Art. -Nr.: HY-182548

BTS 72664

BTS 72664 is a broad-spectrum, non-sedating, orally effective anticonvulsant. Its anticonvulsant effect mainly arises from enhancing GABA_A receptor (GABA_A receptor)-mediated chloride channel currents, while it exerts weak blocking effects on Na⁺ channels (K_i = 350 μM) and NMDA receptors (NMDA receptor) (IC₅₀ = 43 μM). BTS 72664 prevents the elevation of extracellular glutamate, glycine and serine concentrations in neurons, reduces cerebral infarct size, promotes functional recovery, prevents multiple types of epileptic seizures, and has low sedative potential. BTS 72664 can be used for the research of epilepsy, stroke and migraine.

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CAS. Nr.: 165383-52-8
Formel: C₁₃H₁₁ClN₄O
Molecular Weight:274.71

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

BTS 72664 Chemical Structure

CAS. Nr.: 165383-52-8

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Biologische Aktivität
- Beschreibung
- In Vitro
- In Vivo
Chemical Information
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Verweise
Calculators
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Beschreibung

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In Vitro

BTS 72664 (350 μM) weakly binds to voltage-gated Na⁺ channels in rat brain synaptosomal membranes with a K_i of 350 μM^[1].
BTS 72664 (300 μM; 0-6 seconds) significantly reduces ⁸⁶Rb⁺ efflux by 50% from depolarized, Ca²⁺-exposed rat brain synaptosomes^[1].
BTS 72664 inhibits Veratridine (HY-N6691)-induced glutamate efflux from rat brain synaptosomes without altering basal efflux^[1].
BTS 72664 (3-100 μM) weakly reduces NMDA-induced depolarization by ~20% in rat brain cortical wedges, with no significant activity at non-NMDA glutamate receptors^[1].
BTS 72664 (0.3-300 μM) attenuates spontaneous epileptiform discharges in rat brain cortical wedges, with greater potency against Bicuculline (HY-N0219)-induced SEDs (IC₅₀ 94 μM for frequency) than Mg²⁺-removal-induced SEDs (IC₅₀ 189 μM for frequency)^[1].
BTS 72664 (100 μM; 20-45 min) hyperpolarizes the resting membrane potential of rat hippocampal slice CA1 pyramidal neurons by a mean of 9.5 mV^[1].
BTS 72664 (10-100 μM) attenuates NMDA-evoked currents in cultured Swiss mouse cortical neurons with an IC₅₀ of 43 μM^[1].
BTS 72664 (10-100 μM) potentiates GABA-evoked currents in cultured Swiss mouse cortical neurons via a benzodiazepine-independent, Picrotoxin (HY-101391)-sensitive GABA_A channel mechanism, producing a 511% potentiation at 100 μM^[1].

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

In Vivo

BTS 72664 (1.9-9.4 mg/kg; p.o.; single dose; daily; 5 days) potently protects against Bicuculline-induced seizures in mice with an ED₅₀ of 1.9 mg/kg p.o. at peak effect, and no rapid tolerance develops with 5 days of daily dosing^[1].
BTS 72664 (47.5-77.2 mg/kg; p.o.; single dose) protects against maximal electroshock-induced seizures in mice with an ED₅₀ of 47.5 mg/kg p.o. at peak effect, has a duration of action of 4-6 hours, and is more potent at increasing seizure threshold than blocking seizure generalization^[1].
BTS 72664 (14 mg/kg; p.o.; single dose) protects against pentylenetetrazol-induced seizures in mice with an ED₅₀ of 14 mg/kg p.o., and is highly potent at increasing seizure initiation thresholds^[1].
BTS 72664 (60 mg/kg; p.o.; single dose) protects against Picrotoxin-induced seizures in mice with an ED₅₀ of 60 mg/kg p.o^[1].
BTS 72664 (25 mg/kg; p.o.; single dose) protects against 4-aminopyridine (HY-B0604)-induced seizures in mice with an ED₅₀ of 25 mg/kg p.o^[1].
BTS 72664 (18 mg/kg; p.o.; single dose) protects against NMDA (HY-17551)-induced seizures in mice with an ED₅₀ of 18 mg/kg p.o^[1].
BTS 72664 (9 mg/kg; p.o.; single dose) protects against audiogenic seizures in DBA/2 mice with an ED₅₀ of 9 mg/kg p.o^[1].
BTS 72664 (29 mg/kg; p.o.; single dose) protects against seizures in GEPR-9 rats with an ED₅₀ of 29 mg/kg p.o^[1].
BTS 72664 (4.6 mg/kg; p.o.; single dose) protects against Bicuculline-induced seizures in rats with an ED₅₀ of 4.6 mg/kg p.o., showing minimal species difference in potency compared to mice^[1].
BTS 72664 (90 mg/kg; p.o.; single dose) protects against maximal electroshock-induced seizures in rats with an ED₅₀ of 90 mg/kg p.o., showing minimal species difference in potency compared to mice^[1].
BTS 72664 (100-150 mg/kg; p.o.; single dose) dose-dependently improves seizure parameters in amygdala-kindled rats, with a 150 mg/kg p.o. dose producing a 177% increase in seizure threshold and 65% reduction in seizure duration^[1].
BTS 72664 (50 mg/kg; p.o.; every 12 hours; 4 total doses), starting 15 min post-occlusion, reduces ischemic lesion volume by 31% and accelerates functional recovery in Rattus norvegicus with permanent middle cerebral artery occlusion^[1].
BTS 72664 (20-35 mg/kg; i.p.; single initial dose; every 12 hours; 3 subsequent doses), starting 60 min post-occlusion, reduces ischemic lesion volume by 40% in rats with permanent middle cerebral artery occlusion, with no hypothermic contribution to neuroprotection^[1].
BTS 72664 (50 mg/kg; p.o.; single dose), administered 15 min post-cortical insult, rapidly and persistently abolishes cortical spreading depression-associated increases in extracellular glutamate, glycine, and serine in rats^[1].

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

Animal Model:

Swiss CD1 mice^[1]
Dosage:

1.9 mg/kg (30 min post-dose); 9.4 mg/kg (60 min post-dose); 2.8 mg/kg (chronic)
Administration:

p.o.; single dose; p.o.; daily; 5 days
Result:

Had an ED₅₀ of 1.9 mg/kg p.o.
for protection against bicuculline-induced seizures at 30 min post-dose.
Had an ED₅₀ of 9.4 mg/kg p.o.
for protection against bicuculline-induced seizures at 60 min post-dose.
Showed no significant attenuation of anticonvulsant efficacy after 5 consecutive days of 2.8 mg/kg p.o.
daily dosing compared to a single dose.

Animal Model:

Swiss CD1 mice^[1]
Dosage:

47.5 mg/kg (30 min post-dose); 77 mg/kg (60 min post-dose); 77.2 mg/kg (peak protection)
Administration:

p.o.; single dose
Result:

Had an ED₅₀ of 47.5 mg/kg p.o.
for protection against maximal electroshock-induced seizures at 30 min post-dose.
Had an ED₅₀ of 77 mg/kg p.o.
for protection against maximal electroshock-induced seizures at 60 min post-dose.
Provided peak protection against maximal electroshock-induced seizures at 30 min post-dose with a duration of action of 4-6 hours at 77.2 mg/kg p.o.
Had a TID₂₀ of 5.7 mg/kg p.o.
for increasing seizure current threshold by 20%.

Animal Model:

Swiss CD1 mice^[1]
Dosage:

14 mg/kg
Administration:

p.o.; single dose
Result:

Had an ED₅₀ of 14 mg/kg p.o.
for protection against subcutaneous pentylenetetrazol-induced seizures.
Had a TID₂₀ of 5.6 mg/kg p.o.
for increasing pentylenetetrazol-induced initial myoclonic twitch threshold by 20%.
Had a TID₂₀ of 1.1 mg/kg p.o.
for increasing pentylenetetrazol-induced generalized clonic seizure threshold by 20%.

Animal Model:

Swiss CD1 mice^[1]
Dosage:

60 mg/kg
Administration:

p.o.; single dose
Result:

Had an ED₅₀ of 60 mg/kg p.o.
for protection against subcutaneous picrotoxin-induced seizures.

Animal Model:

Swiss CD1 mice^[1]
Dosage:

25 mg/kg
Administration:

p.o.; single dose
Result:

Had an ED₅₀ of 25 mg/kg p.o.
for protection against intracerebroventricular 4-aminopyridine-induced seizures.

Animal Model:

Swiss CD1 mice^[1]
Dosage:

18 mg/kg
Administration:

p.o.; single dose
Result:

Had an ED₅₀ of 18 mg/kg p.o.
for protection against intracerebroventricular NMDA-induced seizures.

Animal Model:

DBA/2 mice^[1]
Dosage:

9 mg/kg
Administration:

p.o.; single dose
Result:

Had an ED₅₀ of 9 mg/kg p.o.
for protection against audiogenic seizures in DBA/2 mice.

Animal Model:

GEPR-9 rats^[1]
Dosage:

29 mg/kg
Administration:

p.o.; single dose
Result:

Had an ED₅₀ of 29 mg/kg p.o.
for protection against seizures in GEPR-9 rats.

Animal Model:

Rats^[1]
Dosage:

4.6 mg/kg
Administration:

p.o.; single dose
Result:

Had an ED₅₀ of 4.6 mg/kg p.o.
for protection against bicuculline-induced seizures in rats.

Animal Model:

Rats^[1]
Dosage:

90 mg/kg
Administration:

p.o.; single dose
Result:

Had an ED₅₀ of 90 mg/kg p.o.
for protection against maximal electroshock-induced seizures in rats.

Animal Model:

Rats^[1]
Dosage:

100 mg/kg; 150 mg/kg
Administration:

p.o.; single dose
Result:

Increased mean kindled seizure threshold by 68% at 100 mg/kg p.o.
Increased mean kindled seizure threshold by 177% at 150 mg/kg p.o.
Reduced mean seizure severity by 59% at 150 mg/kg p.o.
Reduced mean seizure duration by 65% (from 69 to 24 sec) at 150 mg/kg p.o.
Reduced mean afterdischarge duration by 68% (from 105 to 34 sec) at 150 mg/kg p.o.
Caused mild ataxia at 150 mg/kg p.o.
but no significant motor impairment in the rotarod test.

Animal Model:

Rats^[1]
Dosage:

50 mg/kg
Administration:

p.o.; every 12 hours; 4 total doses
Result:

Reduced cerebral lesion volume by 31% (treated: 56.9 mm³; vehicle: 82.6 mm³) at 2 days post-insult.
Showed a significant reduction in contralateral forelimb faults on day 8 post-insult, and when data from days 3, 6, and 8 were combined, compared to vehicle-treated controls.

Animal Model:

Rats^[1]
Dosage:

20 mg/kg (subsequent doses); 35 mg/kg (initial dose)
Administration:

i.p.; single initial dose; i.p.; every 12 hours; 3 subsequent doses
Result:

Reduced cerebral lesion volume by 40% (treated: 43.6 mm³; vehicle: 72.0 mm³) at 6 days post-insult.
Did not decrease core body temperature when monitored for 18 hours after the initial 35 mg/kg i.p.
dose.

Animal Model:

Rats^[1]
Dosage:

50 mg/kg
Administration:

p.o.; single dose
Result:

Abolished the transient, insult-induced increases in extracellular glutamate, glycine, and serine levels in the parietal cortex.
Did not alter extracellular GABA levels, but reduced extracellular glutamate levels compared to basal values in anesthetic-only controls.
Exhibited a rapid onset (30 min post-administration) and effect lasting for at least 2.25 hours from peak brain levels.

Chemical Information

CAS. Nr. 165383-52-8
Molecular Weight 274.71
Formel C₁₃H₁₁ClN₄O
SMILES

ClC(C=C1)=CC=C1O[C@@H](C2=CC=NC3=NC=NN23)C
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[1]. Smith SL, et al. BTS 72664-- a novel CNS drug with potential anticonvulsant, neuroprotective, and antimigraine properties. CNS Drug Rev. 2001;7(2):146-171. [Content Brief]

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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BTS 72664

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Alle iGluR Isoform-spezifische Produkte anzeigen

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BTS 72664 Related Classifications

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