1. Membrane Transporter/Ion Channel
    Neuronal Signaling
  2. GABA Receptor
  3. Gaboxadol hydrochloride

Gaboxadol hydrochloride (Synonyms: Lu 02-030 hydrochloride; THIP hydrochloride)

Cat. No.: HY-10233 Purity: 99.34%
Handling Instructions

Gaboxadol hydrochloride (Lu 02-030 hydrochloride; THIP hydrochloride) is a potent agonist of the GABAA receptor and an antagonist of GABAC receptors (IC50=25 μM). Gaboxadol hydrochloride displays a partial agonist efficacy on subunit α1β2γ2 with an ED50 value of 143 µM, a full agonist efficacy at α5 subunit (ED50=28-129 µM) and a superagonist efficacy at α4β3δ (ED50=6 µM). Gaboxadol hydrochloride is a non-opioid analgesic and has hypnotic activities.

For research use only. We do not sell to patients.

Gaboxadol hydrochloride Chemical Structure

Gaboxadol hydrochloride Chemical Structure

CAS No. : 85118-33-8

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10 mM * 1 mL in DMSO USD 97 In-stock
Estimated Time of Arrival: December 31
5 mg USD 150 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

Gaboxadol hydrochloride (Lu 02-030 hydrochloride; THIP hydrochloride) is a potent agonist of the GABAA receptor and an antagonist of GABAC receptors (IC50=25 μM). Gaboxadol hydrochloride displays a partial agonist efficacy on subunit α1β2γ2 with an ED50 value of 143 µM, a full agonist efficacy at α5 subunit (ED50=28-129 µM) and a superagonist efficacy at α4β3δ (ED50=6 µM). Gaboxadol hydrochloride is a non-opioid analgesic and has hypnotic activities[1][2].

IC50 & Target

GABAA receptor; GABAC receptor[1]

In Vitro

Gaboxadol hydrochloride (0.34, 3.5 and 7.0 μM) decreses permeability across Caco-2 cell monolayers with a dose dependent manner, shows the mean Papp values with 8.1 × 10-6 cm·s-1, 6.1 × 10-1 cm·s-6 and 5.6 × 10-6 cm·s-1 for 0.34, 3.5 and 7 μM gaboxadol, respectively[3].

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

In Vivo

Gaboxadol hydrochloride (intraperitoneal injection; 0.5, 1, 1.5, 2, 3, 4, or 5 mg/kg; once daily; three-day interval) normalizes the distance traveled by Fmr1 KO2 mice to WT activity levels at 0.5 mg/kg, additionally, this compound has no effect on locomotor activity in Fmr1 KO2 mice[2].

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

Animal Model: Fmr1 KO2 mice (deletion of the promoter and first exon of Fmr1 resulting in mRNA and protein null mice)[2]
Dosage: 0.5, 1, 1.5, 2, 3, 4, or 5 mg/kg
Administration: Intraperitoneal injection
Result: Normalized Hyperactivity Observed in Fmr1 KO2 mice.
Clinical Trial
Molecular Weight

176.60

Formula

C₆H₉ClN₂O₂

CAS No.

85118-33-8

SMILES

O=C1C2=C(CNCC2)ON1.Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 75 mg/mL (424.69 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 5.6625 mL 28.3126 mL 56.6251 mL
5 mM 1.1325 mL 5.6625 mL 11.3250 mL
10 mM 0.5663 mL 2.8313 mL 5.6625 mL
*Please refer to the solubility information to select the appropriate solvent.
References
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Keywords:

GaboxadolLu 02-030THIPGABA ReceptorGamma-aminobutyric acid Receptorγ-Aminobutyric acid ReceptorGABAAGABACnon-opioidanalgesichypnoticsleepInhibitorinhibitorinhibit

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Product Name:
Gaboxadol hydrochloride
Cat. No.:
HY-10233
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