2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. GlyT
  4. Org 24461

Org 24461 is a selective and brain-penetrant GlyT-1 inhibitor. Org 24461 blocks glycine uptake, reuptake, reverse operation, [3H]glycine efflux and release. Org 24461 enhances NMDA receptor function, modulates striatal monoamine/glutamate levels, and reverses PCP-induced behavioral and electrographic abnormalities. Org 24461 can be used for the research of retinal hypoxia/ischemia, and schizophrenia.

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Org 24461

Org 24461 Chemical Structure

CAS No. : 372198-80-6

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Description

Org 24461 is a selective and brain-penetrant GlyT-1 inhibitor. Org 24461 blocks glycine uptake, reuptake, reverse operation, [3H]glycine efflux and release. Org 24461 enhances NMDA receptor function, modulates striatal monoamine/glutamate levels, and reverses PCP-induced behavioral and electrographic abnormalities. Org 24461 can be used for the research of retinal hypoxia/ischemia, and schizophrenia[1][2][3][4][5].

IC50 & Target[1]

GLT1

 

In Vitro

Org 24461 (40 min) potently inhibits glycine uptake in CHO cells stably expressing hGlyT-1b with an IC50 of 100 nM[1][2].
Org 24461 (0.1-30 μM; 20 min) reverses 7-Chlorokynurenic acid (HY-100811)-induced extension of NMDA-mediated spreading depression latency in isolated chicken retina with an IC50 of 0.36 μM, and reduces NMDA (HY-17551)-induced spreading depression latency at 10-30 μM in the absence of 7-chlorokynurenic acid[1].
Org 24461 (0.3 mM; 90 min) potently inhibits oxygen-glucose deprivation-induced [3H]glycine release from isolated chicken retina, while having no effect on basal normoxic glycine efflux[2].
Org 24461 (5 min preincubation; 10 min incubation at 37°C) potently inhibits high-affinity [3H]glycine uptake in rat cerebral cortex synaptosomes (IC50 = 1.3 μM) and rat striatum synaptosomes (IC50 = 1.8 μM)[3].
Org 24461 inhibits [3H]glycine uptake in rat hippocampal P2 synaptosomes with an IC50 of 2.5 μM at a low [3H]glycine concentration, and an IC50 of 28 μM at a high [3H]glycine concentration[4].
Org 24461 does not affect spontaneous [3H]glycine efflux from superfused rat hippocampal slices, but inhibits glycine-stimulated [3H]glycine efflux in the same preparation[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Org 24461 Related Antibodies
In Vivo

Org 24461 (10 mg/kg; i.p.; single dose) significantly decreases extracellular striatal dopamine concentrations in conscious rats, with no effect on glutamate or serine levels[3].
Org 24461 (10 mg/kg; i.p.; single dose; co-administered with Risperidone (HY-11018) 1 mg/kg i.p.) normalizes extracellular striatal dopamine concentrations, maintains elevated extracellular glycine concentrations, and induces a significant increase in extracellular glutamate concentrations in conscious rats[3].
Org 24461 (2-8 mg/kg; i.p.; single dose) inhibits PCP-induced hypermotility in male NMRI mice with an ID50 of 3.8 mg/kg i.p[4].
Org 24461 (3-30 mg/kg; i.p.; single dose) inhibits D-amphetamine-induced hypermotility in male NMRI mice with an ID50 of 13.5 mg/kg i.p[4].
Org 24461 (1-10 mg/kg; i.p.; single dose) dose-dependently reverses PCP-induced EEG power spectral changes in conscious male Wistar rats[4].
Org 24461 (10 mg/kg; i.v.; single dose) significantly reverses the L-701324 (HY-18698)-induced reduction in rat dorsal raphe nucleus single neuron firing rate[5].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: NMRI (male, 25-33 g, phencyclidine/PCP-induced hypermotility model)[4]
Dosage: 2 mg/kg; 4 mg/kg; 8 mg/kg
Administration: i.p.; single dose
Result: Dose-dependently inhibited PCP-induced hypermotility, with an ID50 value of 3.8 mg/kg i.p.
Animal Model: NMRI (male, 25-33 g, D-amphetamine-induced hypermotility model)[4]
Dosage: 3 mg/kg; 10 mg/kg; 30 mg/kg
Administration: i.p.; single dose
Result: Dose-dependently inhibited D-amphetamine-induced hypermotility, with an ID50 value of 13.5 mg/kg i.p.
Animal Model: Wistar (male, 500 g, PCP-induced EEG power spectral change model)[4]
Dosage: 1 mg/kg; 3 mg/kg; 10 mg/kg
Administration: i.p.; single dose
Result: Dose-dependently attenuated PCP-induced power decrements at higher frequencies (5-30 Hz) in prefrontal and sensorimotor cortices.
Induced synchronization peaks at 3-5 Hz and 8-20 Hz frequency bands in the prefrontal cortex at 10 mg/kg i.p.
Animal Model: Wistar (male, 250-300 g, neuronal hypofunction induced by NMDA receptor glycineB site blockade)[5]
Dosage: 10 mg/kg
Administration: i.v.; single dose
Result: Reversed L-701324-induced inhibition of dorsal raphe nucleus neuron firing, restoring rates from 3.64 Hz to near control levels (7.64 vs. 7.92 Hz) with statistical significance.
Increased firing within 1 minute after injection, peaked at 4–5 minutes, then declined gradually.
Tended to elevate dorsal raphe nucleus neuronal firing when given alone, but the effect was not significant.
Molecular Weight

367.36

Formula

C19H20F3NO3
CAS No.
SMILES

O=C(CN(CCC(C1=CC=CC=C1)OC2=CC=C(C(F)(F)F)C=C2)C)O
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Storage

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Keywords:

Org 24461372198-80-6Org24461Org-24461GlyTGlycine transportersrisperidoneblood-brain barrierschizophreniaCHO cells7-chlorokynurenic acidstriatal dopaminePCPGlyT-1glycineNMDA receptorsInhibitorinhibitorinhibit

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