Histamine H3 receptor agonists

被引：12

作者：

De Esch, IJP ^{[1
]}

Belzar, KJ ^{[1
]}

机构：

[1] De Novo Pharmaceut, Cambridge CB4 9ZR, England

来源：

MINI-REVIEWS IN MEDICINAL CHEMISTRY | 2004年 / 4卷 / 09期

关键词：

Histamine; H-3; GPCR; agonist; isoform; activity; efficacy; affinity;

D O I：

10.2174/1389557043403134

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The SAR of H-3 ligands has been difficult to evaluate because of species differences, multiple isoforms and constitutive activity, among other complicating factors. A review is given of the sometimes-conflicting affinity, activity and efficacy data of H-3 agonists that has been described in literature to date.

引用

页码：955 / 963

页数：9

共 50 条

[31] Identification of the Antiarrhythmic Drugs Amiodarone and Lorcainide as Potent H3 Histamine Receptor Inverse Agonists
Del Tredici, Andria L.
Ma, Jian-Nong
Piu, Fabrice
Burstein, Ethan S.
JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS, 2014, 348 (01): : 116 - 124
[32] Discovery of Novel Steroid-Based Histamine H3 Receptor Antagonists/Inverse Agonists
Ledneczki, Istvan
Tapolcsanyi, Pal
Gabor, Eszter
Eles, Janos
Barabas, Julia
Beni, Zoltan
Varga, Balazs
Balazs, Ottilia
Roman, Viktor
Fodor, Laszlo
Szikra, Judit
Vastag, Monika
Levay, Gyorgy
Schmidt, Eva
Lendvai, Balazs
Greiner, Istvan
Kiss, Bela
Nemethy, Zsolt
Maho, Sandor
JOURNAL OF MEDICINAL CHEMISTRY, 2024, 67 (05) : 3643 - 3667
[33] Synthesis and structure-activity relationships of conformationally constrained histamine H3 receptor agonists
Kitbunnadaj, R
Zuiderveld, OP
De Esch, IJP
Vollinga, RC
Bakker, R
Lutz, M
Spek, AL
Cavoy, E
Deltent, MF
Menge, WMPB
Timmerman, H
Leurs, R
JOURNAL OF MEDICINAL CHEMISTRY, 2003, 46 (25) : 5445 - 5457
[34] Augmentation by histamine H3 receptor agonists of methamphetamine-induced stereotypical biting in mice
Kitanaka, Junichi
Kitanaka, Nobue
Tatsuta, Tomohiro
Tanaka, Koh-ichi
Nishiyama, Nobuyoshi
Morita, Yoshio
Takemura, Motohiko
JOURNAL OF PHARMACOLOGICAL SCIENCES, 2010, 112 : 187P - 187P
[35] Synthesis, potency, and in vivo profiles of quinoline containing histamine H3 receptor inverse agonists
Altenbach, Robert J.
Liu, Huaqing
Banfor, Patricia N.
Brownian, Kaitlin E.
Fox, Gerard B.
Fryer, Ryan M.
Komater, Victoria A.
Krueger, Kathleen M.
Marsh, Kennan
Miller, Thomas R.
Pan, Jia Bao
Pan, Liping
Sun, Minghua
Thiffault, Christine
Wetter, Jill
Zhao, Chen
Zhou, Deliang
Esbenshade, Timothy A.
Hancock, Arthur A.
Cowart, Marlon D.
JOURNAL OF MEDICINAL CHEMISTRY, 2007, 50 (22) : 5439 - 5448
[36] Histamine H3 Receptor Agonists Decrease Hypothalamic Histamine Levels and Increase Stereotypical Biting in Mice Challenged with Methamphetamine
Junichi Kitanaka
Nobue Kitanaka
F. Scott Hall
George R. Uhl
Tomohiro Tatsuta
Yoshio Morita
Koh-ichi Tanaka
Nobuyoshi Nishiyama
Motohiko Takemura
Neurochemical Research, 2011, 36 : 1824 - 1833
[37] Histamine H3 Receptor Agonists Decrease Hypothalamic Histamine Levels and Increase Stereotypical Biting in Mice Challenged with Methamphetamine
Kitanaka, Junichi
Kitanaka, Nobue
Hall, F. Scott
Uhl, George R.
Tatsuta, Tomohiro
Morita, Yoshio
Tanaka, Koh-ichi
Nishiyama, Nobuyoshi
Takemura, Motohiko
NEUROCHEMICAL RESEARCH, 2011, 36 (10) : 1824 - 1833
[38] Dynamics of histamine H3 receptor antagonists on brain histamine metabolism:: do all histamine H3 receptor antagonists act at a single site?
Barnes, W
Boyd, D
Hough, L
EUROPEAN JOURNAL OF PHARMACOLOGY, 2001, 431 (02) : 215 - 221
[39] Identification of histamine receptors, and role of the histamine H3 receptor in obesity
Kotani, H
Takahashi, K
Tokita, S
JOURNAL OF PHARMACOLOGICAL SCIENCES, 2005, 97 : 49P - 49P
[40] Potent partial agonists for the histamine H3 receptor lacking a nitrogen atom in the side chain.
Pelloux-Leon, N
Fkyerat, A
Schunack, W
Stark, H
Garbarg, M
Ligneau, X
Schwartz, JC
Ganellin, CR
ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2002, 223 : A88 - A88

← 1 2 3 4 5 →