Zobrazeno 1 - 10
of 16
pro vyhledávání: '"Awilda Stapelfeld"'
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
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.
Publikováno v:
ChemInform. 25
Autor:
Awilda Stapelfeld, D. W. Jun. Hansen, B. S. Pitzele, Donna L. Hammond, M. A. Savage, Michael Clare, S. Tsymbalov, Robert W. Hamilton, K. D. Kudla
Publikováno v:
ChemInform. 25
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
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
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
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
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
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