Bd1047

Manufactured by Merck Group

Sourced in United States

The BD1047 is a laboratory equipment product. It serves as a core function for laboratory processes, but a detailed description while maintaining an unbiased and factual approach is not available.

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BD1047 dihydrobromide (3 citations)

7 protocols using bd1047

Investigating CXCL10-Mediated Signaling Pathways

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Cocaine, σ-1R antagonist BD1047, IKK-2 inhibitor SC514, and FITC Dextran-4 were purchased from Sigma-Aldrich. Tyrosine kinase inhibitor STI571 was obtained from Novartis. Src kinase inhibitor (PP2) and its inactive orthologue (PP3) were purchased from Calbiochem. CXCR3 antagonist AMG487 was obtained from Tocris Bioscience. The concentrations of these inhibitors were based on the concentration curve study and our previous reports (Niu et al., 2014 (link)).
Cell Tracker Green 5-chloromethylfluorescein diacetate was purchased from Invitrogen. The human CXCL10/IP-10 DuoSet Kit was obtained from R&D Systems. CT-B conjugated to Alexa Fluor 488 was purchased from Invitrogen. Neutralizing human CXCL10/IP-10 antibody was purchased from R&D Systems.

Niu F., Liao K., Hu G., Sil S., Callen S., Guo M.L., Yang L, & Buch S. (2019). Cocaine-induced release of CXCL10 from pericytes regulates monocyte transmigration into the CNS. The Journal of Cell Biology, 218(2), 700-721.

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Neuromodulatory Effects of Pharmacological Agents

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The drugs used in the present study include Fura2-AM, adenosine 5′ triphosphate (ATP), donepezil, acetylcholine, methyllycaconitine (MLA), BD1047, BD1063, LY294002, U73122, PD98059, KN-62, 4,5-diaminofluorescein diacetate (DAF-2DA), and human recombinant TNFα were purchased from Sigma-Aldrich (St. Louis, MO). MSPG [(R,S)-α-2-methyl-4sulfonophenylglycine] was purchased from Tocris Bioscience (Bristol, UK). human recombinant TNFα was diluted with the standard external solution to obtain the final concentration. donepezil was diluted with the standard external solution to obtain the final concentration (5 μM). This donepezil concentration is sufficient to inhibit the AChE activity in both human blood cells and monkey brain samples [23 (link)] or to suppress the LPS-induced NO production in mouse primary microglial cells [21 (link)]. Drugs that were insoluble in water were first dissolved in dimethylsulfoxide (DMSO; Wako Pure Chemical Industries, Osaka, Japan) and then diluted in the standard external solution. The final concentration of DMSO was always less than 0.1%.

Haraguchi Y., Mizoguchi Y., Ohgidani M., Imamura Y., Murakawa-Hirachi T., Nabeta H., Tateishi H., Kato T.A, & Monji A. (2017). Donepezil suppresses intracellular Ca2+ mobilization through the PI3K pathway in rodent microglia. Journal of Neuroinflammation, 14, 258.

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Radiosynthesis and PET Imaging of [19F]FTC-146

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Unless otherwise stated, chemicals were purchased from commercial sources and used without further purification. BD1047 for mice studies was purchased from Sigma Aldrich. [¹⁹F]FTC-146 (99.1 % chemical purity) reference compound was provided by Albany Molecular Research Inc. (Albany, NY). Radiochemistry and semi-preparative high performance liquid chromatography (HPLC) was performed using a TRACERlab FX-FN module (GE Healthcare) with an ancillary HPLC pump (Dionex P680) and UV detector (KNAUER K-2001). Analytical HPLC was performed on a quaternary pump (Agilent 1200 series) equipped with an autosampler, a photodiode array UV detector, and a model 105S single-channel radiation detector (Carroll & Ramsey Associates). Radiotracer doses for animal studies were measured using a dose calibrator (Capintec, CRC-15 PET). Positron emission tomography/computed tomography (PET/CT) imaging of mice was performed using microPET/CT hybrid scanner (Siemens Inveon). All PET data were reconstructed using a 3-dimensional ordered subsets expectation maximization algorithm (16 subsets, 4 iterations) with scatter and dead time correction, and a matrix size of 128 × 128 × 159. Attenuation correction was applied to dataset from CT image.

Shen B., James M.L., Andrews L., Lau C., Chen S., Palner M., Miao Z., Arksey N.C., Shuhendler A.J., Scatliffe S., Kaneshige K., Parsons S.M., McCurdy C.R., Salehi A., Gambhir S.S, & Chin F.T. (2015). Further validation to support clinical translation of [18F]FTC-146 for imaging sigma-1 receptors. EJNMMI Research, 5, 49.

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Cocaine and Sigma-1 Receptor Blockade

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Cocaine was added to cultures at a concentration of 10⁻⁸ M. The sigma-1 receptor blockade BD1047 (Sigma-Aldrich, St. Louis, MO, USA) was added to cultures at a concentration of 10⁻⁶ M. Both remained in culture for forty eight hours until cells were plated in methylcellulose.

Nixon C.C., Schwartz B.H., Dixit D., Zack J.A, & Vatakis D.N. (2015). Cocaine exposure impairs multineage hematopoiesis of human hematopoietic progenitor cells mediated by the sigma-1 receptor. Scientific Reports, 5, 8670.

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Comprehensive S1R Ligand Evaluation

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S1R ligands
haloperidol (Halo), PRE-084 (PRE),
pentazocine (PTZ), and BD-1047 (BD) were purchased from Sigma-Aldrich
(St. Louis, MO, USA), and NE-100 (NE), PD-144418 (PD), and 4-IBP were
from Tocris Bioscience (Bristol, U.K.). A 10 mM stock solution of
each ligand was prepared in DMSO and stored at −20 °C.

Morató X., Fernández-Dueñas V., Pérez-Villamor P., Valle-León M., Vela J.M., Merlos M., Burgueño J, & Ciruela F. (2023). Development of a Novel σ1 Receptor Biosensor Based on Its Heterodimerization with Binding Immunoglobulin Protein in Living Cells. ACS Chemical Neuroscience, 14(11), 2201-2207.

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Intrathecal Administration of Pharmacological Agents

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The following drugs were used: Levo-tetrahydropalmatine (l-THP; Santa Cruz Biotechnology, Santa Cruz, CA, USA); PRE084 (a selective sigma-1 receptor agonist, Sigma); BD1047 (a selective sigma-1 receptor antagonist, Sigma); gabapentin (GBP, a ligand of the α2δ1 subunit of voltage-gated calcium channels, Fluka); naloxone (a non-selective opioid receptor antagonist, Sigma). The doses used in the present study were selected based on doses previously used in literatures28 (link)34 (link)35 (link)36 (link). The drugs were dissolved in 10 μl of saline, while l-THP was dissolved in 5% dimethyl sulfoxide (DMSO, Sigma, St. Louis, MO, USA) in saline solution. For i.t injection, we used the modified method of direct transcutaneous i.t injection in mice37 (link). I.t injections were made into the L5-L6 intervertebral space using a 50 μl Hamilton syringe connected to a 30-gauge needle. The flick of the tail was considered indicative of a successful i.t administration.

Kang D.W., Moon J.Y., Choi J.G., Kang S.Y., Ryu Y., Park J.B., Lee J.H, & Kim H.W. (2016). Antinociceptive Profile of Levo-tetrahydropalmatine in Acute and Chronic Pain Mice Models: Role of spinal sigma-1 receptor. Scientific Reports, 6, 37850.

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Molecular Mechanisms of Cocaine-Induced Vascular Impairment

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Cocaine hydrochloride, SU5416 (antagonist of VEGFR-2), and BD1047 (antagonist of sigma receptor) was obtained from Sigma Aldrich (St. Louis, MO). HIV-1 Tat 1–72 was purchased from University of Kentucky College of Medicine (Lexington, KY). U0126, phosphorylated ERK (Thr202/Tyr204) and PCNA antibody were purchased from Cell Signaling Technology (Beverly, MA). Glutathione, α-tocapherol and β-integrin antibody were purchased from Santa Cruz Biotechnology, Inc (Santa Cruz, CA). L-ascorbate acid sodium salt was obtained from ACROS Organics (Belgium). ZO-1 antibody for immunocytofluorescence staining was purchased from Life Technologies (Carlsbad, CA). ZO-1 antibody for Western blot, Ras activation assay kit, In- vitro vascular permeability assay kit, and compartmental protein extraction kit were purchased from EMD Millipore (Billerica, MA).

Dalvi P., Wang K., Mermis J., Zeng R., Sanderson M., Johnson S., Dai Y., Sharma G., Ladner A.O, & Dhillon N.K. (2014). HIV-1/Cocaine Induced Oxidative Stress Disrupts Tight Junction Protein-1 in Human Pulmonary Microvascular Endothelial Cells: Role of Ras/ERK1/2 Pathway. PLoS ONE, 9(1), e85246.

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