Ligand-Gated Channels
Cambridge Bioscience, through our collaboration with ChanTest, offers access to screening services to the following ligand-gated channel targets:
5-HT3A
Target Class: Ion Channel
Gene Name: HTR3A
Validated Assay/Platform: FLIPR®, IonWorks Quattro™, Manual Patch Clamp & PatchXpress®
Description: The human HTR3A gene encodes the pore-forming subunit of 5-HT3A, a ligand-gated cation channel activated by 5-hydroxytryptamine (serotonin). 5-HT3A channels expressed in the CNS and GI tract, are therapeutic targets in nausea and irritable bowel syndrome.
GABAA (α1/β2/γ2)
Target Class: Ion Channel
Gene Name: GABRA1/GABRB2/GABRG2
Validated Assay/Platform: FLIPR®/ Manual Patch Clamp
Description: The human GABRA1, GABRB2, and GABRG2 genes encode the Cl--selective, ionotropic GABAA receptor-channel. Mutations in GABRA1 have been linked to familial juvenile myoclonic epilepsy. GABAA receptors expressed in CNS neurons are therapeutic targets in treatment seizure and anxiety.
GABAA (a2β2γ2)
Target Class: Ion Channel
Gene Name: GABRA2/GABRB2/GABRG2
Validated Assay/Platform: FLIPR®/ Manual Patch Clamp
Description: The human GABRA2 GABR2 and GABRG2 genes encode the Cl--selective, ionotropic GABAA receptor-channel. GABAA receptors expressed in neurons are therapeutic targets in treatment of neurological and psychological disorders (e.g., seizure and anxiety).
GABAA (a5β2γ2)
Target Class: Ion Channel
Gene Name: GABRA5/GABRB2/GABRG2
Validated Assay/Platform: FLIPR® & Manual Patch Clamp
Description: The human GABRA5 GABR2 and GABRG2 genes encode the Cl--selective, ionotropic GABAA receptor-channel. GABAA receptors expressed in neurons are therapeutic targets in treatment of neurological and psychological disorders (e.g., cognitive impairment and schizophrenia).
Nicotinic Receptor (nAChR) a3/β4
Target Class: Ion Channel
Gene Name: CHRNA3/CHRNB4
Validated Assay/Platform: FLIPR®
Description: Nicotinic receptors (nAChR) are acetylcholine-activated non-selective cation channels that mediate excitatory neurotransmission. The receptor-channels are configured as hetero- or homopentamers. The human CHRNA3 and CHRNB4 genes encode a cationic-selective, ionotropic α3/β4 nicotinic acetylcholine receptor (nAChR). Channels that contain a3 subunits typically have lower Ca2+ permeability compared to those containing a7 subunits. Therefore, α7 nAChRs are particularly important in regulation of Ca2+-dependent signalling pathways. Tissue distribution also differs with α3/β4 receptors prominent in autonomic ganglia and α7 receptors widely distributed in the CNS.
Nicotinic Receptor (nAChR) α7
Target Class: Ion Channel
Gene Name: CHRNA7
Validated Assay/Platform: FLIPR® & QPatch HT
Description: The human CHRNA7 gene encodes the acetylcholine-activated, cationic-selective, nAChRα7 channel, expressed in CNS neurons and non-neuronal cells (placenta, endothelia, vascular smooth muscle). The nAChRα7 channel is a therapeutic target in treatment of inflammation, schizophrenia, and cognitive impairment.
NMDA (NR1/NR2A)
Target Class: Ion Channel
Synonym: GluN1/GluN2A
Gene Name: GRIN1/GRIN2A
Validated Assay/Platform: FLIPR®
Description: The human GRIN1/GRIN2A genes encode the cationic-selective, n-methyl-d-aspartic acid receptor-channel expressed in the CNS. NMDA receptors are therapeutic targets in treatment of neurological disorders including seizure, pain, and Alzheimer's disease.
NMDA (NR1/NR2B)
Target Class: Ion Channel
Synonym: GluN1/GluN2B
Gene Name: GRIN1/GRIN2B
Validated Assay/Platform: FLIPR®
Description: The human GRIN1/GRIN2B genes encode the cationic-selective, n-methyl-d-aspartic acid receptor-channel expressed in the CNS. NMDA receptors are therapeutic targets in treatment of neurological disorders including seizure, pain, and Alzheimer's disease.
Platforms Available
Cambridge Bioscience, through our collaboration with ChanTest, offers access to the widest range of screening platforms, from manual patch clamp up to the most recent innovations in automated electrophysiology, allowing you to select the right balance of speed, throughput and data quality to suit your needs.
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