HIGH-AFFINITY NEUROPEPTIDE-Y RECEPTOR ANTAGONISTS

被引：142

作者：

DANIELS, AJ ^{[1
]}

MATTHEWS, JE ^{[1
]}

SLEPETIS, RJ ^{[1
]}

JANSEN, M ^{[1
]}

VIVEROS, OH ^{[1
]}

TADEPALLI, A ^{[1
]}

HARRINGTON, W ^{[1
]}

HEYER, D ^{[1
]}

LANDAVAZO, A ^{[1
]}

LEBAN, JJ ^{[1
]}

SPALTENSTEIN, A ^{[1
]}

机构：

[1] BURROUGHS WELLCOME CO,DIV ORGAN CHEM,RES TRIANGLE PK,NC 27709

来源：

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA | 1995年 / 92卷 / 20期

关键词：

D O I：

10.1073/pnas.92.20.9067

中图分类号：

O [数理科学和化学]; P [天文学、地球科学]; Q [生物科学]; N [自然科学总论];

学科分类号：

07 ; 0710 ; 09 ;

摘要：

Neuropeptide Y (NPY) is one of the most abundant peptide transmitters in the mammalian brain. In the periphery it is costored and coreleased with norepinephrine from sympathetic nerve terminals. However, the physiological functions of this peptide remain unclear because of the absence of specific high-affinity receptor antagonists. Three potent NPY receptor antagonists were synthesized and tested for their biological activity in in vitro, ex vivo, and in vivo functional assays. We describe here the effects of these antagonists inhibiting specific radiolabeled NPY binding at Y1 and Y2 receptors and antagonizing the effects of NPY in human erythroleukmia cell intracellular calcium mobilization, perfusion pressure in the isolated rat kidney, and mean arterial blood pressure in anesthetized rats.

引用

页码：9067 / 9071

页数：5

共 24 条

[1] NEUROPEPTIDE-Y DISTRIBUTION IN HUMAN-BRAIN
ADRIAN, TE
ALLEN, JM
BLOOM, SR
GHATEI, MA
ROSSOR, MN
ROBERTS, GW
CROW, TJ
TATEMOTO, K
POLAK, JM
[J]. NATURE, 1983, 306 (5943) : 584 - 586
[2] [D-TRP(32)]NEUROPEPTIDE-Y - A COMPETITIVE ANTAGONIST OF NPY IN RAT HYPOTHALAMUS
BALASUBRAMANIAM, A
SHERIFF, S
JOHNSON, ME
PRABHAKARAN, M
HUANG, Y
FISCHER, JE
CHANCE, WT
[J]. JOURNAL OF MEDICINAL CHEMISTRY, 1994, 37 (06) : 811 - 815
[3] STRUCTURE-ACTIVITY-RELATIONSHIPS OF NEUROPEPTIDE-Y ANALOGS WITH RESPECT TO Y-1 AND Y-2 RECEPTORS
BECKSICKINGER, AG
JUNG, G
[J]. BIOPOLYMERS, 1995, 37 (02) : 123 - 142
[4] NONPEPTIDE PEPTIDOMIMETIC ANTAGONISTS OF THE NEUROPEPTIDE-Y RECEPTOR - BENEXTRAMINE ANALOGS WITH SELECTIVITY FOR THE PERIPHERAL Y-2 RECEPTOR
CHAURASIA, C
MISSE, G
TESSEL, R
DOUGHTY, MB
[J]. JOURNAL OF MEDICINAL CHEMISTRY, 1994, 37 (14) : 2242 - 2248
[5] DANIELS AJ, 1992, MOL PHARMACOL, V41, P767
[6] DANIELS AJ, 1989, BIOCHEM BIOPH RES CO, V187, P1138
[7] DANIELS AJ, 1994, Patent No. 9400486
[8] BENEXTRAMINE NEUROPEPTIDE-Y RECEPTOR INTERACTIONS - CONTRIBUTION OF THE BENZYLIC MOIETIES TO [H-3] NEUROPEPTIDE-Y DISPLACEMENT ACTIVITY
DOUGHTY, MB
CHAURASIA, CS
LI, K
[J]. JOURNAL OF MEDICINAL CHEMISTRY, 1993, 36 (02) : 272 - 279
[9] [LEU31,PRO34]NEUROPEPTIDE-Y - A SPECIFIC Y-1 RECEPTOR AGONIST
FUHLENDORFF, J
GETHER, U
AAKERLUND, L
LANGELANDJOHANSEN, N
THOGERSEN, H
MELBERG, SG
OLSEN, UB
THASTRUP, O
SCHWARTZ, TW
[J]. PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 1990, 87 (01) : 182 - 186
[10] CHARACTERIZATION OF FUNCTIONAL NEUROPEPTIDE-Y RECEPTORS IN A HUMAN NEUROBLASTOMA CELL-LINE
GORDON, EA
KOHOUT, TA
FISHMAN, PH
[J]. JOURNAL OF NEUROCHEMISTRY, 1990, 55 (02) : 506 - 513

← 1 2 3 →