2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. GABA Receptor
  4. ASP8062

ASP8062 is an orally active, blood-brain barrier-permeable selective GABAB receptor allosteric modulator. ASP8062 enhances GABA-mediated activation of GABAB receptors and strengthens GABAergic neurotransmission. ASP8062 reverses Reserpine (HY-N0480)-induced myalgia, regulates the sleep-wake cycle, increases delta wave power during non-REM sleep, and impairs motor coordination at high doses. ASP8062 penetrates the central nervous system with a half-life of 40-50 h. ASP8062 can be used in research related to opioid use disorder, fibromyalgia, chronic pain, and alcohol use disorder[1][2][3][4].

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ASP8062

ASP8062 Chemical Structure

CAS No. : 1704716-36-8

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ASP8062 Related Antibodies

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Description

ASP8062 is an orally active, blood-brain barrier-permeable selective GABAB receptor allosteric modulator. ASP8062 enhances GABA-mediated activation of GABAB receptors and strengthens GABAergic neurotransmission. ASP8062 reverses Reserpine (HY-N0480)-induced myalgia, regulates the sleep-wake cycle, increases delta wave power during non-REM sleep, and impairs motor coordination at high doses. ASP8062 penetrates the central nervous system with a half-life of 40-50 h. ASP8062 can be used in research related to opioid use disorder, fibromyalgia, chronic pain, and alcohol use disorder[1][2][3][4].

IC50 & Target[1]

GABAB receptor

 

In Vitro

ASP8062 acts as a positive allosteric modulator to enhance the potency and maximal response of transfected cell lines stably expressing human or mouse GABAB1c/2 receptors across a wide range of GABA concentrations[2].
ASP8062 exhibits limited to no inhibitory effects on CYP2C9, CYP1A2, CYP2B6, CYP2C8, CYP2C19, CYP2D6, and CYP3A enzymes in human liver microsomes[2].
Metabolism of ASP8062 in liver tissue fractions from mice, rats, rabbits, dogs, monkeys, and humans is mediated primarily by CYP3A4 and secondarily by CYP2D6[2].
ASP8062 (0.003-1 μM) acts as a positive allosteric modulator for both human and rat GABAB receptors in HEK293 cells, decreasing GABA's EC50 and increasing its maximal calcium mobilization response at concentrations of 0.003, 0.3, and 1 μM[3].

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

ASP8062 Related Antibodies
Parmacokinetics
Species Dose Route Cmax Tmax AUC0-24 T1/2
Cynomolgus Monkey[1] 3 mg/kg p.o. 202 ng·h/mL 2.67 h 1700 ng/mL 4.02 h
Cynomolgus Monkey[1] 10 mg/kg p.o. 404 ng·h/mL 3.00 h 4660 ng/mL 7.79 h
In Vivo

ASP8062 (0.3-3 mg/kg; p.o.; once daily for 3 consecutive days; 1 hour prior to morphine self-administration) dose-dependently inhibits morphine self-administration behavior in rhesus monkeys, with an IC50 of 0.97 mg/kg, and the 3 mg/kg dose causes a statistically significant reduction in the number of morphine self-administration episodes[1].
ASP8062 (10 mg/kg; p.o.; single administration; administered immediately after subcutaneous injection of 10 mg/kg morphine) does not potentiate morphine-induced respiratory depression in cynomolgus monkeys[1].
ASP8062 (0.01-10 mg/kg; p.o.; single administration; once daily for 6 consecutive days) exerts significant analgesic effects in a rat fibromyalgia model at oral doses of 0.03, 0.1, 1, and 10 mg/kg, and maintains sustained efficacy after 6 consecutive days of administration[3].
ASP8062 (3-100 mg/kg; p.o.; single administration) impairs motor coordination in normal rats only at the oral dose of 100 mg/kg[3].
ASP8062 (1-10 mg/kg; p.o.; single administration) modulates the sleep architecture of normal rats at an oral dose of 10 mg/kg, reduces rapid eye movement (REM) sleep and sleep fragmentation, and enhances delta wave power during non-rapid eye movement (NREM) sleep[3].
ASP8062 (1-10 mg/kg; p.o.; once daily; for 4 consecutive days) significantly reduces all indicators of operant voluntary alcohol intake in male Sprague Dawley rats without inducing non-specific motor effects, with the highest dose yielding the best therapeutic efficacy[4].
ASP8062 (1-10 mg/kg; p.o.; once daily; for 4 consecutive days) significantly reduces operant alcohol self-administration behavior in female Sprague Dawley rats without inducing non-specific motor effects, with the 3 mg/kg and 10 mg/kg doses showing the strongest efficacy in lever pressing and nose poke entry measures[4].

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

Animal Model: Rhesus monkeys (adult, 1 male, 2 female, 4.16-6.14 kg)[1]
Dosage: 0.3 mg/kg; 1 mg/kg; 3 mg/kg
Administration: p.o.; once daily for 3 days; 1 hour prior to morphine self-administration
Result: Reduced the mean number of morphine self-administrations significantly at 3 mg/kg compared to vehicle-treated controls.
Reached an IC50 value of 0.97 mg/kg.
Showed no gross behavioral signs in any animals during the self-administration period.
Animal Model: Cynomolgus monkeys (male, 4-6 years old, 4.1-5.3 kg)[1]
Dosage: 10 mg/kg
Administration: p.o.; single dose; administered immediately after 10 mg/kg morphine s.c.
Result: Did not produce marked differences in respiratory rate, tidal volume, or minute volume compared to morphine alone.
Did not potentiate morphine-induced reduction in tidal volume (near-significant trend, P=0.06) or statistically significant reduction in minute volume.
Animal Model: Sprague-Dawley (SD) (male, fibromyalgia model via repeated s.c. reserpine injections)[3]
Dosage: 0.01 mg/kg; 0.03 mg/kg; 0.1 mg/kg; 1 mg/kg; 10 mg/kg; 0.3 mg/kg
Administration: p.o.; single dose; daily for 6 days
Result: Significantly reversed the reserpine-induced decrease in muscle pressure threshold at oral doses of 0.03, 0.1, 1, and 10 mg/kg.
Did not produce a significant effect at the 0.01 mg/kg oral dose.
Had its analgesic effect significantly blocked at 0.3 mg/kg p.o. by co-administration of CGP55845 at 3 and 30 mg/kg i.p.
Showed no reduction in analgesic effect after repeated daily administration for 6 days compared to single administration.
Animal Model: Sprague-Dawley (SD) (male, healthy)[3]
Dosage: 3 mg/kg; 10 mg/kg; 30 mg/kg; 100 mg/kg
Administration: p.o.; single dose
Result: Had no significant effect on rotarod retention time at oral doses up to 30 mg/kg.
Significantly reduced time on the rod compared to vehicle-treated rats at 100 mg/kg p.o.
Animal Model: Sprague-Dawley (SD) (male, healthy, surgically implanted with EEG/EMG electrodes)[3]
Dosage: 1 mg/kg; 3 mg/kg; 10 mg/kg
Administration: p.o.; single dose
Result: Significantly decreased the percentage of time spent in REM sleep and the frequency of sleep interruptions at 10 mg/kg p.o.
Dramatically increased the power of delta waves (0.5-4 Hz) during non-REM sleep at 10 mg/kg p.o.
Slightly increased the power of theta waves (4-8 Hz) during REM sleep at 10 mg/kg p.o.
Did not produce significant changes to sleep/wake cycle or EEG activity at 1 and 3 mg/kg p.o.
Animal Model: Sprague Dawley (male, ≥100 days old, initial weight 250−350 gm, chronic intermittent alcohol vapor exposure for 6 weeks, trained to lever press for alcohol under fixed ratio 2 schedule)[4]
Dosage: 1 mg/kg; 3 mg/kg; 10 mg/kg
Administration: p.o.; daily; 4 consecutive days
Result: Significantly decreased active lever presses (P < 0.001), reinforcers earned (P < 0.01−0.001), head entries (P < 0.01−0.001), and estimated alcohol consumed (g/kg, P < 0.001) compared to vehicle.
Produced a significantly greater reduction in reinforcers earned (P < 0.05) and head entries (P < 0.01) at 10 mg/kg than at 1 mg/kg, and a significantly greater reduction in head entries at 10 mg/kg than at 3 mg/kg (P < 0.05).
Showed no significant differences in inactive lever presses across doses.
Did not alter total distance traveled in open field tests.
Animal Model: Sprague Dawley (female, ≥100 days old, initial weight 250−350 gm, chronic intermittent alcohol vapor exposure for 6 weeks, trained to lever press for alcohol under fixed ratio 2 schedule)[4]
Dosage: 1 mg/kg; 3 mg/kg; 10 mg/kg
Administration: p.o.; daily; 4 consecutive days
Result: Significantly decreased active lever presses (P < 0.001) at 3 and 10 mg/kg doses compared to vehicle.
Significantly decreased reinforcers earned (P < 0.05−0.001) across all doses compared to vehicle.
Significantly decreased head entries (P < 0.01) at 3 and 10 mg/kg doses compared to vehicle.
Significantly decreased estimated alcohol consumed (g/kg, P < 0.05−0.001) across all doses compared to vehicle.
Showed no significant differences in inactive lever presses across doses.
Did not alter total distance traveled in open field tests.
Molecular Weight

407.59

Formula

C20H29N3O2S2
CAS No.
SMILES

O=S1(CCN(CC1)CC2=C3C=C(C4CCC(C)(CC4)C)SC3=NC(C)=N2)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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ASP8062 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

ASP80621704716-36-8ASP 8062ASP-8062GABA ReceptorGamma-aminobutyric acid Receptorγ-Aminobutyric acid ReceptorCYP3A4rat fibromyalgia modelGABAcynomolgus monkeysHEK293 cellsrhesus monkeyshuman liver microsomesGABAB receptorSprague Dawley ratsCYP2D6Inhibitorinhibitorinhibit

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