DPNI-caged-GABA

IC50: N/A DPNI-GABA, also known as Nitroindoline-caged GABA, has similar photochemical properties with MNI-glutamate, including the same quantum yield (0.085), highly water soluble, exhibitting fast photorelease that is efficient at near-UV and 405 nm wavelengths. In vitro: Under the condition of retaining the advantages of nitroindoline cages, DPNI-GABA were modified to minimize the pharmacological interference commonly found with caged GABA reagents. Unlike previous test of the 5-methoxycarbonylmethyl-7-nitroindolinyl-GABA, DPNI-GABA reduced peak GABA-evoked responses with an IC50 of approximately 0.5mM, and blocked GABAA receptors with much lower affinity,. It is most important that the kinetics of receptor activation, comparable to synaptic events, were determined as 10–90% rise-times, and had no effect by DPNI-GABA present at 1 mM concentration, and permitted photolysis of DPNI-GABA to mimic synaptic activation of GABAA receptors. As estimated, the spatial resolution of uncaging DPNI-GABA in dendrites was 2m laterally and 7.5m focally with a laser spot of 1mapplied to cerebellar molecular layer interneurons. Finally, photorelease restricted to the area of the soma inhibited spiking in single Purkinje neurons or molecular layer interneurons for periods regulated by the flash intensity and duration at low DPNI-GABA concentration [1,2]. Under resting conditions, miniature synaptic currents have long been known to represent random transmitter release, but their nature and function in central synapses much remains to be learned about. A new class of miniature currents (‘‘preminis’’) arise by the autocrine activation of axonal receptors following random vesicular release. During the development of the molecular layer, preminis are prominent in gabaergic synapses made by cerebellar interneurons. Premini frequencies, unlike ordinary miniature postsynaptic currents in the same cells, are strongly enhanced by subthreshold depolarization, suggesting that themembrane depolarization they produce belongs to a feedback loop controlling neurotransmitter release. Thus, preminis enhanced neurotransmitter release to guide the formation of the interneuron network at recently formed synaptic contacts . In vivo: So far, no study in vivo has been conducted Clinical trial: So far, no clinical study has been conducted.

Product information

CAS Number: 927866-58-8

Molecular Weight: 499.30

Formula: C15H23N3O12P2

Chemical Name: (2-{[1-(4-aminobutanoyl)-7-nitro-2,3-dihydro-1H-indol-4-yl]oxy}-3-(phosphonooxy)propoxy)phosphonic acid

Smiles: NCCCC(=O)N1CCC2C1=C(C=CC=2OC(COP(O)(O)=O)COP(O)(O)=O)N(=O)=O

InChiKey: QLCHBTSDKGMLRN-UHFFFAOYSA-N

InChi: InChI=1S/C15H23N3O12P2/c16-6-1-2-14(19)17-7-5-11-13(4-3-12(15(11)17)18(20)21)30-10(8-28-31(22,23)24)9-29-32(25,26)27/h3-4,10H,1-2,5-9,16H2,(H2,22,23,24)(H2,25,26,27)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

Products are for research use only. Not for human use.