Isoguvacine hydrochloride

SKU: orb1940794

Description

Isoguvacine hydrochloride is a GABA receptor agonist. Isoguvacine hydrochloride binds to rat synaptic cortical membranes and activates α1β2γ2S, α2β2γ2S, α3β2γ2S, α5β2γ2S, and ρ1 subunit GABAA receptors.(In Vitro):Treatment of 50 μM Isoguvacine to block epileptiform events in 2 of 6 organotypic hippocampal slice cultures, Isoguvacine dose-dependently inhibits hypomagnesium-induced epileptiform events. Isoguvacine binds to mouse forebrain synaptic membrane preparations and can specifically bind to GABA, muscimol and bicuculline, but not picrotoxin or diaminobutyric acid. The highest levels of binding are observed in the cerebellum, cortex and hippocampus.

Key Properties

• CAS Number: 68547-97-7
• MW: 163.6
• Purity: >98% (HPLC)
• Formula: C₆H₁₀ClNO₂
• SMILES: Cl.OC(=O)C1=CCNCC1
• Target: NR2B-NMDA
• Solubility: In Vitro: H2O : 100 mg/mL (611.25 mM)

Bioactivity

• In Vitro:
  Isoguvacine binds to a mouse forebrain synaptic membrane preparation. The specific binding is displaceable by GABA, muscimol and bicuculline but not by picrotoxin or diaminobutyric acid. Kinetic data suggest two binding affinities. Highest levels of binding are observed in the cerebellum, cortex and hippocampus. Isoguvacine binds to membrane preparations of rat forebrain with pharmacological characteristics similar to the postsynaptic GABA recognition site: that it is transported into synaptosomal preparations by an uptake system similar to the high-affinity GABA uptake system; and that recently accumulated isoguvacine is released in a Ca2+-dependent manner and by heteroexchange with external GABA. Isoguvacine at a concentration of 50 μM blocks the seizure like events in 2 out of 6 organotypic hippocampal slice cultures. Isoguvacine inhibits the low magnesium induced seizure like events dose dependently.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

1,2,3,6-tetrahydro-4-pyridinecarboxylic acid hydrochloride

Quick Database Links

Gene Symbol

NR2B-NMDA