ion channel selectivity profiling: psychiatric …...ion channel selectivity profiling: psychiatric...

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www.criver.com EVERY STEP OF THE WAY Ion Channel Selectivity Profiling: Psychiatric Disorder Our Psychiatric Disorder Channel Panel ® includes neurotransmitter receptor channels that are important in anxiety and schizophrenia. Selectivity Profiling Identification of a compound’s target specificity and potential for off-target effects is a critical step in the drug discovery process and often includes assessments against specific target class families, critical safety targets or by therapeutic area. In addition to our therapeutic area-specific Channel Panels ® , we offer screening on a number of electrophysiology platforms. When required, our scientists can design customized panels to meet a client’s needs. As pioneers in the field of ion channels, we are able to provide expert consultation to facilitate interpretation of results. Ion Channels and Psychiatric Disorders Antipsychotic and antianxiety drugs that include ion channel targets are generally thought to modulate synaptic transmission in specific brain regions (e.g., the limbic system in schizophrenia, and both the limbic and brainstem reticular activating systems in anxiety). Our Psychiatric Disorder Channel Panel ® includes neurotransmitter receptor channels that are important in anxiety (GABA) and schizophrenia (NMDA and nAChRα 7 ). Voltage-gated potassium channels (KCNQ) that regulate excitability and are potential therapeutic targets for anxiety and schizophrenia also are included. Ion Channel Families: Calcium, voltage-gated (Cav1.3/β 3 /α 2 δ) Ligand-gated (GABA (α 1 β 3 γ 2 , α 2 β 3 γ 2 , α 3 β 3 γ 2 , α 4 β 3 γ 2 and α 5 β 3 γ 2 ), nACHR (α 4 /β 2 , α 7 , α 3 β 4 α 5 , α 6/3 β 2 β 3 ) and NMDA (NR1/NR2A, NR1/NR2B, NR1/NR2C and NR1/NR2D)) Potassium, voltage-gated (KCNQ2/3 and KCNQ3/5) Potassium, calcium-activated (SK1, SK2 and SK3) DISCOVERY © 2020, Charles River Laboratories International, Inc. Need a custom version of this assay? Visit criver.com/pi-ds-ion- channel-profiling-assay Click to learn more Summary The Charles River ion channel portfolio includes over 120 targets which have been organized into Channel Panels ® based on current scientific findings, proving a useful tool in guiding early screening and selectivity profiling.

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Page 1: Ion Channel Selectivity Profiling: Psychiatric …...Ion Channel Selectivity Profiling: Psychiatric Disorder Datasheet Keywords Neurotransmitter receptors, anxiety, schizophrenia,

www.criver.com

EVERY STEP OF THE WAY

Ion Channel Selectivity Profiling:

Psychiatric Disorder Our Psychiatric Disorder Channel Panel® includes neurotransmitter receptor channels that are important in anxiety and

schizophrenia.

Selectivity ProfilingIdentification of a compound’s target specificity and potential for off-target effects is a critical step in the drug discovery

process and often includes assessments against specific target class families, critical safety targets or by therapeutic

area. In addition to our therapeutic area-specific Channel Panels®, we offer screening on a number of electrophysiology

platforms. When required, our scientists can design customized panels to meet a client’s needs. As pioneers in the field of

ion channels, we are able to provide expert consultation to facilitate interpretation of results.

Ion Channels and Psychiatric DisordersAntipsychotic and antianxiety drugs that include ion channel targets are generally thought to modulate synaptic transmission

in specific brain regions (e.g., the limbic system in schizophrenia, and both the limbic and brainstem reticular activating

systems in anxiety). Our Psychiatric Disorder Channel Panel® includes neurotransmitter receptor channels that are important

in anxiety (GABA) and schizophrenia (NMDA and nAChRα7). Voltage-gated potassium channels (KCNQ) that regulate

excitability and are potential therapeutic targets for anxiety and schizophrenia also are included.

Ion Channel Families:

• Calcium, voltage-gated (Cav1.3/β3/α2δ)

• Ligand-gated (GABA (α1β3γ2, α2β3γ2, α3β3γ2, α4β3γ2 and α5β3γ2), nACHR (α4/β2, α7, α3β4α5, α6/3β2β3) and NMDA (NR1/NR2A, NR1/NR2B, NR1/NR2C and NR1/NR2D))

• Potassium, voltage-gated (KCNQ2/3 and KCNQ3/5)

• Potassium, calcium-activated (SK1, SK2 and SK3)

DISCOVERY

© 2020, Charles River Laboratories International, Inc.

Need a custom version of this assay? Visit criver.com/pi-ds-ion-

channel-profiling-assay

Click to learn more

SummaryThe Charles River ion channel

portfolio includes over 120

targets which have been

organized into Channel Panels®

based on current scientific

findings, proving a useful tool

in guiding early screening and

selectivity profiling.