Potent neuropeptide Y Y1 receptor antagonist, 1229U91: blockade of neuropeptide Y-induced and physiological food intake.
نویسندگان
چکیده
منابع مشابه
A potent neuropeptide Y antagonist, 1229U91, suppressed spontaneous food intake in Zucker fatty rats.
Neuropeptide Y (NPY) is one of the most potent orexigenic substances known. 1229U91 was found to be a potent and selective NPY antagonist. To elucidate a physiological role of NPY in hyperphagia in obese animals, we studied the effect of 1229U91 on spontaneous food intake in obese and lean Zucker rats. The food intake of Zucker rats was suppressed by intracerebroventricular administration of 12...
متن کاملSynthetic routes to the Neuropeptide Y Y1 receptor antagonist 1229U91 and related analogues for SAR studies and cell-based imaging.
The potent Y1 receptor antagonist, 1229U91 has an unusual cyclic dimer structure that makes syntheses of analogue series quite challenging. We have examined three new routes to the synthesis of such peptides that has given access to novel structural variants including heterodimeric compounds, ring size variants and labelled conjugates. These compounds, including a fluorescently labelled analogu...
متن کاملPharmacological Characterization of I-1229U91 Binding to Y1 and Y4 Neuropeptide Y/Peptide YY Receptors
1229U91 (GW1229 or GR231118) [lle,Glu,Pro,Dpr,Tyr, Arg,Leu,Arg,Tyr-NH2)2 cyclic (2,49),(294)-diamide] has been reported by several research groups to be a potent antagonist at the Y1 neuropeptide Y (NPY) receptor subtype. However, 1229U91 also displaces I-peptide YY (PYY) with high affinity from the Y4 subtype. Previously, we reported that 1229U91 had full agonist properties for the Y4 receptor...
متن کاملPharmacological characterization of (125)I-1229U91 binding to Y1 and Y4 neuropeptide Y/Peptide YY receptors.
1229U91 (GW1229 or GR231118) [lle,Glu,Pro,Dpr,Tyr, Arg,Leu,Arg, Tyr-NH(2))2 cyclic (2,4'),(2'4)-diamide] has been reported by several research groups to be a potent antagonist at the Y1 neuropeptide Y (NPY) receptor subtype. However, 1229U91 also displaces (125)I-peptide YY (PYY) with high affinity from the Y4 subtype. Previously, we reported that 1229U91 had full agonist properties for the Y4 ...
متن کامل[Leu31, Pro34]neuropeptide Y: a specific Y1 receptor agonist.
Two types of binding sites have previously been described for 36-amino acid neuropeptide Y (NPY), called Y1 and Y2 receptors. Y2 receptors can bind long C-terminal fragments of NPY-e.g., NPY-(13-36)-peptide. In contrast, Y1 receptors have until now only been characterized as NPY receptors that do not bind such fragments. In the present study an NPY analog is presented, [Leu31, Pro34]NPY, which ...
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ژورنال
عنوان ژورنال: Endocrinology
سال: 1996
ISSN: 0013-7227,1945-7170
DOI: 10.1210/endo.137.8.8754736