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Rediscovery of old drugs: the forgotten case of dermorphin for postoperative pain and palliation.

Journal of pain research

Hesselink JMK, Schatman ME.
PMID: 30538538
J Pain Res. 2018 Nov 23;11:2991-2995. doi: 10.2147/JPR.S186082. eCollection 2018.

The repurposing of old drugs for new indications is becoming more accepted as a cost-efficient solution for complicated health problems. However, older drugs are often forgotten when they are not repositioned. This analysis makes a case for re-exploration of...

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Hesselink JMK, Schatman ME. Rediscovery of old drugs: the forgotten case of dermorphin for postoperative pain and palliation. J Pain Res. 2018;11:2991-2995doi: 10.2147/JPR.S186082.
Hesselink, J. M. K., & Schatman, M. E. (2018). Rediscovery of old drugs: the forgotten case of dermorphin for postoperative pain and palliation. Journal of pain research, 112991-2995. https://doi.org/10.2147/JPR.S186082
Hesselink, Jan M Keppel, and Schatman, Michael E. "Rediscovery of old drugs: the forgotten case of dermorphin for postoperative pain and palliation." Journal of pain research vol. 11 (2018): 2991-2995. doi: https://doi.org/10.2147/JPR.S186082
Hesselink JMK, Schatman ME. Rediscovery of old drugs: the forgotten case of dermorphin for postoperative pain and palliation. J Pain Res. 2018 Nov 23;11:2991-2995. doi: 10.2147/JPR.S186082. eCollection 2018. PMID: 30538538; PMCID: PMC6260176.
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Fluorescent opioid receptor ligands as tools to study opioid receptor function.

Journal of pharmacological and toxicological methods

Giakomidi D, Bird MF, Guerrini R, Calo G, Lambert DG.
PMID: 34728348
J Pharmacol Toxicol Methods. 2021 Oct 30;107132. doi: 10.1016/j.vascn.2021.107132. Epub 2021 Oct 30.

Opioid receptors are divided into the three classical types: MOP(μ:mu), DOP(δ:delta) and KOP(κ:kappa) that are naloxone-sensitive and an additional naloxone-insensitive nociceptin/orphanin FQ(N/OFQ) peptide receptor(NOP). Studies to determine opioid receptor location and turnover variably rely on; (i) measuring receptor mRNA,...

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Giakomidi D, Bird MF, Guerrini R, et al. Fluorescent opioid receptor ligands as tools to study opioid receptor function. J Pharmacol Toxicol Methods. 2021;107132doi: 10.1016/j.vascn.2021.107132.
Giakomidi, D., Bird, M. F., Guerrini, R., Calo, G., & Lambert, D. G. (2021). Fluorescent opioid receptor ligands as tools to study opioid receptor function. Journal of pharmacological and toxicological methods, 107132. https://doi.org/10.1016/j.vascn.2021.107132
Giakomidi, Despina, et al. "Fluorescent opioid receptor ligands as tools to study opioid receptor function." Journal of pharmacological and toxicological methods vol. (2021): 107132. doi: https://doi.org/10.1016/j.vascn.2021.107132
Giakomidi D, Bird MF, Guerrini R, Calo G, Lambert DG. Fluorescent opioid receptor ligands as tools to study opioid receptor function. J Pharmacol Toxicol Methods. 2021 Oct 30;107132. doi: 10.1016/j.vascn.2021.107132. Epub 2021 Oct 30. PMID: 34728348.
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Fluorescent opioid receptor ligands as tools to study opioid receptor function.

Journal of pharmacological and toxicological methods

Giakomidi D, Bird MF, Guerrini R, Calo G, Lambert DG.
PMID: 34728348
J Pharmacol Toxicol Methods. 2022 Jan-Feb;113:107132. doi: 10.1016/j.vascn.2021.107132. Epub 2021 Oct 30.

Opioid receptors are divided into the three classical types: MOP(μ:mu), DOP(δ:delta) and KOP(κ:kappa) that are naloxone-sensitive and an additional naloxone-insensitive nociceptin/orphanin FQ(N/OFQ) peptide receptor(NOP). Studies to determine opioid receptor location and turnover variably rely on; (i) measuring receptor mRNA,...

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Giakomidi D, Bird MF, Guerrini R, et al. Fluorescent opioid receptor ligands as tools to study opioid receptor function. J Pharmacol Toxicol Methods. 2021;113:107132doi: 10.1016/j.vascn.2021.107132.
Giakomidi, D., Bird, M. F., Guerrini, R., Calo, G., & Lambert, D. G. (2022). Fluorescent opioid receptor ligands as tools to study opioid receptor function. Journal of pharmacological and toxicological methods, 113107132. https://doi.org/10.1016/j.vascn.2021.107132
Giakomidi, Despina, et al. "Fluorescent opioid receptor ligands as tools to study opioid receptor function." Journal of pharmacological and toxicological methods vol. 113 (2022): 107132. doi: https://doi.org/10.1016/j.vascn.2021.107132
Giakomidi D, Bird MF, Guerrini R, Calo G, Lambert DG. Fluorescent opioid receptor ligands as tools to study opioid receptor function. J Pharmacol Toxicol Methods. 2022 Jan-Feb;113:107132. doi: 10.1016/j.vascn.2021.107132. Epub 2021 Oct 30. PMID: 34728348.
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χ-Space Screening of Dermorphin-Based Tetrapeptides through Use of Constrained Arylazepinone and Quinolinone Scaffolds.

ACS medicinal chemistry letters

Van der Poorten O, Van Den Hauwe R, Eiselt E, Betti C, Guillemyn K, Chung NN, Hallé F, Bihel F, Schiller PW, Tourwé D, Sarret P, Gendron L, Ballet S.
PMID: 29152051
ACS Med Chem Lett. 2017 Oct 04;8(11):1177-1182. doi: 10.1021/acsmedchemlett.7b00347. eCollection 2017 Nov 09.

Herein, the synthesis of novel conformationally constrained amino acids, 4-amino-8-bromo-2-benzazepin-3-one (8-Br-Aba), 3-amino-3,4-dihydroquinolin-2-one, and regioisomeric 4-amino-naphthoazepinones (1- and 2-Ana), is described. Introduction of these constricted scaffolds into the

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Van der Poorten O, Van Den Hauwe R, Eiselt E, et al. χ-Space Screening of Dermorphin-Based Tetrapeptides through Use of Constrained Arylazepinone and Quinolinone Scaffolds. ACS Med Chem Lett. 2017;8(11):1177-1182doi: 10.1021/acsmedchemlett.7b00347.
Van der Poorten, O., Van Den Hauwe, R., Eiselt, E., Betti, C., Guillemyn, K., Chung, N. N., Hallé, F., Bihel, F., Schiller, P. W., Tourwé, D., Sarret, P., Gendron, L., & Ballet, S. (2017). χ-Space Screening of Dermorphin-Based Tetrapeptides through Use of Constrained Arylazepinone and Quinolinone Scaffolds. ACS medicinal chemistry letters, 8(11), 1177-1182. https://doi.org/10.1021/acsmedchemlett.7b00347
Van der Poorten, Olivier, et al. "χ-Space Screening of Dermorphin-Based Tetrapeptides through Use of Constrained Arylazepinone and Quinolinone Scaffolds." ACS medicinal chemistry letters vol. 8,11 (2017): 1177-1182. doi: https://doi.org/10.1021/acsmedchemlett.7b00347
Van der Poorten O, Van Den Hauwe R, Eiselt E, Betti C, Guillemyn K, Chung NN, Hallé F, Bihel F, Schiller PW, Tourwé D, Sarret P, Gendron L, Ballet S. χ-Space Screening of Dermorphin-Based Tetrapeptides through Use of Constrained Arylazepinone and Quinolinone Scaffolds. ACS Med Chem Lett. 2017 Oct 04;8(11):1177-1182. doi: 10.1021/acsmedchemlett.7b00347. eCollection 2017 Nov 09. PMID: 29152051; PMCID: PMC5683700.
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Regular physical activity reduces the percentage of spinally projecting neurons that express mu-opioid receptors from the rostral ventromedial medulla in mice.

Pain reports

Sluka KA, Danielson J, Rasmussen L, Kolker SJ.
PMID: 33294758
Pain Rep. 2020 Dec 02;5(6):e857. doi: 10.1097/PR9.0000000000000857. eCollection 2020.

INTRODUCTION: Regular physical activity/exercise is an effective nonpharmacological treatment for individuals with chronic pain. Central inhibitory mechanisms, involving serotonin and opioids, are critical to analgesia produced by regular physical activity. The rostral ventromedial medulla (RVM) sends projections to the...

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Sluka KA, Danielson J, Rasmussen L, et al. Regular physical activity reduces the percentage of spinally projecting neurons that express mu-opioid receptors from the rostral ventromedial medulla in mice. Pain Rep. 2020;5(6):e857doi: 10.1097/PR9.0000000000000857.
Sluka, K. A., Danielson, J., Rasmussen, L., & Kolker, S. J. (2020). Regular physical activity reduces the percentage of spinally projecting neurons that express mu-opioid receptors from the rostral ventromedial medulla in mice. Pain reports, 5(6), e857. https://doi.org/10.1097/PR9.0000000000000857
Sluka, Kathleen A, et al. "Regular physical activity reduces the percentage of spinally projecting neurons that express mu-opioid receptors from the rostral ventromedial medulla in mice." Pain reports vol. 5,6 (2020): e857. doi: https://doi.org/10.1097/PR9.0000000000000857
Sluka KA, Danielson J, Rasmussen L, Kolker SJ. Regular physical activity reduces the percentage of spinally projecting neurons that express mu-opioid receptors from the rostral ventromedial medulla in mice. Pain Rep. 2020 Dec 02;5(6):e857. doi: 10.1097/PR9.0000000000000857. eCollection 2020. PMID: 33294758; PMCID: PMC7717783.
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2',6'-dimethylphenylalanine: a useful aromatic amino Acid surrogate for tyr or phe residue in opioid peptides.

International journal of medicinal chemistry

Sasaki Y, Ambo A.
PMID: 25954528
Int J Med Chem. 2012;2012:498901. doi: 10.1155/2012/498901. Epub 2012 Apr 04.

Two aromatic amino acids, Tyr(1) and Phe(3) or Phe(4), are important structural elements in opioid peptides because they interact with opioid receptors. The usefulness of an artificial amino acid residue 2',6'-dimethylphenylalanine (Dmp) was investigated as an aromatic amino acid...

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Sasaki Y, Ambo A. 2',6'-dimethylphenylalanine: a useful aromatic amino Acid surrogate for tyr or phe residue in opioid peptides. Int J Med Chem. 2012;2012:498901doi: 10.1155/2012/498901.
Sasaki, Y., & Ambo, A. (2012). 2',6'-dimethylphenylalanine: a useful aromatic amino Acid surrogate for tyr or phe residue in opioid peptides. International journal of medicinal chemistry, 2012498901. https://doi.org/10.1155/2012/498901
Sasaki, Yusuke, and Ambo, Akihiro. "2',6'-dimethylphenylalanine: a useful aromatic amino Acid surrogate for tyr or phe residue in opioid peptides." International journal of medicinal chemistry vol. 2012 (2012): 498901. doi: https://doi.org/10.1155/2012/498901
Sasaki Y, Ambo A. 2',6'-dimethylphenylalanine: a useful aromatic amino Acid surrogate for tyr or phe residue in opioid peptides. Int J Med Chem. 2012;2012:498901. doi: 10.1155/2012/498901. Epub 2012 Apr 04. PMID: 25954528; PMCID: PMC4412257.
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Evaluation of Dermorphin Metabolism Using Zebrafish Water Tank Model and Human Liver Microsomes.

Current drug metabolism

de L Castro J, Pereira HMG, de Sousa VP, Martucci MEP.
PMID: 33593255
Curr Drug Metab. 2021;22(5):372-382. doi: 10.2174/1389200222666210216095753.

BACKGROUND: Dermorphin is a heptapeptide with an analgesic potential higher than morphine that does not present the same risk for the development of tolerance. These pharmacological features make dermorphin a potential doping agent in competitive sports and it is...

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de L Castro J, Pereira HMG, de Sousa VP, et al. Evaluation of Dermorphin Metabolism Using Zebrafish Water Tank Model and Human Liver Microsomes. Curr Drug Metab. 2021;22(5):372-382doi: 10.2174/1389200222666210216095753.
de L Castro, J., Pereira, H. M. G., de Sousa, V. P., & Martucci, M. E. P. (2021). Evaluation of Dermorphin Metabolism Using Zebrafish Water Tank Model and Human Liver Microsomes. Current drug metabolism, 22(5), 372-382. https://doi.org/10.2174/1389200222666210216095753
de L Castro, Juliana, et al. "Evaluation of Dermorphin Metabolism Using Zebrafish Water Tank Model and Human Liver Microsomes." Current drug metabolism vol. 22,5 (2021): 372-382. doi: https://doi.org/10.2174/1389200222666210216095753
de L Castro J, Pereira HMG, de Sousa VP, Martucci MEP. Evaluation of Dermorphin Metabolism Using Zebrafish Water Tank Model and Human Liver Microsomes. Curr Drug Metab. 2021;22(5):372-382. doi: 10.2174/1389200222666210216095753. PMID: 33593255.
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Showing 1 to 7 of 7 entries