Concepedia

Allosteric Antagonists

Allosteric Antagonist is a type of allosteric modulator that binds to a site distinct from the orthosteric site of a receptor and induces a conformational change that reduces or inhibits the receptor's activity in response to its endogenous agonist.

103

Publications

5.6K

Citations

731

Authors

203

Institutions

Publications per year

2017–2026

26

Variants

Allosteric Inhibitors

Parents

Publications

103

Human eosinophil major basic protein is an endogenous allosteric antagonist at the inhibitory muscarinic M2 receptor.

David B. Jacoby, Gerald J. Gleich, A.D. Fryer · Journal of Clinical Investigation · 1993 · 338 citations · Full text

, , +16

Fenobam: A Clinically Validated Nonbenzodiazepine Anxiolytic Is a Potent, Selective, and Noncompetitive mGlu5 Receptor Antagonist with Inverse Agonist Activity

Richard H. Porter, Georg Jaeschke, Will Spooren et al. · Journal of Pharmacology and Experimental Therapeutics · 2005 · 314 citations · Full text

, , +15

The CCR5 Receptor-Based Mechanism of Action of 873140, a Potent Allosteric Noncompetitive HIV Entry Inhibitor

Christian Watson, Stephen Jenkinson, Wieslaw M. Kazmierski et al. · Molecular Pharmacology · 2005 · 302 citations

, , +16

Structure of CC chemokine receptor 2 with orthosteric and allosteric antagonists

Yi Zheng, Ling Qin, Natalia V. Ortiz Zacarı́as et al. · Nature · 2016 · 296 citations · Full text

, , +14

In primary cultures of cerebellar granule cells the activation of N-methyl-D-aspartate-sensitive glutamate receptors induces c-fos mRNA expression.

A M Szekely, Maria Luisa Barbaccia, Hannu Alho et al. · Molecular Pharmacology · 1989 · 252 citations

, , +17

1–5 of 103

Authors

731

  1. PJ
    P. Jeffrey Conn

    Vanderbilt University, United States

    6 publications · 318 citations

    6

    h-index

  2. KM
    Klaus Mohr

    University of Bonn, Germany

    4 publications · 196 citations

    4

    h-index

  3. HO
    Hisashi Ohta

    Food Research Institute, Japan

    3 publications · 182 citations

    3

    h-index

  4. AP
    Adriaan P. IJzerman

    Centre for Human Drug Research, Netherlands

    3 publications · 381 citations

    3

    h-index

  5. GS
    Gisbert Schneider

    ETH Zurich, Switzerland

    3 publications · 84 citations

    3

    h-index

1–5 of 731

Institutions

203

  1. Novartis (Switzerland)

    Basel, Switzerland

    6 h-index

    42 publications

    3.4K citations

  2. University of Bonn

    Bonn, Germany

    6 h-index

    27 publications

    1.4K citations

  3. Vanderbilt University Medical Center

    Nashville, United States

    5 h-index

    40 publications

    1.2K citations

  4. Vanderbilt University

    Nashville, United States

    5 h-index

    8 publications

    273 citations

  5. Latvijas Organiskās Sintēzes Institūts

    Riga, Latvia

    4 h-index

    10 publications

    308 citations

  6. Leiden University

    Leiden, The Netherlands

    4 h-index

    28 publications

    2.1K citations

  7. Goethe University Frankfurt

    Frankfurt am Main, Germany

    4 h-index

    11 publications

    374 citations

  8. MerLion Pharma (Germany)

    Berlin, Germany

    4 h-index

    22 publications

    536 citations

1–8 of 203

Venues

  1. Molecular Pharmacology

    11 publications · 1.1K citations

    11

    h-index

  2. Journal of Medicinal Chemistry

    9 publications · 351 citations

    9

    h-index

  3. 7

    h-index

  4. Bioorganic & Medicinal Chemistry Letters

    7 publications · 163 citations

    7

    h-index

  5. British Journal of Pharmacology

    BJP · 4 publications · 230 citations

    4

    h-index

1–5