Abstract: The present invention relates to a method of treating or preventing obesity (or suppressing the appetite) in a human patient by antagonizing CB1 receptors and inhibiting the enzyme 11?-HSD1 in an amount that is effective to treat or prevent obesity. Compounds useful in the present invention have an ion channel activity level greater than about 2 ?M.

Abstract: A neuropeptide Y Y5 antagonist is useful, alone or in conjunction with other agents, for altering circadian rhythmicity and alleviating circadian rhythm disorders and for enhancing and improving the quality of sleep. The present invention further provides for the use of a medicament for carrying out these methods.

Abstract: Cells and non-human transgenic animals have been engineered to be deficient in the gene encoding the melcanocortin-3 receptor protein (MC-3R). MC-3R deficient transgenic animals have increased fatmass and reduced lean body mass, showing that the MC-3R protein is involved in the regulation of body fat and muscle mass. These MC-3R deficient transgenic animals can be used to select for and test potential modulators of MC-3R. This data allows for methods of screening for MC-3R modulators which effect body weight and associated methods of treating various disorders associated with inappropriate regulation of body weight. The disclosure also relates to a MC-3R/MC-4R double knockout mouse which can be used to select for and test potential modulators (e.g., agonists or antagonists) of MC-3R and/or MC-4R. It is shown that MC-3R serves a non-redundant role, when compared to MC-4R, in the regulation of energy homeostasis.

Abstract: Mutant ob receptors have been made which a) lack a functional first CK-F3 domain; b) lack a functional second CK-F3 domain or c) lack a functional intracellular domain. These receptors may be used in various assays, such as a transactivation assay to identify novel ligands.

Abstract: The present invention is directed to ?.sup.35 S!-N-?1(R)-?(1,2-dihydro-1-methanesulfonylspiro?3H-indole-3,4'-piperidin!- 1'-yl)carbonyl!-2-(phenylmethyloxy)ethyl!-2-amino-2-methylpropanamide, and pharmaceutically acceptable salts thereof. This ?.sup.35 S! radioligand is useful in identifying and characterizing cellular receptors which play a role in the activity of growth hormone secretatogogues. In addition, this ?.sup.35 S! radioligand is useful in assays which test compounds for growth hormone secretagogue activity.