Last update 01 Nov 2024

CACNG8

Last update 01 Nov 2024

Basic Info

Synonyms

CACNG6, CACNG8, calcium voltage-gated channel auxiliary subunit gamma 8

+ [4]

Introduction

Regulates the activity of L-type calcium channels that contain CACNA1C as pore-forming subunit (By similarity). Regulates the trafficking and gating properties of AMPA-selective glutamate receptors (AMPARs). Promotes their targeting to the cell membrane and synapses and modulates their gating properties by slowing their rates of activation, deactivation and desensitization and by mediating their resensitization. Does not show subunit-specific AMPA receptor regulation and regulates all AMPAR subunits.

Drugs associated with CACNG8

CERC-611

Target

CACNG8

Mechanism

CACNG8 inhibitors

Active Org.

ES Therapeutics Australia Pty Ltd

Originator Org.

Eli Lilly & Co. [+1]

Active Indication

Essential Tremor [+1]

Inactive Indication

Pain [+1]

Drug Highest PhasePhase 2

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

11C-TARP-2105

Target

CACNG8

Mechanism

CACNG8 inhibitors

Active Org.

Southern University of Science & Technology [+2]

Originator Org.

The General Hospital Corp.

Active Indication

Central Nervous System Diseases

Inactive Indication-

Drug Highest PhasePreclinical

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

JNJ-64140284

Target

CACNG8

Mechanism

CACNG8 inhibitors

Active Org.-

Originator Org.

Johnson & Johnson

Active Indication-

Inactive Indication-

Drug Highest PhaseDiscontinued

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

Clinical Trials associated with CACNG8

NCT05234762 / RecruitingPhase 2

A Phase 2A, Randomized, Double-Blind, Placebo-Controlled Study to Evaluate the Efficacy, Safety, and Pharmacokinetics of ES-481 in Adult Patients With Essential Tremors

This Pilot Phase 2A study will investigate the safety, tolerability, and pharmacokinetics (PK) of ES-481 in adult patients with essential tremor.

Start Date21 Nov 2021

Sponsor / Collaborator

ES Therapeutics Australia Pty Ltd

NCT04737174 / WithdrawnPhase 2

Adjunctive ES-481 for Uncontrolled Glioma-Associated Epilepsy and Assessment for Potential Anti-Tumorigenic Effect in Patients With Isocitrate Dehydrogenase 1 (IDH1) Mutant Tumors

Phase 2A single-arm exploratory clinical study in up to 12 adult subjects aged 18 and older with primary glioma, IDH1 mutation, and uncontrolled focal-onset seizure activity to determine the potential efficacy, safety and pharmacokinetics of ES-481 as adjunctive therapy in glioma-associated epilepsy and to assess for potential anti-tumorigenic effects.

Start Date25 Mar 2021

Sponsor / Collaborator

ES Therapeutics Australia Pty Ltd

ACTRN12621000033842 / RecruitingPhase 2

A Phase 2A, Randomized, Double-Blind, Placebo-Controlled Study to Evaluate the Efficacy, Safety and Pharmacokinetics of ES-481 in Adult Patients with Drug Resistant Epilepsy.

Start Date29 Jan 2021

Sponsor / Collaborator

ES Therapeutics Australia Pty Ltd

100 Clinical Results associated with CACNG8

100 Translational Medicine associated with CACNG8

0 Patents (Medical) associated with CACNG8

Literatures (Medical) associated with CACNG8

19 Sep 2024·Cells

Cannabinol (CBN) Influences the Ion Channels and Synaptic-Related Genes in NSC-34 Cell Line: A Transcriptomic Study.

Article

Author: Trainito, Alessandra ; Gugliandolo, Agnese ; D'Angiolini, Simone ; Salamone, Stefano ; Muscarà, Claudia ; Chiricosta, Luigi ; Mazzon, Emanuela ; Pollastro, Federica

Neurological disorders such as Alzheimer's, Parkinson's, amyotrophic lateral sclerosis, and schizophrenia are associated with altered neuronal excitability, resulting from dysfunctions in the molecular architecture and physiological regulation of ion channels and synaptic transmission. Ion channels and synapses are regarded as suitable therapeutic targets in modern pharmacology. Cannabinoids have received great attention as an original therapeutic approach for their effects on human health due to their ability to modulate the neurotransmitter release through interaction with the endocannabinoid system. In our study, we explored the effect of cannabinol (CBN) through next-generation sequencing analysis of NSC-34 cell physiology. Our findings revealed that CBN strongly influences the ontologies related to ion channels and synapse activity at all doses tested. Specifically, the genes coding for calcium and potassium voltage-gated channel subunits, and the glutamatergic and GABAergic receptors (Cacna1b, Cacna1h, Cacng8, Kcnc3, Kcnd1, Kcnd2, Kcnj4, Grik5, Grik1, Slc17a7, Gabra5), were up-regulated. Conversely, the genes involved into serotoninergic and cholinergic pathways (Htr3a, Htr3b, Htr1b, Chrna3, Chrnb2, Chrnb4), were down-regulated. These findings highlight the influence of CBN in the expression of genes involved into ion influx and synaptic transmission.

01 Jun 2024·Pharmacological Research

Baicalin restore intestinal damage after early-life antibiotic therapy: the role of the MAPK signaling pathway

Article

Author: Zhang, Shunfen ; Zhang, Hongfu ; Chen, Liang ; Lv, Huiyuan ; Zhong, Ruqing ; Tang, Shanlong ; Liu, Zhengqun ; Cai, Xueying

Antibiotic related intestinal injury in early life affects subsequent health and susceptibility. Here, we employed weaned piglets as a model to investigate the protective effects of baicalin against early-life antibiotic exposure-induced microbial dysbiosis. Piglets exposed to lincomycin showed a marked reduction in body weight (p < 0.05) and deterioration of jejunum intestinal morphology, alongside an increase in antibiotic-resistant bacteria such as Staphylococcus, Dolosicoccus, Escherichia-Shigella, and Raoultella. In contrast, baicalin treatment resulted in body weights, intestinal morphology, and microbial profiles that closely resembled those of the control group (p > 0.05), with a significant increase in norank_f_Muribaculaceae and Prevotellaceae_NK3B31_group colonization compared with lincomycin group (p < 0.05). Further analysis through fecal microbial transplantation into mice revealed that lincomycin exposure led to significant alterations in intestinal morphology and microbial composition, notably increasing harmful microbes and decreasing beneficial ones such as norank_Muribaculaceae and Akkermansia (p < 0.05). This shift was associated with an increase in harmful metabolites and disruption of the calcium signaling pathway gene expression. Conversely, baicalin supplementation not only counteracted these effects but also enhanced beneficial metabolites and regulated genes within the MAPK signaling pathway (MAP3K11, MAP4K2, MAPK7, MAPK13) and calcium channel proteins (ORA13, CACNA1S, CACNA1F and CACNG8), suggesting a mechanism through which baicalin mitigates antibiotic-induced intestinal and microbial disturbances. These findings highlight baicalin's potential as a plant extract-based intervention for preventing antibiotic-related intestinal injury and offer new targets for therapeutic strategies.

15 Mar 2024·ChemBioChem

Preclinical Evaluation of Azabenzimidazole‐Based PET Radioligands for γ‐8 Dependent Transmembrane AMPA Receptor Regulatory Protein Imaging

Article

Author: Yu, Qingzhen ; Yuan, Hongjie ; Liang, Steven ; Zhou, Xin ; Bi, Chunyang ; Rong, Jian ; Song, Zhendong ; Chaudhary, Ahmad F ; Zhao, Chunyu ; Chen, Jiahui ; Zhang, Kuo ; Collier, Lee ; Li, Yinlong ; Haider, Ahmed ; Patel, Jimmy S ; Davenport, April T ; Daunais, James B ; Zhang, Wei

AbstractAMPA glutamate receptors (AMPARs) play a pivotal role in excitatory neurotransmission, particularly in the hippocampus where the TARP γ‐8 subunit is enriched and serves as a target for emerging anti‐epileptic drugs. To enable in vivo visualization of TARP γ‐8 distribution and expression by positron emission tomography (PET), this study focuses on the development of novel 18F‐labeled TARP γ‐8 inhibitors and their corresponding precursors, stemming from the azabenzimidazole scaffold. The resulting radioligands [18F]TARP‐2204 and [18F]TARP‐2205 were successfully synthesized with acceptable radiochemical yield, high molar activity, and excellent radiochemical purity. In vitro autoradiography demonstrates high level of specific binding of [18F]TARP‐2205 to TARP γ‐8 in both rat and nonhuman primate brain tissues. However, unexpected radiodefluorination in PET imaging studies of rodents emphasizes the need for further structural refinement. This work serves as an excellent starting point for the development of future 18F‐labeled TARP γ‐8 PET tracers, offering valuable insights into medicinal chemistry design, radiosynthesis and subsequent PET evaluation.

Analysis

Perform a panoramic analysis of this field.

view full example data

Chat with Hiro

Get started for free today!

Accelerate Strategic R&D decision making with Synapse, PatSnap’s AI-powered Connected Innovation Intelligence Platform Built for Life Sciences Professionals.

Start your data trial now!

Synapse data is also accessible to external entities via APIs or data packages. Empower better decisions with the latest in pharmaceutical intelligence.

Bio

Bio Sequences Search & Analysis

Chemical

Chemical Structures Search & Analysis