L 741 626

Manufactured by Bio-Techne

Sourced in United Kingdom, United States

L-741,626 is a selective dopamine D2 receptor antagonist used in scientific research. It functions by binding to and inhibiting the activity of the dopamine D2 receptor, which is involved in various physiological and behavioral processes.

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L-741,626 (1003) (4 citations)

21 protocols using l 741 626

D2R Modulation of Activated CD4+ T Cells

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The spleens of DBA/1 CIA mice were dissected and CD4⁺ T cells were obtained by magnetic cell sorting using a CD4⁺ T cell enrichment kit (BD Biosciences, USA) according to the manufacturer's protocol. Sorted cells were suspended in RPMI 1640 medium containing 10% heat-inactivated calf serum at a final concentration of 5 × 10⁶ cells/ml and stimulated with anti-CD3 and anti-CD28 antibodies (both 2 μg/ml; both from BD Pharmingen, USA) at 37 °C for 48 h to activate the cells. Simultaneously, the CD4⁺ T cells were exposed to the D2R agonist sumanirole (Sigma-Aldrich, USA) with the concentrations of 10^–7 M or 10^–6 M or to the D2R antagonist L-741,626 (Tocris Bioscience, USA) with the concentration of 10^–6 M, which was incubated at 37 °C for 48 h. A combined treatment with L-741,626 (10^–6 M, 30 min earlier) and sumanirole (10^–6 M) was also performed in the cultured CD4⁺ T cells to show a blockage of the D2R agonist by the D2R antagonist.

Wang X.Q., Cai H.H., Deng Q.W., Chang Y.Z., Peng Y.P, & Qiu Y.H. (2023). Dopamine D2 receptor on CD4+ T cells is protective against inflammatory responses and signs in a mouse model of rheumatoid arthritis. Arthritis Research & Therapy, 25, 87.

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Signaling Pathway Analysis in Neuronal Cells

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B-27, L-glutamic acid, deoxyribonuclease (DNase), fluorescent dye, anti-glyceraldehyde-3-phosphate dehydrogenase (GAPDH), soybean trypsin inhibitor, fluo-8, and poly-l-lysine (PLL) were obtained from Sigma-Aldrich (St. Louis, MO, USA). Anti-p-p38 MAPK (p-p38), anti-p-JNK, anti-p-p44/42 MAPK (p-ERK1/2), anti-p38 MAPK, anti-JNK, anti-ERK1/2, and anti-rabbit/mouse IgG antibodies were purchased from Cell Signaling Technology (Beverly, MA, USA). Donkey anti-rabbit/mouse secondary antibodies and Alexa Fluor 488 were obtained from Jackson ImmunoResearch Laboratories, Inc., (PA, USA). Fetal bovine serum, neurobasal medium, RPMI 1640 medium, and trypsin were purchased from Gibco (Gaithersburg, MD, USA). The Gαq inhibitor YM 254,890 was obtained from Wako Pure Chemical Industries (Osaka, Japan). L-741,626, SCH 23390, NMDA, and PP2, LY 23,959 were purchased from Tocris Bioscience (Ellisville, MO, UK). YM 254,896 and PP2 were dissolved in 2% DMSO, L-741,626 was dissolved in 25% DMSO, SCH 23390, NMDA and LY2359549 were dissolved in sterilized saline.

Dai W.L., Bao Y.N., Fan J.F., Ma B., Li S.S., Zhao W.L., Yu B.Y, & Liu J.H. (2020). Blockade of spinal dopamine D1/D2 receptor suppresses activation of NMDA receptor through Gαq and Src kinase to attenuate chronic bone cancer pain. Journal of Advanced Research, 28, 139-148.

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Locomotor Activity Measurement Protocols

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SCH 58261 (Tocris Bioscience, Bristol, UK) was dissolved in saline containing 15% DMSO and 15% Cremophor EL (Sigma-Aldrich). L-741626 (Tocris Bioscience) was dissolved in a saline solution by adding drops of an acetic acid solution. The pH was adjusted to 7.0 with an NaOH solution. SKF 81297 (Tocris Bioscience) was dissolved in saline. All saline-based solutions also served as the vehicle control. The locomotor activity was examined in a VersaMax activity monitoring system (AccuScan Instruments, Columbus, OH, USA) and quantified for 1 h.

Lin C.Y., Lai H.L., Chen H.M., Siew J.J., Hsiao C.T., Chang H.C., Liao K.S., Tsai S.C., Wu C.Y., Kitajima K., Sato C., Khoo K.H, & Chern Y. (2019). Functional roles of ST8SIA3-mediated sialylation of striatal dopamine D2 and adenosine A2A receptors. Translational Psychiatry, 9, 209.

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Dopamine D3 receptor ligand administration

Cited 1 time

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Quinpirole dihydrochloride (Sigma-Aldrich, St. Louis, Missouri, USA) was dissolved in sterile 0.9% saline and administered i.p. in a volume of 1 ml/kg body weight. L-741,626 (Tocris, Ellisville, Missouri, USA) was dissolved in 5% ethanol with 1 M HCl, added by drops until the solution was clear, and injected s.c., typically in a volume of 1 ml/kg body weight (see Baladi et al., 2011a (link); Collins et al., 2005 (link), 2007 (link)). PG 01037 hydrochloride, generously provided by Dr. Amy Newman, was synthesized by J Cao in the Medicinal Chemistry Section, Intramural Research Program, National Institute on Drug Abuse (Baltimore, Maryland, USA) using previously published methods (Grundt et al., 2005 (link)); PG 01037 was dissolved in 0.9% saline and administered s.c., typically in a volume of 1 ml/kg body weight.

Serafine K.M., Bentley T.A., Kilborn D.J., Koek W, & France C.P. (2015). Drinking sucrose or saccharin enhances sensitivity of rats to quinpirole-induced yawning. European journal of pharmacology, 764, 529-536.

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Dopamine Modulation in Postnatal Mice

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All dopamine pharmacological modulators, except for antagonists 2-CMDO (2-Chloro-11-(4-methylpiperazino)dibenz(Z)[b,f]oxepin maleate), were injected at 1 mg/kg body weight^{7 (link)} intraperitoneally (i.p.) into nursing dams on day of birth and P2, then directly into pups until P8. 2-CMDO was injected into pups P5-P8 at 2 mg/kg body weight. Injection was done in dim red light one hour before lights on. Dopamine agonist SKF38393 hydrobromide; high affinity D₂ antagonist L-741626; dopamine transporter 1 inhibitor, GBR12909 dihydrochloride; 2-CMDO were all purchased from Tocris Biosciences. For experiments with Pdgfb-icreERT2 mouse lines, 2 mg Tamoxifen was injected into nursing dams on the day of birth and on P2 to activate tamoxifen-dependent cre.

Nguyen M.T., Vemaraju S., Nayak G., Odaka Y., Buhr E.D., Alonzo N., Tran U., Batie M., Upton B.A., Darvas M., Kozmik Z., Rao S., Hegde R.S., Iuvone P.M., Van Gelder R.N, & Lang R.A. (2019). An Opsin 5-dopamine pathway mediates light-dependent vascular development in the eye. Nature cell biology, 21(4), 420-429.

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Intracranial Drug Infusion Protocol

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JWH133, AM630, SCH23390 and L741,626 were purchased from Tocris Bioscience (Minneapolis, MN). Both JWH133 and AM630 were dissolved in DMSO for in vitro electrophysiology assays and in Tocrisolve-100 (vehicle) for intracranial microinjection. All other drugs were dissolved in saline.

Zhang H.Y., Shen H., Gao M., Ma Z., Hempel B., Bi G.H., Gardner E.L., Wu J, & Xi Z.X. (2021). Cannabinoid CB2 receptors are expressed in glutamate neurons in the red nucleus and functionally modulate motor behavior in mice. Neuropharmacology, 189, 108538.

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Pharmacological Modulation of Neural Signaling

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All drugs were purchased from Sigma Aldrich (St. Louis, MO), or Tocris (Bristol, UK). SKF 81297 hydrobromide (Tocris, 1447) was applied either as puff (500 µM) or flow in (10 µM) depending on experiment type. All other drugs were bath applied: SCH-39166 hydrobromide (Tocris,2299), SCH-23390 hydrochloride (Tocris, 0925), SKF-83566 hydrobromide (Tocris, 1586), Strychnine (Sigma-Aldrich, 8753), Tetraethylammonium chloride (Sigma-Aldrich, 86614), TTX (Tocris Bioscience, 1069), (RS)-CPP (Tocris Bioscience, 0173), NBQX (Tocris Bioscience, 0373), SR 95531 hydrobromide (Tocris Bioscience, 1262), MNI-caged-L-glutamate (Tocris Biosciences 1490), L-741,626 (Tocris Bioscience, 1003), Pyr-3 (Tocris,3753), prazosin (Sigma-Aldrich, P7791), propranolol (Sigma-Aldrich, 40543), and quinpirole hydrochloride (Tocris Bioscience, 1061). For experiments requiring pharmacological agents dissolved in DMSO the concentration never exceeded 0.02% DMSO.

Canton-Josh J.E., Qin J., Salvo J, & Kozorovitskiy Y. (2022). Dopaminergic regulation of vestibulo-cerebellar circuits through unipolar brush cells. eLife, 11, e76912.

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Pharmacological Modulation of Wheel Running

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Haloperidol (Haldol®, Janssen-Cilag, Berchem, Belgium) and SCH23390 (Tocris Bioscience, Ellisville, MO, USA) were dissolved in distilled water and then administered in the drinking water at doses of 0, 0.15 and 0.30, and 0, 0.05 and 0.1 mg/kg-day, respectively. The concentrations of haloperidol and SCH23390 were calculated taking into account the average daily water consumption and weight of mice. Bottles were wrapped in aluminum foil and the drugged water was renewed on a daily basis. Prior to drug exposure, wheel running at the plateau phase was recorded for three consecutive days and taken as baseline. L-741,626 (Tocris Bioscience) was first dissolved in ethanol and then diluted with distilled water (final ethanol concentration 6%). The animals were accustomed to handling and i.p. injections with vehicle for 7 days before exposure to L-741,626 (1, 2, 5 and 10 mg/kg). The last three days of the habituation period were used as baseline.

Jardí F., Laurent M.R., Kim N., Khalil R., De Bundel D., Van Eeckhaut A., Van Helleputte L., Deboel L., Dubois V., Schollaert D., Decallonne B., Carmeliet G., Van den Bosch L., D’Hooge R., Claessens F, & Vanderschueren D. (2018). Testosterone boosts physical activity in male mice via dopaminergic pathways. Scientific Reports, 8, 957.

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Neurotransmitter Receptor Binding Assay

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KA, Physo, PD-128907, PG-01037, and L-741,626 were purchased from Tocris Bioscience (Bristol, UK). ACh was purchased from Sigma–Aldrich (Taufkirchen, Germany).

Lemercier C.E., Schulz S.B., Heidmann K.E., Kovács R, & Gerevich Z. (2016). Dopamine D3 Receptors Inhibit Hippocampal Gamma Oscillations by Disturbing CA3 Pyramidal Cell Firing Synchrony. Frontiers in Pharmacology, 6, 297.

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Pharmacological Agents for Neuroscience Research

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Picrotoxin, MK-801, sulpiride, DNQX, AP5, SCH23390, DHβE, scopolamine, PG01037, L-741626, L-741742, CGP55845 were obtained from Tocris Bioscience. JHU37160 was from Hello Bio. Cocaine and amphetamine were from the NIDA Drug Supply Program. All the other chemicals were from Sigma-Aldrich.

Gong S., Fayette N., Heinsbroek J.A, & Ford C.P. (2021). Cocaine Shifts Dopamine D2 Receptor Sensitivity to Gate Conditioned Behaviors. Neuron, 109(21), 3421-3435.e5.

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