Hancock, A A
GPCRs. Type 2 ligands can also suppress constitutive activity but interact outside of the agonist binding site (allosteric, ectopic). Thus, type 2 antagonists are predicted to bind concurrently with the agonist and still be able to repress receptor signalling. Remarkable examples of such cases ...
Cruz S, Villarreal J, Volkow N. Further evidence that naloxone acts as an inverse opiate agonist: implications for drug dependence and withdrawal. Life Sci 1996;56(26):381-9.Cruz, S.L., Villarreal, J.E., Volkow, N.D., 1996. Further evidence that naloxone acts as an inverse opiate ...
Compounds of the formula ##STR1## where the symbols have the meaning defined in the specification, have retinoid, retinois antagonist or retinoid inverse agonist type biological activity.
Therefore it may be important that a H3R antagonist would also have inverse agonist activity to both block exogenous histamine effects and to shift the receptor from its constitutively active (inhibitory) form to a neutral state. The wide distribution of H3 receptors in the mammalian CNS indicates...
The cannabinoid CB_1 receptor, a G-protein-cou-pled receptor expressed in the nervous system, has been linked to the control of food intake and energy expenditure in a variety of studies. The CB_1 receptor inverse agonist rimonabant (Acomplia~R) has proven to decrease food intake and ...
Elucidation of an Allosteric Mode of Action for a Thienopyrazole RORγt Inverse AgonistNuclear ReceptorsRORγtAllosteric ModulatorsStructure ElucidationDrug DiscoveryThe demand for allosteric targeting of nuclear receptors is high, but examples are limited, and structural information is scarce. The retinoic...
Drug screening for inverse agonist by monitoring binding of two polypeptides having specific domains in presence of test compounddoi:US6218128 B1Methods of characterizing and identifying negative hormones of nuclear receptors. Also disclosed are methods of making modulators of retinoid nuclear receptor ...
BETA-CARBOLINE-DERIVED COMPOUND WITH BENZODIAZEPIENE-RECEPTOR LIGAND HAVING INVERSE AGONIST AND ANTAGONIST EFFECT, AND DRUG CONTAINING SAMEPURPOSE: To obtain new β-carboline-derived compounds exhibiting compatibility with benzodiazepine receptors and on the other hand having an inverse agonist and ...
combination with an antagonist or inverse agonist of the receptor and are causing a antipsychotic or antidepressant drug h3 and to prevent adverse effects.a psychotropikaMedicament comprising, in a pharmaceutically acceptable vehicle, an anti-psychotic or an antidepressant (A), which, on its own, ...