lu-aa33810 and Mood-Disorders

lu-aa33810 has been researched along with Mood-Disorders* in 1 studies

Other Studies

1 other study(ies) available for lu-aa33810 and Mood-Disorders

Article	Year
Discovery of Lu AA33810: a highly selective and potent NPY5 antagonist with in vivo efficacy in a model of mood disorder. Bioorganic & medicinal chemistry letters, 2011, Sep-15, Volume: 21, Issue:18 The structure-activity relationship of a series of tricyclic-sulfonamide compounds 11-32 culminating in the discovery of N-[trans-4-(4,5-dihydro-3,6-dithia-1-aza-benzo[e]azulen-2-ylamino)-cyclohexylmethyl]-methanesulfonamide (15, Lu AA33810) is reported. Compound 15 was identified as a selective and high affinity NPY5 antagonist with good oral bioavailability in mice (42%) and rats (92%). Dose dependent inhibition of feeding was observed after i.c.v. injection of the selective NPY5 agonist ([cPP(1-7),NPY(19-23),Ala(31),Aib(32),Gln(34)]-hPP). In addition, ip administration of Lu AA33810 (10 mg/kg) produced antidepressant-like effects in a rat model of chronic mild stress. Topics: Animals; Benzothiepins; Biological Availability; Disease Models, Animal; Dose-Response Relationship, Drug; Drug Discovery; Drug Evaluation, Preclinical; Mice; Molecular Structure; Mood Disorders; Rats; Receptors, Neuropeptide Y; Stereoisomerism; Structure-Activity Relationship; Sulfonamides	2011

Article

Year

Discovery of Lu AA33810: a highly selective and potent NPY5 antagonist with in vivo efficacy in a model of mood disorder.

Bioorganic & medicinal chemistry letters, 2011, Sep-15, Volume: 21, Issue:18

The structure-activity relationship of a series of tricyclic-sulfonamide compounds 11-32 culminating in the discovery of N-[trans-4-(4,5-dihydro-3,6-dithia-1-aza-benzo[e]azulen-2-ylamino)-cyclohexylmethyl]-methanesulfonamide (15, Lu AA33810) is reported. Compound 15 was identified as a selective and high affinity NPY5 antagonist with good oral bioavailability in mice (42%) and rats (92%). Dose dependent inhibition of feeding was observed after i.c.v. injection of the selective NPY5 agonist ([cPP(1-7),NPY(19-23),Ala(31),Aib(32),Gln(34)]-hPP). In addition, ip administration of Lu AA33810 (10 mg/kg) produced antidepressant-like effects in a rat model of chronic mild stress.

Topics: Animals; Benzothiepins; Biological Availability; Disease Models, Animal; Dose-Response Relationship, Drug; Drug Discovery; Drug Evaluation, Preclinical; Mice; Molecular Structure; Mood Disorders; Rats; Receptors, Neuropeptide Y; Stereoisomerism; Structure-Activity Relationship; Sulfonamides

2011