geoscience.net logo
+ Resolve Article
+ Follow Us
Follow on FacebookFollow on Facebook
Follow on TwitterFollow on Twitter

+ Translate
+ Subscribe to Site Feed
GeoScience Most Shared ContentMost Shared Content

Suppression of food intake and food-reinforced behavior produced by the novel CB1 receptor antagonist/inverse agonist AM 1387


, : Suppression of food intake and food-reinforced behavior produced by the novel CB1 receptor antagonist/inverse agonist AM 1387. Pharmacology, Biochemistry, and Behavior 83(3): 396-402

Cannabinoid CB1 receptor antagonist/inverse agonists are becoming increasingly recognized for their potential therapeutic utility as appetite suppressants. In the current paper we characterize the biochemical and behavioral effects of AM 1387, which is a novel CB1 antagonist. AM 1387 exhibited binding affinity and selectivity for the CB1 over the CB2 receptor. Moreover, AM 1387 decreased GTP gamma S (EC50: 22.82nM) and increased forskolin-stimulated cAMP (EC50: 274.6nM), as did the CB1 inverse agonist AM 251 (GTP gamma S EC50: 25.82nM; cAMP EC50: 363.8nM), indicating that AM1387 also has inverse agonist properties in vitro. In the behavioral characterization in rats, AM 1387 suppressed lever pressing for food on two operant schedules (fixed-ratio 1 and 5). Timecourse of the effect on fixed-ratio 5 responding was then determined, and the half-life (t(1/2)=4.87 h) was found to be threefold shorter than what has been shown for SR 141716A, and fourfold shorter than AM 251. Finally, AM 1387 was found to suppress food intake using three diets of differing macronutrient composition and palatability. It was concluded that AM 1387 may be a useful tool for examining the effects of CBI receptor antagonism or inverse agonism on food intake. (c) 2006 Elsevier Inc. All rights reserved.

US$19.90

PMID: 16616951

DOI: 10.1016/j.pbb.2006.02.022


Other references

May, A.G.; DeWesse, J.A.; Rob, C.G., 1965: Arterialized in situ saphenous vein. Archives of Surgery 91(5): 743-750

Chang, B.H.; Bae, Y.C.an, 2003: Salting-out in the aqueous single-protein solution: The effect of shape factor. A molecular-thermodynamic model is developed to describe salt-induced protein precipitation. The protein-protein interaction goes through the potential of mean force. An equation of state is derived based on the generalized van der Waals partition...

Volckaert, A.; D.B.uyne, R.; Van der Niepen, P.; Cauchie, P.; Van Belle, S., 1987: Systemic hypersensitivity reaction due to sulfadiazin. Acta Clinica Belgica 42(5): 381-383

Ostertag, S.-G.F.ayer, W., W., 1983: Feeding the premature infant - general principles. Small premature infants have special nutritional requirements. Current knowledge is this area related to nutritional requirements, functioning of the digestive tract and new product formulation are discussed. Basic goals and objectives have been t...

Maruthamuthu, M.Kannan.; Ganesh, I.; Ravikumar, S.; Hong, S.Ho., 2015: Evaluation of zraP gene expression characteristics and construction of a lead (Pb) sensing and removal system in a recombinant Escherichia coli. A ZraP-based lead sensing and removal system was constructed in E. coli. It was regulated by the ZraS/ZraR two-component system. The expression profile of the zraP gene towards extracellular lead was studied via real-time PCR. A dual-function bact...

Spadea, L.; Ablasi, M.A.; D'amico, M.; Dragani, T.; Balestrazzi, E., 1994: Corneal endothelium and excimer laser photorefractive keratectomy A specular microscopy study. Investigative Ophthalmology & Visual Science 35(4): 2016

Tulchinsky, E.; Riolo, L., 1994: A Biomechanical Motion Analysis of the Violinist's Bow Arm. A large percentage of musicians, especially violinists, are affected by occupationally related repetitive motion injuries that alter their musical performances. Normal motion of a violinist's upper extremity must first be analyzed to generate...

Shtykov; Vij; Lewis; Hird; Goodby, 2000: Field-induced phase transitions in an antiferroelectric liquid crystal using the pyroelectric effect. The antiferroelectric liquid crystal (AFLC) under investigation possesses different helical polar phases. Measurements of pyroelectric response of these phases as a function of temperature and bias field have elucidated the ability of this method...

Dhaliwal, B.; Yuan, D.; Pang, M.O.Y.; Henry, A.J.; Cain, K.; Oxbrow, A.; Fabiane, S.M.; Beavil, A.J.; McDonnell, J.M.; Gould, H.J.; Sutton, B.J., 2012: Crystal structure of IgE bound to its B-cell receptor CD23 reveals a mechanism of reciprocal allosteric inhibition with high affinity receptor FcεRI. The role of IgE in allergic disease mechanisms is performed principally through its interactions with two receptors, FcεRI on mast cells and basophils, and CD23 (FcεRII) on B cells. The former mediates allergic hypersensitivity, the latter regul...

Sauvage, H.E., 1896: Les Crocodiliens et les Dinosauriens des Terrains Mesozoiques du Portugal. Bulletin de la Societe Geologique de France, 3(xxiv): 46-48