PMID- 29767953
OWN - NLM
STAT- MEDLINE
DCOM- 20191223
LR  - 20191223
IS  - 1948-7193 (Electronic)
IS  - 1948-7193 (Linking)
VI  - 9
IP  - 11
DP  - 2018 Nov 21
TI  - Pharmacological and Electrophysiological Characterization of Novel NMDA Receptor 
      Antagonists.
PG  - 2722-2730
LID - 10.1021/acschemneuro.8b00154 [doi]
AB  - This work reports the synthesis and pharmacological and electrophysiological 
      evaluation of new N-methyl-d-aspartic acid receptor (NMDAR) channel blocking 
      antagonists featuring polycyclic scaffolds. Changes in the chemical structure 
      modulate the potency and voltage dependence of inhibition. Two of the new 
      antagonists display properties comparable to those of memantine, a clinically 
      approved NMDAR antagonist.
FAU - Leiva, Rosana
AU  - Leiva R
AD  - Laboratori de Quimica Farmaceutica (Unitat Associada al CSIC), Facultat de 
      Farmacia i Ciencies de l'Alimentacio i Institut de Biomedicina (IBUB) , 
      Universitat de Barcelona , Av. Joan XXIII, 27-31 , 08028 Barcelona , Spain.
FAU - Phillips, Matthew B
AU  - Phillips MB
AD  - Department of Neuroscience and Center for Neuroscience , University of Pittsburgh 
      , Pittsburgh , Pennsylvania 15260 , United States.
FAU - Turcu, Andreea L
AU  - Turcu AL
AD  - Laboratori de Quimica Farmaceutica (Unitat Associada al CSIC), Facultat de 
      Farmacia i Ciencies de l'Alimentacio i Institut de Biomedicina (IBUB) , 
      Universitat de Barcelona , Av. Joan XXIII, 27-31 , 08028 Barcelona , Spain.
AD  - Neurophysiology Laboratory, Physiology Unit, Department of Biomedicine , Medical 
      School Universitat de Barcelona, August Pi i Sunyer Biomedical Research Institute 
      (IDIBAPS), Barcelona, and Institut of Neurosciences , 08036 Barcelona , Spain.
FAU - Gratacos-Batlle, Esther
AU  - Gratacos-Batlle E
AD  - Neurophysiology Laboratory, Physiology Unit, Department of Biomedicine , Medical 
      School Universitat de Barcelona, August Pi i Sunyer Biomedical Research Institute 
      (IDIBAPS), Barcelona, and Institut of Neurosciences , 08036 Barcelona , Spain.
FAU - Leon-Garcia, Lara
AU  - Leon-Garcia L
AD  - Pharmacology Unit, Faculty of Medicine and Health Sciences , Universitat Rovira i 
      Virgili , C./St. Llorenc 21 , 43201 Reus , Tarragona , Spain.
FAU - Sureda, Francesc X
AU  - Sureda FX
AD  - Pharmacology Unit, Faculty of Medicine and Health Sciences , Universitat Rovira i 
      Virgili , C./St. Llorenc 21 , 43201 Reus , Tarragona , Spain.
FAU - Soto, David
AU  - Soto D
AD  - Neurophysiology Laboratory, Physiology Unit, Department of Biomedicine , Medical 
      School Universitat de Barcelona, August Pi i Sunyer Biomedical Research Institute 
      (IDIBAPS), Barcelona, and Institut of Neurosciences , 08036 Barcelona , Spain.
FAU - Johnson, Jon W
AU  - Johnson JW
AD  - Department of Neuroscience and Center for Neuroscience , University of Pittsburgh 
      , Pittsburgh , Pennsylvania 15260 , United States.
FAU - Vazquez, Santiago
AU  - Vazquez S
AUID- ORCID: 0000-0002-9296-6026
AD  - Laboratori de Quimica Farmaceutica (Unitat Associada al CSIC), Facultat de 
      Farmacia i Ciencies de l'Alimentacio i Institut de Biomedicina (IBUB) , 
      Universitat de Barcelona , Av. Joan XXIII, 27-31 , 08028 Barcelona , Spain.
LA  - eng
GR  - R01 MH045817/MH/NIMH NIH HHS/United States
PT  - Journal Article
PT  - Research Support, N.I.H., Extramural
PT  - Research Support, Non-U.S. Gov't
DEP - 20180601
PL  - United States
TA  - ACS Chem Neurosci
JT  - ACS chemical neuroscience
JID - 101525337
RN  - 0 (Amines)
RN  - 0 (Excitatory Amino Acid Antagonists)
RN  - 0 (Polycyclic Compounds)
RN  - 0 (Receptors, N-Methyl-D-Aspartate)
RN  - W8O17SJF3T (Memantine)
SB  - IM
MH  - Amines/chemical synthesis/pharmacology
MH  - Animals
MH  - Cerebellum/cytology
MH  - Excitatory Amino Acid Antagonists/*chemical synthesis/pharmacology
MH  - Inhibitory Concentration 50
MH  - Memantine/pharmacology
MH  - Neurons/*drug effects
MH  - Patch-Clamp Techniques
MH  - Polycyclic Compounds/*chemical synthesis/pharmacology
MH  - Rats
MH  - Receptors, N-Methyl-D-Aspartate/*antagonists & inhibitors
MH  - Structure-Activity Relationship
PMC - PMC6249113
MID - NIHMS969636
OTO - NOTNLM
OT  - Alzheimer's disease
OT  - NMDA receptor
OT  - electrophysiology
OT  - glutamate
OT  - memantine
OT  - polycyclic amines
COIS- Notes The authors declare no competing financial interest.
EDAT- 2018/05/17 06:00
MHDA- 2019/12/24 06:00
PMCR- 2019/11/21
CRDT- 2018/05/17 06:00
PHST- 2018/05/17 06:00 [pubmed]
PHST- 2019/12/24 06:00 [medline]
PHST- 2018/05/17 06:00 [entrez]
PHST- 2019/11/21 00:00 [pmc-release]
AID - 10.1021/acschemneuro.8b00154 [doi]
PST - ppublish
SO  - ACS Chem Neurosci. 2018 Nov 21;9(11):2722-2730. doi: 
      10.1021/acschemneuro.8b00154. Epub 2018 Jun 1.