EFFECTS OF VARIOUS NEUROPEPTIDE-Y PEPTIDE-YY FRAGMENTS ON ELECTRICALLY-EVOKED CONTRACTIONS OF THE RAT VAS-DEFERENS

被引:55
作者
GRUNDEMAR, L
HAKANSON, R
机构
[1] Department of Pharmacology, University of Lund, S-223 62 Lund
关键词
D O I
10.1111/j.1476-5381.1990.tb12075.x
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
1. The effects of various neuropeptide Y (NPY) and peptide YY (PYY) fragments on electrically-evoked twitches in the rat isolated vas deferens were studied and compared with the effects of full length NPY and PYY. The aim was to identify the shortest NPY/PYY fragments that are capable of suppressing the contractions. 2. NPY (1-36) and C-terminal fragments of NPY (from 11-36 to 22-36) suppressed the electrically-evoked twitches in a concentration-dependent manner. On the whole there seemed to be a gradual lowering of the pIC50 values with progressive shortening of the NPY fragments (except for fragments 16-36 and 22-36 that had rather high pIC50 values). NPY 23-36, 24-36 and 25-36 suppressed the twitches at high concentrations (3 μM). NPY 26-36 was without effect as were C-terminal carboxy-deaminated NPY and glycine extended NPY (NPY-Gly-Lys-Arg). 3. PYY (1-36) and C-terminal fragments of PYY (from 11-36 to 23-36) suppressed the electrically-evoked twitches in a concentration-dependent manner. PYY 1-36 was more potent than any of the fragments. There was a tendency for shorter fragments to have lower pIC50 values. PYY 24-36 and 25-36 suppressed the twitches at high concentrations (3 μM). PYY 26-36 was without effect. 4. The findings suggest that the 12 C-terminal amino acid residues of NPY and PYY are the minimum length required to activate the Y2-receptor.
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页码:190 / 192
页数:3
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