Fig. 1 · Structure

Cat. No.: A11937
CAS No.: 67469-81-2
Formula: C₂₈H₃₄N₂O.2HCl
Mol. Weight: 487.51

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GBR-12935 2HCl

Name: GBR-12935 2HCl
Brand: Adooq Bioscience
SKU: A11937
Availability: InStock
Rating: 5 (1 reviews)

Cat. No. A11937 CAS 67469-81-2

DAT and SLC6A2 inhibitor

GBR-12935 is a piperazine derivative which is a potent and selective dopamine reuptake inhibitor.

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In Vitro Studies

GBR-12935 2HCl produced a response in a rat striatal synaptosomal dopamine-release assay, with a reported EC50 of 3.047 μM (95% CI 1.765–5.260 μM; five determinations). This endpoint is distinct from cellular uptake inhibition and does not by itself identify the mechanism of dopamine release in vivo. [1]

Literature-reported observations and conditions; not Adooq-tested protocols or general treatment recommendations.

Micromolar response in a rat synaptosomal dopamine-release assay

Biochemical assay · Isolated rat striatal synaptosomes preloaded with [3H]dopamine [1]

The original reports a micromolar release-assay EC50 for GBR-12935. This preparation-based result limits an interpretation of the compound as having only uptake-blocking effects; it does not establish the molecular route of release in vivo.

Measured endpoints — not treatment concentrations
Endpoint	Reported result	Reference
Reported dopamine-release response in [3H]dopamine-preloaded striatal synaptosomes	EC50 3.047 μM; 95% confidence interval 1.765–5.260 μM; N = 5	[1]

Literature-Reported Treatment Conditions

Exposure duration: 30 min incubation at 37 °C after drug addition to preloaded synaptosomes
Method: Post-incubation filter harvest and scintillation counting of retained radiolabel, normalized using mazindol and buffer-only controls.
Vehicle: Release buffer; all wells contained final 0.1% DMSO.
Co-treatment: Single-compound release experiment; no amphetamine co-treatment attributed to GBR-12935.
Reported limits: The numerical GBR-12935 concentration series and donor sex/strain are not specified in the selected assay methods. General analysis contains amphetamine/nomifensine-specific wording and a release/inhibition wording inconsistency; result retained as the Table 1 reported release-assay endpoint.

Methods and source locations

Compound reported in the paper: GBR-12935 2HCl; Compound label in the paper: GBR-12935

Applies to the named dihydrochloride used in these experiments; does not validate an Adooq lot or establish clinical efficacy.

Table 1 and footnote; Results: Synaptosomal DA Release; Methods: Test Agents and In Vitro DA Release Experiments (including controls, harvest and Data Analysis)

Reported dopamine-release response in [3H]dopamine-preloaded striatal synaptosomes: Sigmoidal curve fit of normalized radiolabel-retention measurements. Table 1 defines N as repetitions per EC50 determination; values are not an uptake IC50. — Table 1 and footnote; Results: Synaptosomal DA Release; Methods: Test Agents and In Vitro DA Release Experiments (including controls, harvest and Data Analysis)

In Vivo Studies

In rats, a single intraperitoneal dose of GBR-12935 2HCl at 10 mg/kg increased waking relative to vehicle. Cumulative wake time over the first 4 h was 172.8 ± 11.0 min (mean ± SEM; n = 10). The study did not provide a 22 h recovery endpoint for GBR-12935. [1]

Acute wake promotion measured by rat EEG/EMG

Animal study · Rats with EEG/EMG sleep-stage monitoring [1]

A single 10 mg/kg intraperitoneal treatment enhanced waking relative to the within-experiment vehicle. The first 4 h result is retained; broad claims of absent rebound or durable efficacy are not made.

Measured endpoints — not treatment concentrations
Endpoint	Reported result	Reference
Cumulative time awake during the first 4 h after dosing	CWT 172.8 ± 11.0 min; mean ± SEM; drug n = 10	[1]
Lowest tested dose significantly affecting wake in the dose-ranging EEG/EMG design	Minimum effective tested dose 10 mg/kg; significant versus vehicle (study significance criterion P ≤ 0.05)	[1]

Conditions shared by the study groups

Route: Intraperitoneal
Frequency: Single administration per test session at ZT-5 (5 h after lights on)
Treatment course: Acute test; first 4 h cumulative wake endpoint
Vehicle: 0.5% methylcellulose / 0.2% Tween-80 in sterile water; administration volume 5 mL/kg

Study groups and reported outcomes
Group / dose	Comparator	Observed result	Reference
GBR-12935 2HCl, 10 mg/kg 10 mg/kg	Separate within-experiment formulation vehicle group. Sleep scoring investigator blinded to treatment.	4 h cumulative wake time 172.8 ± 11.0 min (mean ± SEM). Table 2 identifies 10 mg/kg as the lowest tested dose with a significant wake effect versus vehicle (Dunnett test after significant ANOVA).	[1]

GBR-12935 2HCl, 10 mg/kg: Model: Rats monitored with EEG/EMG; drug n = 10, within-compound vehicle n = 5 (Table 2); Reported limits: Sex and strain of the EEG/EMG cohort are not specified in the relevant methods. The strain given in the separate pharmacokinetic experiment is not transferred.

Methods and source locations

Compound reported in the paper: GBR-12935 2HCl; Compound label in the paper: GBR-12935

Applies to the named dihydrochloride used in these experiments; does not validate an Adooq lot or establish clinical efficacy.

Tables 2–3 and footnotes; Figure 3 and caption; Methods: Test Agents, EEG-EMG Sleep/Wake Studies and Statistical Analysis; Results: Effects of DA-Releasing versus DAT-Inhibiting Agents on Sleep/Wake Measures

Cumulative time awake during the first 4 h after dosing: Manual EEG/EMG stage scoring in 6-sec epochs by a blinded investigator, followed by cumulative wake calculation. Table 2 provides sample size; Table 3 provides the result. — Tables 2–3 and footnotes; Figure 3 and caption; Methods: Test Agents, EEG-EMG Sleep/Wake Studies and Statistical Analysis; Results: Effects of DA-Releasing versus DAT-Inhibiting Agents on Sleep/Wake Measures

Lowest tested dose significantly affecting wake in the dose-ranging EEG/EMG design: Dunnett test following significant main effect in ANOVA; tested doses 0.3, 1, 3 and 10 mg/kg with n = 4, 3, 9 and 10 respectively; vehicle n = 5 (Table 2). This is not an ED50. — Tables 2–3 and footnotes; Figure 3 and caption; Methods: Test Agents, EEG-EMG Sleep/Wake Studies and Statistical Analysis; Results: Effects of DA-Releasing versus DAT-Inhibiting Agents on Sleep/Wake Measures

GBR-12935 2HCl, 10 mg/kg · Tables 2–3 and footnotes; Figure 3 and caption; Methods: Test Agents, EEG-EMG Sleep/Wake Studies and Statistical Analysis; Results: Effects of DA-Releasing versus DAT-Inhibiting Agents on Sleep/Wake Measures

Specifications

Manufacturer	Adooq Bioscience
Actions	Inhibitor
CAS Number	67469-81-2
Applications	DAT and SLC6A2 inhibitor
Formula	C₂₈H₃₄N₂O.2HCl
Molecular Weight	487.51
Synonyms	GBR12935
SMILES	C1CN(CCN1CCCC2=CC=CC=C2)CCOC(C3=CC=CC=C3)C4=CC=CC=C4.Cl.Cl

Storage & Solubility

In Vitro Solubility

Reported Solubility

No reported solubility data are available for this product.

Preparing Stock Solutions

Stock preparation is unavailable for this product molecular weight.

Calculated stock concentrations do not establish solvent solubility. Refer to the reported solubility data for experimental guidance.

Storage

Store powder at -20°C, keep desiccated.
In powder form, the chemical is stable for 36 months.
In solution, store at -20°C and use within 1 month to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

Research References

[1] John A. Gruner, Val R. Marcy, Yin-Guo Lin, et al. The Roles of Dopamine Transport Inhibition and Dopamine Release Facilitation in Wake Enhancement and Rebound Hypersomnolence Induced by Dopaminergic Agents Sleep (2009). PMID: 19928382 DOI: 10.1093/sleep/32.11.1425 Source material

Publications

1 publication citing this product

Alexander D H Kingdon, .et al. , J Antibiot (Tokyo), 2025, Jan;78(1):54-63 PMID: 39402358