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Endomorphin 1

Manufactured by Bio-Techne
Sourced in United Kingdom, United States

Endomorphin-1 is a synthetic peptide that is a potent and selective agonist of the μ-opioid receptor. It is commonly used in laboratory research to study the effects of μ-opioid receptor activation.

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2 protocols using endomorphin 1

1

Opioid Ligand Preparation and Storage

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All cell culture media and supplements were from Invitrogen (Paisley, UK). All other reagents were from Sigma Chemical Co. (Poole, UK) and were of the highest purity available. DPDPE, endomorphin‐1, naloxone, and SB‐612111 were bought from Tocris Bioscience (Bristol, UK). Fentanyl was bought from SALARAS, Como, Italy) (authorization SP/270, 26/11/2012). Native coelenterazine (CLZN, 5 mmol/L, EtOH) was from Synchem UG & Co. KG (Altenburg, Germany). N/OFQ, dermorphin, dynorphin A, Ro 65‐6570, and cebranopadol were synthesized in house. Stock solutions (1 mmol/L) of peptides and fentanyl were made in distilled water. SB‐612111, Ro 65‐6570, and cebranopadol (10 mmol/L) were solubilized in DMSO. Stock solutions of ligands were stored at −20°C.
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2

Comparative Analysis of MOR Agonists

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We chose six MOR agonists that include endogenous and exogenous ligands and that vary in terms of G-protein bias: morphine (Sigma–Aldrich; St. Louis, MO, USA), DAMGO ([D-Ala2-MePhe4-Gly-ol]-enkephalin; Bachem, Torrance, CA, USA), met-enkephalin (Sigma–Aldrich), β-endorphin (American Peptide Co., Sunnyvale, CA, USA), endomorphin-1 (Tocris Bioscience, Minneapolis, MN, USA), and TRV130 (oliceridine; synthesized by B.E.B.). All ligands except TRV130, which was first dissolved in DMSO (20%), were dissolved in water, then prepared as serial dilutions to concentrations between 10−11 to 10−5 M. GPCR independent substrates including forskolin, TNF-α and PMA (Sigma–Aldrich) were used to activate cAMP, NF-ĸB and MAPK/JNK respectively. All GPCR independent substrates were diluted in DMSO to final concentrations of 10 μM for forskolin, 50 ng/mL for TNF-α, and 10 ng/mL for PMA.
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