drug inverse agonism


Summary: Phenomena and pharmaceutics of compounds that bind to the same receptor binding-site as an agonist (DRUG AGONISM) for that receptor but exerts the opposite pharmacological effect.

Top Publications

  1. Li X, Anderson M, Collin D, Muegge I, Wan J, Brennan D, et al. Structural studies unravel the active conformation of apo ROR?t nuclear receptor and a common inverse agonism of two diverse classes of ROR?t inhibitors. J Biol Chem. 2017;292:11618-11630 pubmed publisher
  2. Laun A, Song Z. GPR3 and GPR6, novel molecular targets for cannabidiol. Biochem Biophys Res Commun. 2017;490:17-21 pubmed publisher
    ..g. treatment of Alzheimer's disease and Parkinson's disease) may be mediated through these important receptors. ..
  3. Hu L, Chang L, Zhang Y, Zhai L, Zhang S, Qi Z, et al. Platelets Express Activated P2Y12 Receptor in Patients With Diabetes Mellitus. Circulation. 2017;136:817-833 pubmed publisher
  4. Martella A, Sijben H, Rufer A, Grether U, Fingerle J, Ullmer C, et al. A Novel Selective Inverse Agonist of the CB2 Receptor as a Radiolabeled Tool Compound for Kinetic Binding Studies. Mol Pharmacol. 2017;92:389-400 pubmed publisher
    ..Altogether, this study shows that the use of a novel tool compound, i.e., [3H]RO6957022, can support the development of novel ligands with a repertoire of kinetic binding profiles for CB2R. ..
  5. Kianirad Y, Simuni T. Pimavanserin, a novel antipsychotic for management of Parkinson's disease psychosis. Expert Rev Clin Pharmacol. 2017;10:1161-1168 pubmed publisher
    ..The development of pimavanserin as an antipsychotic opened a new therapeutic avenue in the treatment of PDP as well as targeting psychosis in other disorders such as Alzheimer's disease. ..