Výsledky vyhledávání - "Awilda Stapelfeld"

Enkephalin Analogs as Systemically Active Antinociceptive Agents: O- and N-Alkylated Derivatives of the Dipeptide Amide L-2,6-Dimethyltyrosyl-N-(3-phenylpropyl)-D-alaninamide

Autor: Michael Clare, Donald W. Hansen, Sofya Tsymbalov, Kathleen D. Kudla, M A Savage, Donna L. Hammond, Barnett S. Pitzele, Robert W. Hamilton, Awilda Stapelfeld

Publikováno v: Journal of Medicinal Chemistry. 37:888-896

A number of O- and N-alkylated derivatives of the antinociceptive, orally active, mu-opioid-selective truncated enkephalin analog L-2,6-dimethyltyrosyl-N-(3-phenylpropyl)-D-alaninamide (2, SC-39566) were synthesized to explore the structure-activity

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ff81d7a6fde2284e3efe9a67773eb3c6
https://doi.org/10.1021/jm00033a005

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8-chlorodibenz[b,f][1,4]oxazepine-10(11H)-carboxylic acid,2-[3-[2-(furanylmethyl)thio]-1-oxopropyl]hydrazide (SC-51322): A potent PGE2 antagonist and analgesic

Autor: Awilda Stapelfeld, Melvin Reichman, M. A. Savage, E. Ann Hallinan

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 4:509-514

SC-51322 is the most potent PGE2 antagonist (pA2 = 8.1) and analgesic (ED50 = 0.9 mg/kg) that has been seen in this series of N-substituted dibenzoxazepines.

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::831b7893a6348ead5f5f14ed4d1f4517
https://doi.org/10.1016/0960-894x(94)80027-8

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ChemInform Abstract: N-Substituted Dibenzoxazepines as Analgesic PGE2 Antagonists

Autor: J.‐P. Vanhoeck, Michael F. Rafferty, M. Reichman, Shashidhar N. Rao, M A Savage, Timothy J. Hagen, Robert K. Husa, E. A. Hallinan, Awilda Stapelfeld, Sofya Tsymbalov

Publikováno v: ChemInform. 25

8-Chlorodibenz[b,f][1,4]oxazepine-10(11H)-carboxylic acid, 2-acetylhydrazide (1, SC-19220) has been previously reported by us and others to be a PGE2 antagonist selective for the EP1 receptor subtype with antinociceptive activities. Analogs of SC-192

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::3fa9e44c870fc553bcb212af542b9b5f
https://doi.org/10.1002/chin.199411197

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Systemic analgesic activity and .delta.-opioid selectivity in [2,6-dimethyl-Tyr1, D-Pen2, D-Pen5]enkephalin

Autor: Donald W. Hansen, M A Savage, Melvin Reichman, Ronald C. Haaseth, Donna L. Hammond, Henry I. Mosberg, Awilda Stapelfeld

Publikováno v: Journal of Medicinal Chemistry. 35:684-687

The cyclic peptide [2,6-dimethyl-Tyr1,D-Pen2,D-Pen5]enkephalin (2) was synthesized by solid-phase techniques and contains the optically pure unnatural amino acid 2,6-dimethyltyrosine (DMT) as a replacement for the Tyr1 residue of [D-Pen2,D-Pen5]enkep

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a3f0f77d0818f06a1d0be237a4c896cd
https://doi.org/10.1021/jm00082a008

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Preparation and opioid activity of analogs of the analgesic dipeptide 2,6-dimethyl-L-tyrosyl-N-(3-phenylpropyl)-D-alaninamide

Autor: Donna L. Hammond, Nizal S. Chandrakumar, Awilda Stapelfeld, M A Savage, Patricia C. Contreras, Elaine Rorbacher, Peter K. Yonan

Publikováno v: Journal of Medicinal Chemistry. 35:223-233

A number of analogues of the recently disclosed analgesic dipeptide 2,6-dimethyl-L-tyrosyl-D-alanine-phenylpropylamide (SC-39566, 2) were prepared. These analogues contained oxymethylene, aminomethylene, ketomethylene, bismethylene, and trans double

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3eec793a787f13f4f07c04bba5d63c06
https://doi.org/10.1021/jm00080a005

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2,4-Disubstituted oxazoles and thiazoles as latent pharmacophores for diacylhydrazine of SC-51089, a potent PGE2 antagonist

Autor: M. A. Savage, Awilda Stapelfeld, Timothy J. Hagen, E. Ann Hallinan, Sofya Tsymbalov

Publikováno v: Bioorganicmedicinal chemistry. 9(1)

8-Chlorodibenz[b,f][1,4]oxazepine-10(11H)-carboxylic acid, 2-[1-oxo-3-(4-pyridinyl)propyl]hydrazide, monohydrochloride ( 1 , SC-51089) is a functional PGE 2 antagonist selective for the EP 1 receptor subtype with antinociceptive activity. 1,2 Analogu

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2610b3afa046da61c041d3165ec834e1
https://pubmed.ncbi.nlm.nih.gov/11197330

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Analogs of the delta opioid receptor selective cyclic peptide [2-D-penicillamine,5-D-penicillamine]-enkephalin: 2',6'-dimethyltyrosine and Gly3-Phe4 amide bond isostere substitutions

Autor: M. A. Savage, Nizal S. Chandrakumar, Awilda Stapelfeld, Drury B, Williamson Ln, M. Reichman, Beardsley Pm, Anthony Ew, Lopez Ot

Publikováno v: Journal of medicinal chemistry. 35(16)

In order to develop systemically-active opioid peptides, the delta-selective, opioid pentapeptide [D-Pen2,D-Pen5]-enkephalin (DPDPE) was modified by esterification and by substitution of 2',6'-dimethyltyrosine for tyrosine to yield 4. Compound 4 was

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9aa0525ffacf05a78c25a52fc2656165
https://pubmed.ncbi.nlm.nih.gov/1323677

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Antinociception after intracerebroventricular administration of naltrindole in the mouse

Autor: Donna L. Hammond, Michael F. Rafferty, Awilda Stapelfeld

Publikováno v: European journal of pharmacology. 214(2-3)

Intracerebroventricular (i.c.v.) injection of the delta-opioid receptor antagonist naltrindole hydrochloride (2.2-22.2 nmol) in mice produced a dose-dependent increase in tail flick and hot plate latencies with respective ED50 and 95% confidence limi

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7ef672d902777645cf2b57b0633aff7d
https://pubmed.ncbi.nlm.nih.gov/1325358

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