GBR 13098
GBR 13098 is a dopamine transporter inhibitor with a rat IC50 of 43 nM, and exhibits dopaminergic activity in vivo.GBR 13098 selectively blocks dopamine uptake, increasing synaptic dopamine availability, with weaker activity against norepinephrine uptake.GBR 13098 induces ipsilateral circling in lesioned rats and increases locomotor activity in naive mice and habituated rats, with effects attenuated by dopamine receptor antagonism.GBR 13098 reduces DOPA formation in dopamine-rich brain regions and enhances inhibitory responses of substantia nigra zona compacta dopamine neurons to dopamine.GBR 13098 serves as a pharmacological agent for studying dopaminergic systems.
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- CAS 番号: 77862-94-3
- 分子式: C30H39F3N2O7S2
- 分子量:660.77
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
GBR 13098 (1000 nM; 15 min) potently and selectively inhibits [3H]dopamine uptake in rat neostriatal tissue slices (IC50 = 43 nM) over [3H]norepinephrine uptake in rat occipital cortex tissue slices (IC50 = 560 nM), with a 13-fold greater potency for dopamine uptake, and exhibits minimal dopamine release activity at 1000 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
GBR 13098 (2.5-10.0 mg/kg; i.p.) produces dose-dependent ipsilateral rotational behavior in 6-hydroxydopamine-lesioned female Sprague-Dawley rats, with the highest cumulative 6-hour response (1,683 turns) at the 10.0 mg/kg i.p. dose, and this effect is dopamine receptor-mediated[1].
GBR 13098 (0.1-40 mg/kg; i.p.; i.v.; 10-30 min prior to microiontophoresis) acts as a potent, selective dopamine uptake inhibitor in rats, producing a maximal >1500% increase in locomotor activity at 20 mg/kg (i.p.), reducing DOPA formation in dopamine-rich brain regions, and enhancing dopamine-mediated inhibition of substantia nigra dopamine neurons without altering basal firing rate[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Swiss-Webster (male, 25-30 g)[1]
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Dosage:5 mg/kg; 10 mg/kg; 20 mg/kg
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Administration:i.p.
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Result:Caused a slight increase in locomotor activity at 5 and 10 mg/kg doses.
Caused a large increase in locomotor activity at 20 mg/kg dose, which persisted for the full 1.5-hour measurement period.
Greatly attenuated locomotor activity increase when mice were pretreated with haloperidol (0.05-1.0 mg/kg).
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Animal Model:Sprague-Dawley (female, 150-175 g, unilateral 6-hydroxydopamine lesion of the left nigrostriatal pathway, selected for ≥500 ipsilateral turns in 2 hours following amphetamine injection)[1]
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Dosage:2.5 mg/kg; 5.0 mg/kg; 10.0 mg/kg
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Administration:i.p.
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Result:Induced cumulative 6-hour ipsilateral turns of 211 at 2.5 mg/kg.
Induced cumulative 6-hour ipsilateral turns of 459 at 5.0 mg/kg.
Induced cumulative 6-hour ipsilateral turns of 1,683 at 10.0 mg/kg.
Sustained rotational behavior for the full 6-hour measurement period.
Greatly attenuated ipsilateral rotation when rats were pretreated with haloperidol.
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Animal Model:Sprague-Dawley (male, 200-300 g)[2]
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Dosage:10 mg/kg; 20 mg/kg; 40 mg/kg (i.p.); 0.1 mg/kg; 2 mg/kg; 20 mg/kg (i.v.); 20 mg/kg (i.p., 10-30 min prior to microiontophoresis)
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Administration:i.p.; i.v.; 10-30 min prior to microiontophoresis
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Result:Caused a marked increase in spontaneous locomotor activity, with a maximal >1500% increase observed 45-60 minutes after 20 mg/kg (i.p.).
Induced a relatively high degree of stereotypies at 40 mg/kg (i.p.).
Had its locomotor stimulation at 20 mg/kg (i.p.) almost totally prevented by pretreatment with haloperidol or reserpine.
Reduced DOPA formation in the striatum and limbic region at 20 mg/kg (i.p.), but had no effect on dopamine-poor hemispheres.
Did not alter the spontaneous firing rate of most substantia nigra zona compacta dopamine neurons at 0.1-20 mg/kg (i.v.) or 20 mg/kg (i.p.); only 2 of 16 cells showed a slight (~20%) reduction in firing rate 30 minutes after 20 mg/kg (i.v.).
Enhanced the inhibitory response of dopamine neurons to microiontophoretically applied dopamine at 20 mg/kg (i.p., 10-30 min), increasing maximal inhibition from 37% to 65% of spontaneous firing rate, but did not affect the inhibitory response to microiontophoretically applied GABA.
化学情報
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CAS 番号 77862-94-3
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分子量 660.77
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分子式 C30H39F3N2O7S2
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SMILES
CS(=O)(O)=O.CS(=O)(O)=O.FC1=CC=C(CCCN2CCN(CCOC(C3=CC=C(F)C=C3)C4=CC=C(F)C=C4)CC2)C=C1
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
[1]. Heikkila RE, et al. Behavioral properties of GBR 12909, GBR 13069 and GBR 13098: specific inhibitors of dopamine uptake. European journal of pharmacology. 1984 Aug 17;103(3-4):241-8. [Content Brief]
[2]. Pileblad E, et al. GBR 13098, a selective dopamine uptake inhibitor; behavioural, biochemical and electrophysiological studies. Naunyn-Schmiedeberg's archives of pharmacology. 1986 Dec;334(4):383-7. [Content Brief]
Calculators
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