sm-130686 and Body-Weight

sm-130686 has been researched along with Body-Weight* in 1 studies

Other Studies

1 other study(ies) available for sm-130686 and Body-Weight

Article	Year
Oxindole derivatives as orally active potent growth hormone secretagogues. Journal of medicinal chemistry, 2001, Dec-20, Volume: 44, Issue:26 A series of substituted oxindole derivatives was synthesized and evaluated for growth hormone (GH) releasing activity using cultured rat pituitary cells. (+)-6-Carbamoyl-3-(2-chlorophenyl)-(2-diethylaminoethyl)-4-trifluoromethyloxindole (SM-130686, 37S) was found to have potent activity (EC(50) = 3.0 nM), while the other enantiomer 37R had reduced activity. The absolute configuration of 37S was confirmed by X-ray crystallographic analysis. Compound 37S showed a good pharmacokinetic profile in rats with 28% oral bioavailability at 10 mg/kg and excellent in vivo activity as evidenced by a significant weight gain after 4 days of oral administration at 10 mg/kg twice a day. Compound 37S displaced the binding of (35)S-MK-677 to human GHS-R with an IC(50) value of 1.2 +/- 0.2 nM. Topics: Administration, Oral; Animals; Biological Availability; Body Weight; CHO Cells; Cricetinae; Crystallography, X-Ray; Ethylamines; Female; Growth Hormone; Human Growth Hormone; Humans; In Vitro Techniques; Indoles; Male; Models, Molecular; Molecular Conformation; Pituitary Gland, Anterior; Rats; Rats, Inbred F344; Rats, Wistar; Receptors, Cell Surface; Receptors, G-Protein-Coupled; Receptors, Ghrelin; Stereoisomerism; Structure-Activity Relationship	2001

Article

Year

Oxindole derivatives as orally active potent growth hormone secretagogues.

Journal of medicinal chemistry, 2001, Dec-20, Volume: 44, Issue:26

A series of substituted oxindole derivatives was synthesized and evaluated for growth hormone (GH) releasing activity using cultured rat pituitary cells. (+)-6-Carbamoyl-3-(2-chlorophenyl)-(2-diethylaminoethyl)-4-trifluoromethyloxindole (SM-130686, 37S) was found to have potent activity (EC(50) = 3.0 nM), while the other enantiomer 37R had reduced activity. The absolute configuration of 37S was confirmed by X-ray crystallographic analysis. Compound 37S showed a good pharmacokinetic profile in rats with 28% oral bioavailability at 10 mg/kg and excellent in vivo activity as evidenced by a significant weight gain after 4 days of oral administration at 10 mg/kg twice a day. Compound 37S displaced the binding of (35)S-MK-677 to human GHS-R with an IC(50) value of 1.2 +/- 0.2 nM.

Topics: Administration, Oral; Animals; Biological Availability; Body Weight; CHO Cells; Cricetinae; Crystallography, X-Ray; Ethylamines; Female; Growth Hormone; Human Growth Hormone; Humans; In Vitro Techniques; Indoles; Male; Models, Molecular; Molecular Conformation; Pituitary Gland, Anterior; Rats; Rats, Inbred F344; Rats, Wistar; Receptors, Cell Surface; Receptors, G-Protein-Coupled; Receptors, Ghrelin; Stereoisomerism; Structure-Activity Relationship

2001