethazine also binds muscarinic acetylcholine receptors (mAChRs, Ki = 22 nM). It...

Pyrimethamine is an antiprotozoal agent that is primarily active against P. falciparum, inhibiting the protozoal enzyme dihydrofolate reductase (DHFR). By blocking DHFR activity, pyrimethamine prevents the production of tetrahydrofolic acid, an essential coenzyme involved in DNA and RNA synthesis. In in vivo...

Trimethoprim is a synthetic antibiotic that inhibits dihydrofolate reductase (DHFR), which is necessary for the synthesis of purines, amino acids, and thymidylic acid. Trimethoprim shows prominent selectivity for bacterial DHFR over mammalian DHFR (IC50s = 5 and 30,000 nM, respectively). Formulations containing...

Danazol is a derivative of testosterone (Cay-15645) and ethisterone that can bind to androgen receptors and sex hormone-binding globulin causing a 3-fold increase in free testosterone. It possesses weak androgenic effects and inhibits the production of gonadotropins. It has been used to address symptoms of...

L-(-)-Fucose is a deoxyhexose monosaccharide found on N- and O-linked glycans and glycolipids of a wide variety of organisms. It can exist as a terminal modification of glycan structures or serve as a point of attachment for adding other sugars. In humans, L-(-)-fucose plays a role in A and B blood group antigen...

Rizatriptan is an agonist of the serotonin (5-HT) receptor subtypes 5-HT1B and 5-HT1D (Kis = 4.3 and 10.1 nM, respectively). It is selective for 5-HT1B and 5-HT1D receptors over 5-HT1A receptors (Ki = 140 nM). Rizatriptan induces vasoconstriction in isolated human middle meningeal arteries (EC50 = 90 nM). In vivo,...

Tizanidine is an alpha2-adrenergic receptor (alpha2-AR) agonist. Administration of tizanidine reduces neuronal excitation induced by noxious stimuli and depresses spontaneous neuronal firing in anesthetized cats. Tizanidine-induced neuronal depression is reversed by the selective alpha2-AR antagonist RX781094 but...

Biochanin A is a natural isoflavone with diverse biological actions, most notably as a phytoestrogen. It can affect hormone levels by inhibiting 5alpha-reductase and 17beta-hydroxysteroid dehydrogenase or altering aromatase (CYP19A1) activity. Also known as 4'-methyl genistein, biochanin A can be metabolized in vivo...