Previous reports shows rimonabant's inverse properties may be a limiting factor for treating cannabinoid dependence. To overcome this limitation, neutral antagonists were developed, to address mechanisms by which an inverse agonist and neutral antagonist elicit withdrawal.Tai, SherricaNikas, Spyros P....
An inverse agonist, also known as a negative antagonist, is a type of ligand that exhibits negative efficacy. It is suggested that the nomenclature of inverse agonism should be expanded to include ligands that act at ectopic sites on receptors, reflecting the underlying topology of interaction. ...
Inverse agonist and neutral antagonist actions of synthetic compounds at an insect 5-HT1 receptor. Troppmann B, Balfanz S, Baumann A, Blenau W (2010) Inverse agonist and neutral antagonist actions of synthetic compounds at an insect 5-HT1 receptor... B Troppmann,S Balfanz,A Baumann,... -...
www.nature.com/scientificreports OPEN S 38093, a histamine H3 antagonist/ inverse agonist, promotes hippocampal neurogenesis and received: 10 October 2016 accepted: 17 January 2017 Published: 20 February 2017 improves context discrimination task in aged mice Jean-Philippe Guilloux1,*, Benjamin A...
Oral administration of the opioid antagonist nalmefene alone (up to 20 mg/kg) failed to show a significant effect on acute food intake in mice. However, combined oral dosing of nalmefene and subthreshold doses of AM251, a cannabinoid CB1 receptor inverse agonist, led to a significant reductio...
In this double-blind, randomized multicenter 28-day study, the tolerability and efficacy of pimavanserin was compared with placebo in 60 patients with L-DOPA or dopamine (DA) agonist-induced PDP. Motor function was evaluated using the Unified Parkinson's Disease Rating Scale (UPDRS) Parts II ...
with their cognate trimeric ligands.2 As many TNF receptor superfamily members have significant roles in the progression of human disease,3 a better understanding of their signalling mechanisms could enable the design of potent agonist and antagonist molecules as candidate drugs for clinical development....
Williams, CEP-26401 (irdabisant), a potent and selective histamine H3 receptor antagonist/inverse agonist with cognition-enhancing and wake-promoting ... Robert,L.,Hudkins,... - 《Journal of Medicinal Chemistry》 被引量: 59发表: 2011年 3,4-Diaza-bicyclo[4.1.0]hept-4-en-2-one phenoxypro...
Effects of an intrathecally adminis- tered benzodiazepine receptor agonist, antagonist and inverse agonist on morphine-induced inhibition of a spinal nociceptive reflex. Br J Pharmacol 1988; 93: 964-8.Morean JL, Pieri L. Effects of an intrathecally administered ben- zodiazepine receptor agonist ...
The stimulatory effect of VIP and other agonist was preserved. This suggested that VPAC 1 (1–436) and (1–441) receptors had a constitutive activity. The selective VPAC 1 receptor antagonist Ac His 1 [ d -Phe 2 , K 15 , R 16 , L 27 ] VIP (3–7)/GRF (8–27) reduced by ...