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Dantrolene na

Manufactured by Merck Group
Sourced in United Kingdom

Dantrolene Na is a chemical compound used in laboratory equipment. It functions as a muscle relaxant by inhibiting the release of calcium from the sarcoplasmic reticulum within muscle cells.

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2 protocols using dantrolene na

1

Cardiac Stress Response Protocols

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All procedures were performed in licensed institutional premises under a UK Home Office project licence approved by a university ethics review board, under the UK Animals (Scientific Procedures) Act (1986), and conforming to European Parliament Directive 2010/63/EU. 3.5- to 11.5-month-old wild-type (WT, n = 22) and RyR2-P2328S (RyR2S/S, n = 23) inbred 129/Sv mice (Harlan, UK) were kept in plastic cages at room temperature in 12-h light/dark cycles. Mice had free access to sterile rodent chow and water. All chemical agents were purchased from Sigma-Aldrich (Poole, UK) except where otherwise indicated, with effects of flecainide studied at concentrations of 1 and 5 μm and dantrolene Na at 10 μm.
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2

Transporter Substrate and Inhibitor Selection

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Commercially available compounds were used in the studies. Substrates for P‐gp: loperamide HCl, quinidine, verapamil HCl, substrates for BCRP: dantrolene Na, 2‐amino‐1‐methyl‐6‐ phenylimidazo[4,5‐b] pyridine (PhIP), glyburide, and the permeability markers/non‐substrates: atenolol and minoxidil were acquired from Sigma‐Aldrich (St Louis, MO). Loperamide, quinidine, and verapamil were selected as the prototypical commercial substrates for P‐gp, dantrolene for BCRP substrate, glyburide as dual P‐gp and BCRP substrate, based upon extensive in‐house in vitro and in vivo studies as well as previously published chemical and genetic knockout studies. atenolol and minoxidil are non‐substrates and were used to monitor the tight junctions in epithelial cells of the rodent BBB. The P‐gp and BCRP dual inhibitor, elacridar, was also acquired from Sigma‐Aldrich. The P‐gp inhibitor, valspodar, was acquired from Sigma‐Aldrich and Tocris Bioscience (Minneapolis, MN). Transporter compound specificity has been a challenge, historically. Many compounds inhibit and/or are transported by numerous drug transporters and/or CYP enzymes. The substrates and inhibitors were selected based upon study design and in vitro and in vivo concentrations.
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