GABA Receptor Inhibitor

FG 7142 (Standard) is the analytical standard of FG 7142. This product is intended for research and analytical applications. FG 7142 (ZK 39106; LSU-65), a non-selectively benzodiazepine inverse agonist, has high affinity for the α1 subunit-containing GABAA receptor (Ki=91 nM). FG 7142 (ZK 39106; LSU-65) also modulates GABA-induced chloride flux at GABAA receptors expressing the α1 subunit (EC50= 137 nM). FG 7142 (ZK 39106; LSU-65) can increase tyrosine hydroxylation and cause upregulation of?β-adrenoceptors in mouse cerebral cortex.

Flutoprazepam (KB-509), a benzodiazepine drug, possesses anticonflict effect. Flutoprazepam (KB-509) prevents maximal electroshock, pentetrazol, and strychnine-induced convulsions in mice.

CI-966 hydrochloride (Standard) is the analytical standard of CI-966 hydrochloride (HY-103534). This product is intended for research and analytical applications. CI-966 hydrochloride is a potent, selective, orally active and brain-penetrant inhibitor of the GABA transporter GAT-1, with IC₅₀s of 0.26 μM and 1.2 μM for hGAT-1, rGAT-1, respectively. CI-966 hydrochloride shows more than 200-fold selectivity over GAT-2, GAT-3, and BGT-3. CI-966 hydrochloride exhibits anticonvulsant and neuroprotective activities.

NNC 05-2090 hydrochloride (Standard) is the analytical standard of NNC 05-2090 hydrochloride (HY-103509). This product is intended for research and analytical applications. NNC 05-2090 hydrochloride is a GABA uptake inhibitor and inhibitor of the β-GABA transporter (BGT-1) (IC₅₀< /sub>: 10.6 μM). NNC 05-2090 hydrochloride also inhibits mGAT2 with a K_i value of 1.4 μM. NNC 05-2090 has anticonvulsant activity and can be used in the study of epilepsy and neurological diseases.

Spinacine (Standard) is the analytical standard of Spinacine (HY-W067716). This product is intended for research and analytical applications. Spinacine ((S)-Spinacine) is a GABA uptake inhibitor. Spinacine enhances synaptic GABA effects via inhibition of gamma-aminobutyric acid uptake in cerebral cortex slices. Spinacine inhibits reflex responses of ventral roots in isolated spinal cord. Spinacine inhibits motor activity and reduces approaches to water dispensers in conflict situations. Spinacine raises pain sensitivity threshold via subarachnoidal injection.

APS3 is a GABA and nACh receptors inhibitor, with a LC₅₀ of 7.2423 μg/mL against Plutella xylostella.

SKF89976A (hydrochloride) (Standard) is the analytical standard of SKF89976A (hydrochloride) (HY-100228A). This product is intended for research and analytical applications. SKF89976A hydrochloride is a selective GABA transporter (GAT-1) inhibitor with IC50s of 0.28 μM, 137.34 μM and 202.8 μM for GAT-1, GAT-2 and GAT-3 in CHO cells, respectively.

L-DABA (Standard) is the analytical standard of L-DABA. This product is intended for research and analytical applications. L-DABA (L-2,4-Diaminobutyric acid) is a week GABA transaminase inhibitor with an IC50 of larger than 500 μM; exhibits antitumor activity in vivo and in vitro.

(S)-SNAP5114 (Standard) is the analytical standard of (S)-SNAP5114 (HY-103504). This product is intended for research and analytical applications. (S)-SNAP5114 is a selective GABA transport inhibitor, with IC₅₀ values of 5 μM and 21 μM for hGAT-3 and rGAT-2, respectively. (S)-SNAP5114 is an anticonvulsant agent.

Gabaculine is an amino acid neurotoxin and blood-brain barrier-permeable GABA transaminase inhibitor, with an IC₅₀ of 1 μM in beef and Pseudomonas ovalis. Gabaculine elevates endogenous synaptic and brain GABA levels and enhances GABA activity. Gabaculine induces sedation, hypothermia, loss of righting reflex, and prevents convulsions in mice. Gabaculine is applicable to research related to neurological disorders.

NNC-711 (Standard) is the analytical standard of NNC-711 (HY-103506). This product is intended for research and analytical applications. NNC-711 (NO-711 hydrochloride) is a potent and selective inhibitor of GAT-1 (GABA transporter 1) with IC₅₀ values of 0.04, 0.38, 171, 1700, 349, 622 μM for human GAT-1, rat GAT-1, rGAT-2, hGAT-3, rGAT-3, hBGT-3, respectively. NNC-711 has anticonvulsant and analgesic effect in vivo and exhibits cognition-enhancing activity.

Nipecotic acid (Standard) is the analytical standard of Nipecotic acid. This product is intended for research and analytical applications. Nipecotic acid ((±)-β-Homoproline) is a potent inhibitor of neuronal and glial-aminobutyric acid (GABA) uptake in vitro. Nipecotic acid can also directly activate GABAA-like chloride channels, with an EC50 of approximately 300 μM.