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Molecular Pharmacology

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Research ArticleArticle

Identifying Drugs that Bind Selectively to Intersubunit General Anesthetic Sites in the α1β3γ2 GABAAR Transmembrane Domain

Selwyn S. Jayakar, Xiaojuan Zhou, David C. Chiara, Carlos Jarava-Barrera, Pavel Y. Savechenkov, Karol S. Bruzik, Mariola Tortosa, Keith W. Miller and Jonathan B. Cohen
Molecular Pharmacology June 2019, 95 (6) 615-628; DOI: https://doi.org/10.1124/mol.118.114975
Selwyn S. Jayakar
Department of Neurobiology, Harvard Medical School, Boston, Massachusetts (S.S.J., D.C.C., J.B.C.); Department of Anesthesia, Critical Care and Pain Medicine, Massachusetts General Hospital, Boston, Massachusetts (X.Z., K.W.M.); Department of Medicinal Chemistry and Pharmacognosy, University of Illinois at Chicago, Chicago, Illinois (P.Y.S., K.S.B.); and the Departamento de Quimica Orgánica, Universidad Autónoma de Madrid, Madrid, Spain (C.J.-B., M.T.)
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Xiaojuan Zhou
Department of Neurobiology, Harvard Medical School, Boston, Massachusetts (S.S.J., D.C.C., J.B.C.); Department of Anesthesia, Critical Care and Pain Medicine, Massachusetts General Hospital, Boston, Massachusetts (X.Z., K.W.M.); Department of Medicinal Chemistry and Pharmacognosy, University of Illinois at Chicago, Chicago, Illinois (P.Y.S., K.S.B.); and the Departamento de Quimica Orgánica, Universidad Autónoma de Madrid, Madrid, Spain (C.J.-B., M.T.)
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David C. Chiara
Department of Neurobiology, Harvard Medical School, Boston, Massachusetts (S.S.J., D.C.C., J.B.C.); Department of Anesthesia, Critical Care and Pain Medicine, Massachusetts General Hospital, Boston, Massachusetts (X.Z., K.W.M.); Department of Medicinal Chemistry and Pharmacognosy, University of Illinois at Chicago, Chicago, Illinois (P.Y.S., K.S.B.); and the Departamento de Quimica Orgánica, Universidad Autónoma de Madrid, Madrid, Spain (C.J.-B., M.T.)
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Carlos Jarava-Barrera
Department of Neurobiology, Harvard Medical School, Boston, Massachusetts (S.S.J., D.C.C., J.B.C.); Department of Anesthesia, Critical Care and Pain Medicine, Massachusetts General Hospital, Boston, Massachusetts (X.Z., K.W.M.); Department of Medicinal Chemistry and Pharmacognosy, University of Illinois at Chicago, Chicago, Illinois (P.Y.S., K.S.B.); and the Departamento de Quimica Orgánica, Universidad Autónoma de Madrid, Madrid, Spain (C.J.-B., M.T.)
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Pavel Y. Savechenkov
Department of Neurobiology, Harvard Medical School, Boston, Massachusetts (S.S.J., D.C.C., J.B.C.); Department of Anesthesia, Critical Care and Pain Medicine, Massachusetts General Hospital, Boston, Massachusetts (X.Z., K.W.M.); Department of Medicinal Chemistry and Pharmacognosy, University of Illinois at Chicago, Chicago, Illinois (P.Y.S., K.S.B.); and the Departamento de Quimica Orgánica, Universidad Autónoma de Madrid, Madrid, Spain (C.J.-B., M.T.)
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Karol S. Bruzik
Department of Neurobiology, Harvard Medical School, Boston, Massachusetts (S.S.J., D.C.C., J.B.C.); Department of Anesthesia, Critical Care and Pain Medicine, Massachusetts General Hospital, Boston, Massachusetts (X.Z., K.W.M.); Department of Medicinal Chemistry and Pharmacognosy, University of Illinois at Chicago, Chicago, Illinois (P.Y.S., K.S.B.); and the Departamento de Quimica Orgánica, Universidad Autónoma de Madrid, Madrid, Spain (C.J.-B., M.T.)
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Mariola Tortosa
Department of Neurobiology, Harvard Medical School, Boston, Massachusetts (S.S.J., D.C.C., J.B.C.); Department of Anesthesia, Critical Care and Pain Medicine, Massachusetts General Hospital, Boston, Massachusetts (X.Z., K.W.M.); Department of Medicinal Chemistry and Pharmacognosy, University of Illinois at Chicago, Chicago, Illinois (P.Y.S., K.S.B.); and the Departamento de Quimica Orgánica, Universidad Autónoma de Madrid, Madrid, Spain (C.J.-B., M.T.)
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Keith W. Miller
Department of Neurobiology, Harvard Medical School, Boston, Massachusetts (S.S.J., D.C.C., J.B.C.); Department of Anesthesia, Critical Care and Pain Medicine, Massachusetts General Hospital, Boston, Massachusetts (X.Z., K.W.M.); Department of Medicinal Chemistry and Pharmacognosy, University of Illinois at Chicago, Chicago, Illinois (P.Y.S., K.S.B.); and the Departamento de Quimica Orgánica, Universidad Autónoma de Madrid, Madrid, Spain (C.J.-B., M.T.)
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Jonathan B. Cohen
Department of Neurobiology, Harvard Medical School, Boston, Massachusetts (S.S.J., D.C.C., J.B.C.); Department of Anesthesia, Critical Care and Pain Medicine, Massachusetts General Hospital, Boston, Massachusetts (X.Z., K.W.M.); Department of Medicinal Chemistry and Pharmacognosy, University of Illinois at Chicago, Chicago, Illinois (P.Y.S., K.S.B.); and the Departamento de Quimica Orgánica, Universidad Autónoma de Madrid, Madrid, Spain (C.J.-B., M.T.)
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Article Information

vol. 95 no. 6 615-628
DOI 
https://doi.org/10.1124/mol.118.114975
PubMed 
30952799

Published By 
American Society for Pharmacology and Experimental Therapeutics
Print ISSN 
0026-895X
Online ISSN 
1521-0111
History 
  • Received October 19, 2018
  • Accepted March 29, 2019
  • Published online May 7, 2019.

Article Versions

  • Earlier version (April 5, 2019 - 12:13).
  • You are viewing the most recent version of this article.
Copyright & Usage 
Copyright © 2019 by The American Society for Pharmacology and Experimental Therapeutics

Author Information

  1. Selwyn S. Jayakar,
  2. Xiaojuan Zhou,
  3. David C. Chiara,
  4. Carlos Jarava-Barrera,
  5. Pavel Y. Savechenkov,
  6. Karol S. Bruzik,
  7. Mariola Tortosa,
  8. Keith W. Miller, and
  9. Jonathan B. Cohen
  1. Department of Neurobiology, Harvard Medical School, Boston, Massachusetts (S.S.J., D.C.C., J.B.C.); Department of Anesthesia, Critical Care and Pain Medicine, Massachusetts General Hospital, Boston, Massachusetts (X.Z., K.W.M.); Department of Medicinal Chemistry and Pharmacognosy, University of Illinois at Chicago, Chicago, Illinois (P.Y.S., K.S.B.); and the Departamento de Quimica Orgánica, Universidad Autónoma de Madrid, Madrid, Spain (C.J.-B., M.T.)
  1. Address correspondence to:
    Jonathan B. Cohen, Department of Neurobiology, Harvard Medical School, 220 Longwood Avenue, Boston, MA 02115. E-mail: jonathan_cohen{at}hms.harvard.edu
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Molecular Pharmacology: 95 (6)
Molecular Pharmacology
Vol. 95, Issue 6
1 Jun 2019
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Research ArticleArticle

Binding Selectivity for α1β3γ2 GABAAR General Anesthetic Sites

Selwyn S. Jayakar, Xiaojuan Zhou, David C. Chiara, Carlos Jarava-Barrera, Pavel Y. Savechenkov, Karol S. Bruzik, Mariola Tortosa, Keith W. Miller and Jonathan B. Cohen
Molecular Pharmacology June 1, 2019, 95 (6) 615-628; DOI: https://doi.org/10.1124/mol.118.114975

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Research ArticleArticle

Binding Selectivity for α1β3γ2 GABAAR General Anesthetic Sites

Selwyn S. Jayakar, Xiaojuan Zhou, David C. Chiara, Carlos Jarava-Barrera, Pavel Y. Savechenkov, Karol S. Bruzik, Mariola Tortosa, Keith W. Miller and Jonathan B. Cohen
Molecular Pharmacology June 1, 2019, 95 (6) 615-628; DOI: https://doi.org/10.1124/mol.118.114975
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