Diprenorphine

Manufactured by Merck Group

Sourced in United States

Diprenorphine is a laboratory reagent used in research applications. It is a synthetic opioid derivative with pharmaceutical properties. Diprenorphine is primarily utilized as a research tool for studying opioid receptor systems and related pharmacological processes.

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Lab products found in correlation

3h diprenorphine, by PerkinElmer (3 mentions) 35s gtpγs, by PerkinElmer (3 mentions) Guanosine diphosphate gdp, by Merck Group (3 mentions) Damgo, by Merck Group (3 mentions) Tris hydroxymethyl aminomethane tris, by Merck Group (2 mentions) D pen2 d pen5 enkephalin u69 593, by Merck Group (2 mentions) Nor bni, by Merck Group (1 mentions) Naloxone methiodide, by Merck Group (1 mentions) 3h damgo, by PerkinElmer (1 mentions) U69 593, by Merck Group (1 mentions) Cell culture media and supplements, by Merck Group (1 mentions) Naloxone, by Merck Group (1 mentions) 125i nt, by PerkinElmer (1 mentions) Pathhunter detection reagent, by Eurofins (1 mentions) Hank s balanced salt solution hbss, by Merck Group (1 mentions) Unlabeled gtpγs, by Merck Group (1 mentions) Forskolin, by Merck Group (1 mentions)

4 protocols using diprenorphine

Assay for Opioid Receptor Binding

Cited 1 time

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Radioligands [³H]U69,593 (49.3 Ci/mmol), [³H]diprenorphine (33.9 Ci/mmol) and [³⁵S]GTPγS (1250 Ci/mmol) were purchased from PerkinElmer (Boston, MA, USA). Guanosine diphosphate (GDP), GTPγS, U69,593, U50,488, diprenorphine, tris(hydroxymethyl) aminomethane (Tris), 2-[4-(2-hydroxyethyl)piperazin-1-yl]ethanesulfonic acid (HEPES), bovine serum albumin (BSA), formalin, nor-BNI and cell culture media and supplements were obtained from Sigma-Aldrich Chemicals (St. Louis, MO, USA). All other chemicals were of analytical grade and obtained from standard commercial sources. Compound A was obtained from Maybridge Chemical Co., Ltd. (Cornwall, UK) as in [50 (link)], and was prepared as 1 mM stock in 0.5% acetic acid solution and further diluted to working concentrations in the appropriate medium.

Puls K., Olivé-Marti A.L., Pach S., Pinter B., Erli F., Wolber G, & Spetea M. (2022). In Vitro, In Vivo and In Silico Characterization of a Novel Kappa-Opioid Receptor Antagonist. Pharmaceuticals, 15(6), 680.

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Radioligand Binding and G-Protein Activation

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Cell culture media
and supplements were obtained from Sigma-Aldrich Chemicals (St. Louis,
MO) or Life Technologies (Carlsbad, CA). Radioligands [³H]DAMGO, [³H]diprenorphine, [³H]U69,593, and
[³⁵S]GTPγS were purchased from PerkinElmer (Boston).
[³H][Ile^5,6]deltorphin II was obtained from
the Institute of Isotopes Co. Ltd. (Budapest, Hungary). DAMGO, [d-Pen²,d-Pen⁵]enkephalin (DPDPE),
diprenorphine, U69,593, naloxone, naloxone methiodide, tris(hydroxymethyl)
aminomethane (Tris), 2-[4-(2-hydroxyethyl)piperazin-1-yl]ethanesulfonic
acid (HEPES), unlabeled GTPγS, and guanosine diphosphate (GDP)
were obtained from Sigma-Aldrich Chemicals (St. Louis, MO). Morphine
hydrochloride was obtained from Gatt-Koller GmbH (Innsbruck, Austria).
All other chemicals were of analytical grade and obtained from standard
commercial sources. Test compounds were prepared as 1 mM stocks in
water and further diluted to working concentrations in the appropriate
medium.

Spetea M., Rief S.B., Haddou T.B., Fink M., Kristeva E., Mittendorfer H., Haas S., Hummer N., Follia V., Guerrieri E., Asim M.F., Sturm S, & Schmidhammer H. (2018). Synthesis, Biological, and Structural Explorations of New Zwitterionic Derivatives of 14-O-Methyloxymorphone, as Potent μ/δ Opioid Agonists and Peripherally Selective Antinociceptives. Journal of Medicinal Chemistry, 62(2), 641-653.

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Radioligand Binding Assay for Opioid Receptors

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Cell culture
media and supplements
were obtained from Sigma-Aldrich Chemicals (St. Louis, MO) or Life
Technologies (Carlsbad, CA). Radioligands [³H][d-Ala²,N-Me-Phe⁴,Gly-ol⁵]enkephalin ([³H]DAMGO, 50 Ci/mmol), [³H]diprenorphine (37 Ci/mmol), [³H]U69,593 (39.1 Ci/mmol),
and [³⁵S]GTPγS (1250 Ci/mmol) were purchased from
PerkinElmer (Traiskirchen, Austria). [¹²⁵I]-NT (∼2200
Ci/mmol) was purchased from PerkinElmer (Billerica, MA). DAMGO, [d-Pen²,d-Pen⁵]enkephalin (DPDPE),
U69,593, diprenorphine, tris(hydroxymethyl)aminomethane (Tris), 2-[4-(2-hydroxyethyl)piperazin-1-yl]ethanesulfonic
acid (HEPES), unlabeled GTPγS, and guanosine diphosphate (GDP)
were obtained from Sigma-Aldrich Chemicals (St. Louis, MO). PathHunter
detection reagents were obtained from DiscoverX (Birmingham, UK).
All other chemicals were of analytical grade and obtained from standard
commercial sources. Test peptides were prepared as 1 mM stocks in
water and further diluted to working concentrations in the appropriate
medium.

Gonzalez S., Dumitrascuta M., Eiselt E., Louis S., Kunze L., Blasiol A., Vivancos M., Previti S., Dewolf E., Martin C., Tourwé D., Cavelier F., Gendron L., Sarret P., Spetea M, & Ballet S. (2020). Optimized Opioid-Neurotensin Multitarget Peptides: From Design to Structure–Activity Relationship Studies. Journal of Medicinal Chemistry, 63(21), 12929-12941.

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Radioligand Binding Assay for Opioid Receptors

Cited 1 time

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Cell culture media and supplements were obtained from Sigma-Aldrich Chemicals (St. Louis, MO), or Life Technologies (Carlsbad, CA). Radioligands [³H][D-Ala²,N-Me-Phe⁴,Gly-ol⁵]enkephalin ([³H]DAMGO, 50 Ci/mmol), [³H]Diprenorphine (37 Ci/mmol), and [³⁵S]GTPγS (1250 Ci/mmol) were purchased from PerkinElmer (Boston, MA). [³H]HS665 (30.65 Ci/mmol) was prepared by Dr. Geza Toth (Institute of Biochemistry, Biological Research Centre, Hungarian Academy of Sciences, Szeged, Hungary) as previously described^{49 (link)}. DAMGO, [D-Pen²,D-Pen⁵]enkephalin (DPDPE), U69,593, Diprenorphine, Tris(hydroxymethyl) aminomethane (Tris), 2-[4-(2-hydroxyethyl)piperazin-1-yl]ethanesulfonic acid (HEPES), Hank’s Balanced Salt Solution (HBSS), unlabeled GTPγS, guanosine diphosphate (GDP) and forskolin were obtained from Sigma-Aldrich Chemicals (St. Louis, MO). Morphine hydrochloride was obtained from Gatt-Koller GmbH (Innsbruck, Austria). Compounds 1a and 2a were synthesized according to the described procedure^{13 (link)}, and 14-OMO (3) and 14-MM (4) were prepared as earlier described^{16 (link),50 (link)}. All other chemicals were of analytical grade and obtained from standard commercial sources.

Dumitrascuta M., Bermudez M., Ben Haddou T., Guerrieri E., Schläfer L., Ritsch A., Hosztafi S., Lantero A., Kreutz C., Massotte D., Schmidhammer H., Wolber G, & Spetea M. (2020). N-Phenethyl Substitution in 14-Methoxy-N-methylmorphinan-6-ones Turns Selective µ Opioid Receptor Ligands into Dual µ/δ Opioid Receptor Agonists. Scientific Reports, 10, 5653.

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