Metergoline

Manufactured by Merck Group

Sourced in United States

Metergoline is a laboratory equipment product manufactured by Merck Group. It is designed for specialized research and analysis applications. The core function of Metergoline is to serve as a tool for scientific investigations, without interpretation or extrapolation on its intended use.

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Metergoline (M3668) (2 citations)

3 protocols using metergoline

Radioligand Binding Assay for 5-HT1A Receptor

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10 μg of membranes from CHO-K1 cells expressing the human 5-HT1A receptor were suspended in 50 mM Tris-HCl, 10 mM MgSO₄, 0.5 mM EDTA, and 0.1% (w/v) ascorbic acid, pH 7.4 and test ligands (91 nM for single point radioligand displacement assay and 1 nM to 1 μM for full competition assay) were incubated with 0.25 nM [³H]8-hydroxy-DPAT (PerkinElmer, Boston, MA, USA) for 60 min at room temperature. The nonspecific binding was determined using 10 μM metergoline (Sigma, St. Louis, MO, USA). After incubation, the bound ligands were filtered using an M-24 Brandel filtration system (Brandel, Gaithersburg, MD, USA), collected on glass fiber papers (Whatman grade 934-AH, GE Healthcare Bio-Sciences, Pittsburgh, PA, USA), and the radioactivity was quantitated using a MicroBeta2 Microplate scintillation counter 2450 (PerkinElmer, Boston, MA, USA).

Lee B., Taylor M., Griffin S.A., McInnis T., Sumien N., Mach R.H, & Luedtke R.R. (2021). Evaluation of Substituted N-Phenylpiperazine Analogs as D3 vs. D2 Dopamine Receptor Subtype Selective Ligands. Molecules, 26(11), 3182.

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Radioligand Binding Assay Protocol

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5-HT (5-HT hydrochloride), clozapine (8-chloro-11-(4-methyl-1-piperazinyl)-5H-dibenzo[b,e][1,4]diazepine), mesulergine (N′-[(8a)-1,6-dimethylergolin-8-yl]-N,N-dimethylsulfamide hydrochloride), metergoline ([[(8β)-1,6-dimethylergolin-8-yl]-methyl]carbamic acid phenylmethyl ester), isoprenaline hydrochloride, chloroquine (N⁴-(7-chloro-4-quinolinyl)-N¹,N¹-dimethyl-1,4-pentanediamine diphosphate) and mouse anti-FLAG M2 were from Sigma-Aldrich (St. Louis, MO, USA). SB269970 ((R)-3-(2-(2-(4-methyl-piperidin-1-yl)ethyl)-pyrrolidine-1-sulphonyl)-phenol) was from Tocris (Bristol, UK). Olanzapine (ad injectabila) was from Eli Lilly & Co. (Indianapolis, IN, USA). G418, penicillin-streptomycin, L-glutamine and LipofectAMINE2000™ were from Life Technologies). Cy5-conjugated donkey anti-mouse IgG was from Jackson ImmunoResearch (West Grove, PA, USA). [³H]-5-CT (5-carboxamidotryptamine) (60–102 Ci·mmol⁻¹), [N⁶-methyl-³H]-mesulergine (87 Ci·mmol⁻¹), [³H]-SB269970 (36 Ci·mmol⁻¹) and [³H]-CGP12177 (37 Ci·mmol⁻¹) were from GE Healthcare (Buckinghamshire, UK).

Andressen K.W., Manfra O., Brevik C.H., Ulsund A.H., Vanhoenacker P., Levy F.O, & Krobert K.A. (2015). The atypical antipsychotics clozapine and olanzapine promote down-regulation and display functional selectivity at human 5-HT7 receptors. British Journal of Pharmacology, 172(15), 3846-3860.

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Antimalarial Compound Preparation and Assay

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For work involving parasites, chlorpheniramine maleate salt, chlorpromazine hydrochloride, desipramine hydrochloride, promethazine hydrochloride, verapamil hydrochloride and CQ diphosphate (all from Sigma-Aldrich) were dissolved in PBS to a working concentration of 1 mM. LynxTag-CQ_GREEN (BioLynx Technologies, Singapore; hereafter abbreviated to ‘CQ_GREEN’) was dissolved in DMSO to the same concentration. All compounds were stored at −20°C and protected from light. For microsome uptake assays, methiothepin mesylate salt, metergoline, loperamide hydrochloride, octoclothepin maleate salt, mibefradil dihydrochloride hydrate, L703,606 oxalate salt hydrate, and chlorprothixene hydrochloride (all from Sigma-Aldrich) were dissolved in DMSO to 10 mM and stored at 4°C. verapamil hydrochloride, adenosine triphosphate (ATP), and CQ diphosphate (all from Sigma-Aldrich) were dissolved in water to 7.5 mM, 50 mM and 0.1 M respectively and stored at −20°C. Tritiated CQ (³H-CQ; from Moravek Biochemicals and Radiochemicals) was diluted in water to 5.32 µM and stored at −20°C; specific activity was 4.7 Ci/mmol.

Loh C.C., Suwanarusk R., Lee Y.Q., Chan K.W., Choy K.Y., Rénia L., Russell B., Lear M.J., Nosten F.H., Tan K.S, & Chow L.M. (2014). Characterization of the Commercially-Available Fluorescent Chloroquine-BODIPY Conjugate, LynxTag-CQGREEN, as a Marker for Chloroquine Resistance and Uptake in a 96-Well Plate Assay. PLoS ONE, 9(10), e110800.

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