Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts:   Target Concepts:
Query: UMLS:C0020505 (hyperphagia)
6,116 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Melanin-concentrating hormone (MCH) is implicated in the feeding behavior in mammals affording a potential target to control overeating in people. Compound 1 (AMG 076) has been identified as a potent MCHr1 antagonist for the treatment of obesity. A synthesis suitable for the large-scale preparation of this lead candidate was developed to support preclinical studies. A Robinson annulation of benzylpiperidone and resolution of the desired enone from a mixture of the diastereomers afforded key intermediate 6 after a stereoselective hydrogenation. Subsequent Fischer indole synthesis with hydrazine 5 then provided the advanced intermediate, indole 2. Two complementary reductive amination strategies employing either aldehyde 3 or lactol 4 led to the synthesis of title compound 1.
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PMID:Stereoselective synthesis of a MCHr1 antagonist. 1799 73

Although restrained eaters intend to limit their caloric intake, they nevertheless frequently fail and indulge in exactly the foods they want to avoid. Because automatic food-relevant approach tendencies and affective associations may both (independently) contribute to the dysregulation of food intake, the present study was designed to investigate the importance of both processes in relation to high-fat and low-fat food in restrained and unrestrained eaters. Both restrained and unrestrained eaters demonstrated stronger automatic liking associations with high-fat food than with low-fat food items, whereas a similar pattern was absent in their self-reports of liking food. Interestingly, specifically restrained eaters also displayed relatively strong automatic approach tendencies. These results appear to be consistent with the incentive-sensitization theory (Robinson & Berridge, 2001), as overeating seems not so much to be characterized by enhanced liking of food but by stronger automatic approach tendencies towards food.
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PMID:Restrained eaters show enhanced automatic approach tendencies towards food. 2029 30