D. Bleakman

发表

A Critical Role of a Facilitatory Presynaptic Kainate Receptor in Mossy Fiber LTP

David Lodge, David Bleakman, G. Collingridge, 2001, Neuron.

LY354740 is a Potent and Highly Selective Group II Metabotropic Glutamate Receptor Agonist in Cells Expressing Human Glutamate Receptors

D. Schoepp, D. Bleakman, J. Monn, 1997, Neuropharmacology.

Pharmacological Characterization of the Competitive GLUK5 Receptor Antagonist Decahydroisoquinoline LY466195 in Vitro and in Vivo

David Bleakman, Kirk W. Johnson, Andrew Alt, 2006, Journal of Pharmacology and Experimental Therapeutics.

GluK1 antagonists from 6-(tetrazolyl)phenyl decahydroisoquinoline derivatives: in vitro profile and in vivo analgesic efficacy.

D. Clawson, P. Ornstein, S. Iyengar, 2013, Bioorganic & medicinal chemistry letters.

The effect of capsaicin on voltage‐gated calcium currents and calcium signals in cultured dorsal root ganglion cells

R. Miller, D. Bleakman, J. Brorson, 1990, British journal of pharmacology.

A procedural framework for good imaging practice in pharmacological fMRI studies applied to drug development #1: processes and requirements.

David Borsook, Richard Baumgartner, Alexandre Coimbra, 2011, Drug discovery today.

Decahydroisoquinolines: novel competitive AMPA/kainate antagonists with neuroprotective effects in global cerebral ischaemia

P. Ornstein, M. O'Neill, D. Bleakman, 1998, Neuropharmacology.

The effects of ifenprodil and eliprodil on voltage-dependent Ca2+ channels and in gerbil global cerebral ischaemia.

J. Gilmore, M. O'Neill, D. Bleakman, 1996, European journal of pharmacology.

Prevention of guanine nucleotide-induced reductions in muscarinic agonist binding to rabbit ileal submucosal membranes by lidamidine and tetracaine

D. Bleakman, R. Naftalin, 1988, Naunyn-Schmiedeberg's Archives of Pharmacology.

Comparison of BOLD Response Modulation During Pain Stimulation and Resting-State Conditions Under Intravenous ( 0 . 2 mg / 70 kg ) or Sublingual ( 2 mg ) Buprenorphine Treatment

A. Schwarz, L. Becerra, D. Borsook, 2009 .

Inhibitory Actions of Synthesised Polyamine Spider Toxins and Their Analogues on Neuronal Voltage-Activated Calcium Currents

J. Gilmore, D. Bleakman, G. Timms, 1997 .

Characteristics of a human N-type calcium channel expressed in HEK293 cells

R. Miller, D. Bleakman, M. Harpold, 1995, Neuropharmacology.

A role for AMPA receptors in mood disorders.

E. Nisenbaum, J. Witkin, D. Bleakman, 2006, Biochemical pharmacology.

AMPA receptor potentiators for the treatment of CNS disorders.

E. Nisenbaum, M. O'Neill, D. Bleakman, 2004, Current drug targets. CNS and neurological disorders.

LY503430, a Novel α-Amino-3-hydroxy-5-methylisoxazole-4-propionic Acid Receptor Potentiator with Functional, Neuroprotective and Neurotrophic Effects in Rodent Models of Parkinson's Disease

E. Nisenbaum, K. Whalley, P. Skolnick, 2003, Journal of Pharmacology and Experimental Therapeutics.

[3H]N-2-(4-(N-benzamido)phenyl)propyl-2-propanesulfonamide: a novel AMPA receptor potentiator and radioligand.

P. Skolnick, P. Ornstein, D. Bleakman, 2001, Journal of medicinal chemistry.

The GluR5 subtype of kainate receptor regulates excitatory synaptic transmission in areas CA1 and CA3 of the rat hippocampus

G. Collingridge, P. Ornstein, D. Bleakman, 1998, Neuropharmacology.

A hippocampal GluR5 kainate receptor regulating inhibitory synaptic transmission

G. Collingridge, C. Davies, B. Ballyk, 1997, Nature.

Neuropharmacology of AMPA and kainate receptors

D. Bleakman, D. Lodge, 1998, Neuropharmacology.

ACET is a highly potent and specific kainate receptor antagonist: Characterisation and effects on hippocampal mossy fibre function

G. Collingridge, M. Mayer, D. Jane, 2009, Neuropharmacology.

Irreversible Inhibition of High‐Affinity [3H]Kainate Binding by a Novel Photoactivatable Analogue: (2′S,3′S,4′R)‐2′‐Carboxy‐4′‐(2‐Diazo‐1‐Oxo‐3,3,3‐Trifluoropropyl)‐3′‐Pyrrolidinyl Acetate

R. Bridges, D. Bleakman, D. Lodge, 1997, Journal of neurochemistry.

Design and synthesis of a novel series of 1,2-disubstituted cyclopentanes as small, potent potentiators of 2-amino-3-(3-hydroxy-5-methyl-isoxazol-4-yl)propanoic acid (AMPA) receptors.

G. Stephenson, D. Bleakman, B. Cantrell, 2002, Journal of medicinal chemistry.

Synthesis of willardiine and 6-azawillardiine analogs: pharmacological characterization on cloned homomeric human AMPA and kainate receptor subtypes.

D. Jane, D. Bleakman, R. Kamboj, 1997, Journal of medicinal chemistry.

Pharmacological characterization of glutamatergic agonists and antagonists at recombinant human homomeric and heteromeric kainate receptors in vitro

D. Bleakman, T. Large, A. Alt, 2004, Neuropharmacology.

Non-NMDA Glutamate Receptors in the Regulation of Neuronal Ca2+ and Excitotoxicity

D. Bleakman, Richard J. Miller, J. Brorson, 1994 .

Calcium Influx and Neurodegeneration a

D. Bleakman, S. Gibbons, J. Brorson, 1993, Annals of the New York Academy of Sciences.

A Role for Ca2+ Stores in Kainate Receptor-Dependent Synaptic Facilitation and LTP at Mossy Fiber Synapses in the Hippocampus

G. Collingridge, J. Isaac, Z. Bortolotto, 2003, Neuron.

The effects of four general anesthetics on intracellular [Ca2+] in cultured rat hippocampal neurons

N. Harrison, D. Bleakman, M. V. Jones, 1995, Neuropharmacology.

Glutamate receptors and pain.

E. Nisenbaum, D. Bleakman, A. Alt, 2006, Seminars in cell & developmental biology.

The properties of intracellular calcium stores in cultured rat cerebellar neurons

D. Bleakman, S. Gibbons, R. Miller, 1991, The Journal of neuroscience : the official journal of the Society for Neuroscience.

Human autoantibodies specific for the alpha1A calcium channel subunit reduce both P-type and Q-type calcium currents in cerebellar neurons.

K. Stauderman, D. Bleakman, D. Lodge, 1998, Proceedings of the National Academy of Sciences of the United States of America.

Actions of Neuropeptide Y on the Electrophysiological Properties of Nerve Cells

W. Colmers, D. Bleakman, Richard J. Miller, 1993 .

Kainate receptor pharmacology and physiology

D. Bleakman, Eli Lilly, 1999, Cellular and Molecular Life Sciences CMLS.

Tachykinins Potentiate N‐Methyl‐D‐Aspartate Responses in Acutely Isolated Neurons from the Dorsal Horn

R. Miller, M. Randić, D. Bleakman, 1993, Journal of neurochemistry.

Imaging Drugs with and without Clinical Analgesic Efficacy

David Borsook, Richard Baumgartner, Alexandre Coimbra, 2011, Neuropsychopharmacology.

Decision-making using fMRI in clinical drug development: revisiting NK-1 receptor antagonists for pain.

David Borsook, Richard Baumgartner, Alexandre Coimbra, 2012, Drug discovery today.

Hypertonic fluid absorption from rabbit descending colon in vitro.

D. Bleakman, R. Naftalin, 1990, The American journal of physiology.

Effects of neuropeptide Y on the electrical properties of neurons

W. Colmers, D. Bleakman, 1994, Trends in Neurosciences.

Synthesis and pharmacology of willardiine derivatives acting as antagonists of kainate receptors.

G. Collingridge, D. Jane, Z. Bortolotto, 2005, Journal of medicinal chemistry.

Structure-activity relationship studies on N3-substituted willardiine derivatives acting as AMPA or kainate receptor antagonists.

G. Collingridge, D. Jane, D. Bleakman, 2006, Journal of medicinal chemistry.

4-Alkyl- and 4-cinnamylglutamic acid analogues are potent GluR5 kainate receptor agonists.

B. Ballyk, C. Dominguez, D. Bleakman, 2000, Journal of medicinal chemistry.

Mechanism of presynaptic inhibition by neuropeptide Y at sympathetic nerve terminals

V. Bindokas, W. Colmers, D. Bleakman, 1993, Nature.

LY 503430 , a novel AMPA receptor potentiator with functional , neuroprotective and neurotrophic effects in rodent models of Parkinson ’ s disease

E. Nisenbaum, K. Whalley, P. Skolnick, 2003 .

LY 503430 , a Novel-Amino-3-hydroxy-5-methylisoxazole-4-propionic Acid Receptor Potentiator with Functional , Neuroprotective and Neurotrophic Effects in Rodent Models of Parkinson ’ s Disease

E. Nisenbaum, K. Whalley, P. Skolnick, 2003 .

Characterisation of UBP296: a novel, potent and selective kainate receptor antagonist

G. Collingridge, D. Jane, Z. Bortolotto, 2004, Neuropharmacology.

Kainate receptors are involved in synaptic plasticity

G. Collingridge, Z. Bortolotto, P. Ornstein, 1999, Nature.

Parallel Buprenorphine phMRI Responses in Conscious Rodents and Healthy Human Subjects

David Borsook, Richard Baumgartner, Alexandre Coimbra, 2013, The Journal of Pharmacology and Experimental Therapeutics.

In vitro and in vivo studies in rats with LY293558 suggest AMPA/kainate receptor blockade as a novel potential mechanism for the therapeutic treatment of anxiety disorders

Xia Li, J. Witkin, D. Bleakman, 2006, Psychopharmacology.

Test–retest reliability of evoked heat stimulation BOLD fMRI

David Borsook, Jeffrey L. Evelhoch, Lino Becerra, 2015, Journal of Neuroscience Methods.

Effects of Ca2+ and Na+ channel inhibitors in vitro and in global cerebral ischaemia in vivo.

M. O'Neill, D. Bleakman, C. Hicks, 1997, European journal of pharmacology.

AMPA receptors in the therapeutic management of depression.

J. Witkin, D. Bleakman, A. Alt, 2007, CNS & neurological disorders drug targets.

Identification of Kainate Receptor‐Mediated Intracellular Calcium Increases in Cultured Rat Cerebellar Granule Cells

D. Bleakman, J. Savidge, D. Bristow, 1997, Journal of neurochemistry.

Novel AMPA receptor potentiators LY392098 and LY404187: effects on recombinant human AMPA receptors in vitro

P. Ornstein, D. Bleakman, D. Zimmerman, 2001, Neuropharmacology.

An AMPA receptor potentiator modulates hippocampal expression of BDNF: an in vivo study

David Bleakman, P. Skolnick, M. O'Neill, 2002, Neuropharmacology.

Pharmacological effects of AMPA receptor potentiators LY392098 and LY404187 on rat neuronal AMPA receptors in vitro

D. Bleakman, D Bleakman, M Gates, 2001, Neuropharmacology.

LY293558, a Novel AMPA/GluR5 Antagonist, is Efficacious and Well-Tolerated in Acute Migraine

Kirk W. Johnson, F Vandenhende, S. Silberstein, 2004, Cephalalgia : an international journal of headache.

Antagonists of GLUK5-containing kainate receptors prevent pilocarpine-induced limbic seizures

G. Collingridge, Z. Bortolotto, Y. Michotte, 2002, Nature Neuroscience.

In vitro and in vivo antagonism of AMPA receptor activation by (3s,4ar,6r,8ar)-6-[2-(1(2)h-tetrazole-5-yl)ethyl]decahydroisoquinoline-3-carboxylic acid

P. Ornstein, D. Schoepp, D. Bleakman, 1995, Neuropharmacology.

Electrophysiological characterisation of the human N-type Ca2+ channel III: pH-dependent inhibition by a synthetic macrocyclic polyamine

A. Randall, D. Bleakman, B. Clark, 1999, Neuropharmacology.

The role of intracellular calcium in the cellular response to ionizing radiation.

D. Hallahan, R. Weichselbaum, D. Kufe, 1994, Radiation research.

Calcium buffering properties of calbindin D28k and parvalbumin in rat sensory neurones.

R. Miller, D. Bleakman, S. Christakos, 1993, The Journal of physiology.

GluK1 antagonists from 6-(carboxy)phenyl decahydroisoquinoline derivatives. SAR and evaluation of a prodrug strategy for oral efficacy in pain models.

P. Ornstein, S. Iyengar, M. del Prado, 2013, Bioorganic & medicinal chemistry letters.

Antiallodynic and Antihyperalgesic Effects of Selective Competitive GLUK5 (GluR5) Ionotropic Glutamate Receptor Antagonists in the Capsaicin and Carrageenan Models in Rats

P. Ornstein, S. Iyengar, D. Bleakman, 2006, Journal of Pharmacology and Experimental Therapeutics.

Activity of 2,3-benzodiazepines at Native Rat and Recombinant Human Glutamate Receptors In Vitro: Stereospecificity and Selectivity Profiles

B. Ballyk, D. Schoepp, D. Bleakman, 1996, Neuropharmacology.

Two prodrugs of potent and selective GluR5 kainate receptor antagonists actives in three animal models of pain.

P. Ornstein, S. Iyengar, M. del Prado, 2005, Journal of medicinal chemistry.

Ethyl (3S,4aR,6S,8aR)-6-(4-ethoxycar- bonylimidazol-1-ylmethyl)decahydroiso-quinoline-3-carboxylic ester: a prodrug of a GluR5 kainate receptor antagonist active in two animal models of acute migraine.

Kirk W. Johnson, P. Ornstein, M. del Prado, 2002, Journal of medicinal chemistry.

[3H]ATPA: a high affinity ligand for GluR5 kainate receptors

P. Skolnick, P. Krogsgaard‐Larsen, D. Bleakman, 1999, Neuropharmacology.

LY339434, a GluR5 kainate receptor agonist

B. Ballyk, B. Small, D. Bleakman, 1998, Neuropharmacology.

Pharmacological characterization of a GluR6 kainate receptor in cultured hippocampal neurons.

P. Ornstein, D. Bleakman, A. Ogden, 1999, European journal of pharmacology.

Measurement of calcium flux through ionotropic glutamate receptors using Cytostar-T scintillating microplates

D. Bleakman, D. Lodge, R. Graves, 1999, Journal of Neuroscience Methods.

The synaptic activation of the GluR5 subtype of kainate receptor in area CA3 of the rat hippocampus

G. Collingridge, G. Collingridge, D. Bleakman, 1997, Neuropharmacology.

Investigations into neuropeptide Y‐mediated presynaptic inhibition in cultured hippocampal neurones of the rat

N. Harrison, W. Colmers, D. Bleakman, 1992, British journal of pharmacology.

Bradykinin-induced modulation of calcium signals in rat dorsal root ganglion neurons in vitro.

R. Miller, S. Glaum, D. Bleakman, 1990, Molecular pharmacology.

A ‘BOLD’ experiment in defining the utility of fMRI in drug development

David Borsook, Richard Hargreaves, Lino Becerra, 2008, NeuroImage.

Calcium homeostasis in rat septal neurons in tissue culture

N. Harrison, B. Wainer, D. Bleakman, 1993, Brain Research.

Electrophysiological characterisation of the human N-type Ca2+ channel II Activation and inactivation by physiological patterns of activity

A. Randall, D. Bleakman, N. McNaughton, 1998, Neuropharmacology.

Neuropeptide Y and pancreatic polypeptide reduce calcium currents in acutely dissociated neurons from adult rat superior cervical ganglia.

V. Bindokas, R. Miller, D. Bleakman, 1993, The Journal of pharmacology and experimental therapeutics.

A procedural framework for good imaging practice in pharmacological fMRI studies applied to drug development #2: protocol optimization and best practices.

David Borsook, Lino Becerra, Richard Baumgartner, 2011, Drug discovery today.

Capsaicin-induced neurotoxicity in cultured dorsal root ganglion neurons: Involvement of calcium-activated proteases

R. Miller, D. Bleakman, J. Savidge, 1995, Neuroscience.

TRP channels as emerging targets for pain therapeutics

M. Blanco, D. Bleakman, L. Broad, 2009, Expert opinion on therapeutic targets.

Howthebrain learnstosee objectsand faces inan impoverishedcontext

G. Collingridge, C. Davies, B. Ballyk, 1997 .

Neuropeptide Y inhibits Ca2+ influx into cultured dorsal root ganglion neurones of the rat via a Y2 receptor

W. Colmers, D. Bleakman, A. Fournier, 1991, British journal of pharmacology.

Calcium directly permeates kainate/alpha-amino-3-hydroxy-5-methyl-4- isoxazolepropionic acid receptors in cultured cerebellar Purkinje neurons.

R. Miller, D. Bleakman, J. Brorson, 1992, Molecular pharmacology.

Chemogenetics: drug-controlled gene therapies for neural circuit disorders

S. Sternson, D. Bleakman, 2020, Cell & gene therapy insights.

Innovative drug development for headache disorders: glutamate

Kirk W. Johnson, N. Ramadan, E. Nisenbaum, 2008 .

4-Alkylidenyl glutamic acids, potent and selective GluR5 agonists.

B. Ballyk, C. Dominguez, D. Bleakman, 2000, Bioorganic & medicinal chemistry letters.

Pharmacological Modulation of GluK1 and GluK2 by NETO1, NETO2, and PSD95.

Kirk W. Johnson, Y. Qian, D. Bleakman, 2016, Assay and drug development technologies.

Modulation of CNS pain circuitry by intravenous and sublingual doses of buprenorphine

David Borsook, Richard Hargreaves, Richard Baumgartner, 2012, NeuroImage.

Synthesis and pharmacological characterization of N3-substituted willardiine derivatives: role of the substituent at the 5-position of the uracil ring in the development of highly potent and selective GLUK5 kainate receptor antagonists.

G. Collingridge, M. Mayer, D. Jane, 2007, Journal of medicinal chemistry.

Kainate receptor agonists, antagonists and allosteric modulators.

D. Bleakman, A. Ogden, M. Gates, 2002, Current pharmaceutical design.

AMPA receptor potentiators as novel antidepressants.

J. Witkin, D. Bleakman, A. Alt, 2005, Current pharmaceutical design.

Improved characterization of BOLD responses for evoked sensory stimuli

David Borsook, Igor D. Grachev, Richard Hargreaves, 2010, NeuroImage.

Anxiolytic-like effects through a GLUK5 kainate receptor mechanism

P. Ornstein, J. Witkin, D. Bleakman, 2007, Neuropharmacology.

ω-conotoxin MVIIC reversibly inhibits a human N-type calcium channel and calcium influx into chick synaptosomes

D. Bell, D. Bleakman, D. Bowman, 1994, Neuropharmacology.

Metabotropic glutamate receptors potentiate ionotropic glutamate responses in the rat dorsal horn.

R. Miller, S. Glaum, D. Bleakman, 1992, Molecular pharmacology.

Biarylpropylsulfonamides as novel, potent potentiators of 2-amino-3- (5-methyl-3-hydroxyisoxazol-4-yl)- propanoic acid (AMPA) receptors.

P. Ornstein, D. Bleakman, B. Cantrell, 2000, Journal of medicinal chemistry.

Identification of Pore-forming Subunit of P-type Calcium Channels: an Antisense Study on Rat Cerebellar Purkinje Cells in Culture

D. Bleakman, D. Lodge, W. Smith, 1997, Neuropharmacology.

The atypical ‘hippocampal’ glutamate receptor coupled to phospholipase D that controls stretch‐sensitivity in primary mechanosensory nerve endings is homomeric purely metabotropic GluK2

R. W. Banks, D. Bleakman, F. Shenton, 2023, Experimental physiology.