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In pharmacology, an inverse agonist is a drug that binds to the same receptor as an agonist but induces a pharmacological response opposite to that of the agonist. A neutral antagonist has no activity in the absence of an agonist or inverse agonist but can block the activity of either; [ 1 ] they are in fact sometimes called blockers (examples ...
Convulsions are induced in captive animals, then high doses of anticonvulsant drugs are administered. [10] [11] [12] For example, kainic acid can lead to status epilepticus in animals as it is a cyclic analog of l-glutamate and an agonist for kainate receptors in the brain which makes it a potent neurotoxin and excitant. [citation needed]
Ro15-4513 is a weak partial inverse agonist of the benzodiazepine class of drugs, developed by Hoffmann–La Roche in the 1980s. [1] It acts as an inverse agonist (which acts in a similar way as a competitive antagonist), and can therefore be an antidote to the acute impairment caused by alcohols, including ethanol, isopropanol, tert-butyl alcohol, tert-amyl alcohol, 3-methyl-3-pentanol ...
Eplivanserin (Sanofi Aventis) – sleeping pill that reached phase II trials (but for which the application for approval was withdrawn), acts as a selective 5-HT 2A inverse agonist. Nelotanserin (APD-125) – selective 5-HT 2A inverse agonist developed by Arena Pharmaceuticals for the treatment of insomnia. APD-125 was shown to be effective and ...
It is an inverse agonist of the histamine H 3 receptor. [3] It represents the first commercially available medication in its class, so that the U.S. Food and Drug Administration (FDA) declares it a first-in-class medication. [7] [8] Pitolisant enhances the activity of histaminergic neurons in the brain that function to improve a person's ...
Pimavanserin acts as a selective inverse agonist or antagonist of the serotonin 5-HT 2A receptor. [2] [10] [9] [11] It is also an antagonist or inverse agonist of the serotonin 5-HT 2C receptor to a lesser extent.
AM-630 (6-Iodopravadoline) is a drug that acts as a potent and selective inverse agonist for the cannabinoid receptor CB 2, with a K i of 32.1 nM at CB 2 and 165x selectivity over CB 1, at which it acted as a weak partial agonist.
AM-251 is an inverse agonist at the CB 1 cannabinoid receptor. AM-251 is structurally very close to rimonabant; both are biarylpyrazole cannabinoid receptor antagonists.In AM-251, the p-chloro group attached to the phenyl substituent at C-5 of the pyrazole ring is replaced with a p-iodo group.