α-substituted n-(sulfonamido)alkyl-β-aminotetralins: Potent and selective neuropeptide Y Y5 receptor antagonists [2]

Journal of Medicinal Chemistry

Volumn 43, Issue 3, 2000, Pages 346-350

  Youngman, Mark A ^a   McNally, James J ^a   Lovenberg, Timothy W ^b   Reitz, Allen B ^a   Willard, Nicole M ^a   Nepomuceno, Diane H ^b   Wilson, Sandy J ^b   Crooke, Jeffrey J ^a   Rosenthal, Daniel ^a   Vaidya, Anil H ^a   Dax, Scott L ^a  

^a R W JOHNSON PHARMACEUTICAL RES I   (United States)

^b NONE   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

NEUROPEPTIDE Y5 RECEPTOR; TETRALIN DERIVATIVE;

DRUG SCREENING; DRUG STRUCTURE; DRUG SYNTHESIS; FOOD INTAKE; LETTER; PSEUDOGENE; STRUCTURE ANALYSIS;

CELL LINE; HUMANS; RADIOLIGAND ASSAY; RECEPTORS, NEUROPEPTIDE Y; STRUCTURE-ACTIVITY RELATIONSHIP; SULFONAMIDES; TETRAHYDRONAPHTHALENES; TRANSFECTION;

EID: 0034628536     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm990468g     Document Type: Letter

References (33)

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32. 125I]PYY binding.
33. Fasted male Long-Evans rats (180-200 g) were housed individually and maintained on a once-a-day feeding schedule (10 a.m. to 4 p.m.) for 5 days following quarantine to allow the animals to acclimate to feeding on powdered chow (#5002 PMI Certified Rodent Meal) during the allotted time. The chow was made available in an open jar, anchored in the cage by a wire, with a metal follower covering the food to minimize spillage. Water was available ad libitum. Animals were fasted for 18 h prior to testing. At the end of the fasting period, animals were administered compound 7 or 8 or vehicle. Vehicle and test compounds were administered 30 min prior to the experiment and given intraperitoneally (1 mL/kg). The test compound 7 or 8 was individually administered intraperitoneally as a solution or suspension in PEG 200; compound concentrations typically ranged from 1-100 mg/kg, preferably from 10-30 mg/kg. Food intake was measured at 2, 4, and 6 h after administration by weighing the special jar containing the food before the experiment and at the specified times. Percent reduction of food consumption was calculated by subtracting the grams of food consumed by the treated group from the grams of food consumed by the control group, divided by the grams of food consumed by the control group, multiplied by 100.