Gershengorn, "A small molecule inverse agonist
for the human thyroid-stimulating hormone receptor," Endocrinology, vol.
A clinical trial assessing the safety and efficacy of the CB1R inverse agonist
taranabant in obese and overweight patients: low-dose study.
For example, GABAA receptor antagonists and inverse agonists
(3) decrease alcohol self-administration in animals (Hyytia and Koob 1995; Rassnick et al.
Though Ro15-4513 is known to be at least a weak inverse agonist
, he says, "if the dose we were using were producing anxiety, we would have been able to pick it up" on the behavioral test they administered to rats.
The pipeline includes CRB-4001, a 2nd generation, selective cannabinoid receptor type 1 (CB1) inverse agonist
designed to be peripherally restricted.
activity of selected ligands of the cysteinyl-leukotriene receptor 1.
Taranabant is a structurally distinct, highly selective cannabinoid-1 (CB-I) receptor inverse agonist
under investigation for the treatment of obesity.
Discovered by Arena, APD125 is a novel and orally bioavailable, highly selective inverse agonist
of the 5-HT2A serotonin receptor.
Pimavanserin is a selective serotonin inverse agonist
and antagonist preferentially targeting 5-HT2A receptors.
AUR-101 is a selective, potent inverse agonist
of the receptor RoR?t, designed as an oral agent for the treatment of IL17-driven immunological conditions, including psoriasis.
Pimavanserin is a potent 5-HT2A inverse agonist
and 5-HT2C inverse agonist
, with 5-fold greater affinity for the 5-HT2A receptor.
But some panelists questioned whether some of the psychiatric and neurologic side effects with Zimulti might indicate that it was acting as an inverse agonist
on the endocannabinoid system, meaning the drug would lock the receptors into inactivity and lead to negative consequences.