Results 121 to 130 of about 169 (165)

Prostaglandin Antagonists: Synthesis and Smooth Muscle Activity

Nature, 1969
WE report here the synthesis of substances, structurally related to the prostaglandins, capable of selectively antagonizing the smooth muscle effects of both prostaglandins E1 and F1α. The availability of specific antagonists of prostaglaiidin may help solve problems about the physiological roles of the prostaglandins1.
J, Fried, T S, Santhanakrishnan, J, Himizu, C H, Lin, S H, Ford, B, Rubin, E O, Grigas   +6 more
openaire   +2 more sources

Scalable Synthesis of a Prostaglandin EP4 Receptor Antagonist

The Journal of Organic Chemistry, 2010
The evolution of scalable, economically viable synthetic approaches to the potent and selective prostaglandin EP4 antagonist 1 is presented. The chromatography-free synthesis of multikilogram quantities of 1 using a seven-step sequence (six in the longest linear sequence) is described.
Danny, Gauvreau, Sarah J, Dolman, Greg, Hughes, Paul D, O'Shea, Ian W, Davies   +4 more
openaire   +2 more sources

The cardiac effects of prostaglandins and their modification by the prostaglandin antagonist N-0164.

The Journal of Pharmacology and Experimental Therapeutics, 1980
The cardiac actions of a number of prostaglandins and their modification by the prostaglandin antagonist sodium p-benzyl-4-[1-oxo-2-(4-chlorobenzyl)-3-phenyl propyl]phenyl phosphonate (N-0164) was studied in the isolated guinea-pig heart. Arachidonic acid, prostaglandin (PG)E2 (0.01--1 micrograms) and prostacyclin (0.01--10 micrograms), administered by
G, Allan, R, Levi
openaire   +2 more sources

Prostaglandin E antagonist activity of 11,15-bisdeoxy prostaglandin E1 and congeners

Prostaglandins, 1977
d,l-11, 15-bisdeoxy PGE1 and certain of its congeners were shown to inhibit gerbil colon contractions induced by l-PGE1. While some of these compounds were selectively antagonistic of PGE1-induced contractions, others additionally inhibited the gerbil colon agonist activities of l-PGE2alpha and acetylcholine. The PGE1 inhibitory activity was apparently
E L, Tolman, R, Partridge, E T, Barris
openaire   +2 more sources

An Agonist Dependent Allosteric Antagonist of Prostaglandin EP2 Receptors

ACS Chemical Neuroscience, 2020
All reported prostaglandin EP2 receptor antagonists have a purely orthosteric, competitive mode of action. Herein, we report the characterization of compound 1 (pubchem CID 664888) as the first EP2 antagonist that features a reversible, agonist dependent allosteric mode of action.
Chunxiang Jiang, Radhika Amaradhi, Thota Ganesh, Ray Dingledine   +3 more
openaire   +2 more sources

Desacetyl-1-nantradol: A selective prostaglandin antagonist

Prostaglandins, Leukotrienes and Medicine, 1984
Progress in understanding the action of specific prostaglandins will be facilitated by the discovery of specific antagonists to different types of prostaglandin receptors. It has been suggested that nantradol, a cannabinoid-related compound with strong analgetic properties, is an antagonist for prostaglandin receptors. The interaction of nantradol with
openaire   +2 more sources

Pharmacokinetics, Pharmacodynamics, and Safety of a Prostaglandin D2 Receptor Antagonist

Clinical Pharmacology & Therapeutics, 2007
Laropiprant is a selective antagonist of the prostaglandin D(2) (PGD(2)) receptor subtype 1 (DP1). Three double-blind, randomized, placebo-controlled studies evaluated the safety, tolerability, pharmacokinetics, and pharmacodynamics of single and multiple oral doses of laropiprant in healthy male volunteers. Single doses up to 900 mg and multiple doses
E, Lai, L A, Wenning, T M, Crumley, I, De Lepeleire, F, Liu, J N, de Hoon, A, Van Hecken, M, Depré, D, Hilliard, H, Greenberg, G, O'Neill, K, Metters, K G, Gottesdiener, J A, Wagner   +13 more
openaire   +2 more sources

Adenosine as a natural prostaglandin antagonist in vascular smooth muscle

Prostaglandins, 1977
Adenosine has actions on smooth muscle similar to those of prostaglandin (PG) antagonists. Like some PG antagonists it is a phosphodiesterase inhibitor and seems to interfere with calcium effects. It has agonist/antagonist interactions with theophylline, a PG antagonist.
A I, Ally, D F, Horrobin, R A, Karmali, R O, Morgan, M, Karmazyn, M S, Manku   +5 more
openaire   +2 more sources

The use of progesterone antagonists in combination with prostaglandin for termination of pregnancy

Human Reproduction, 1994
Antiprogestin alone is not sufficiently effective in terminating early pregnancy to be clinically useful. The only exception seems to be immediate post-ovulatory administration which inhibits endometrial development to an extent that prevents implantation of the fertilized ovum. During early pregnancy the uterus is inactive.
M, Bygdeman, M L, Swahn, K, Gemzell-Danielsson, C, Gottlieb   +3 more
openaire   +2 more sources

Prostaglandin antagonists: Studies on the mode of action of polyphloretin phosphate

Biochemical and Biophysical Research Communications, 1971
Summary Studies with polyphloretin phosphate (PPP), a substance that has been reported to block the action of prostaglandins (PGE1 and PGF2α) in certain in vivo and in vitro situations, reveal it has no effect upon PGE1 stimulated cyclic AMP formation in mouse ovaries or rabbit myometrium.
F A, Kuehl, J L, Humes, L R, Mandel, V J, Cirillo, M E, Zanetti, E A, Ham   +5 more
openaire   +2 more sources