The Journal of pharmacology and experimental therapeutics

J Pharmacol Exp Ther · ISSN (print) 0022-3565 · 6 papers in corpus
other 2026
PRT-064040: A nasal spray of novel, potent, and selective calcitonin gene-related peptide receptor antagonist for migraine
doi:10.1016/j.jpet.2026.104966 ·PMID:42475993

Calcitonin gene-related peptide (CGRP), a neuropeptide, has been implicated in autoimmune diseases, endometriosis, tumors, and primary headaches, including migraine. The development of a novel, fast-acting CGRP receptor antagonist administe…

article 2011
The Translational Efficacy of a Nonsteroidal Progesterone Receptor Antagonist, 4-[3-Cyclopropyl-1-(mesylmethyl)-5-methyl-1H-pyrazol-4-yl]oxy,-2,6-dimethylbenzonitrile (PF-02413873), on Endometrial Growth in Macaque and Human
doi:10.1124/jpet.111.183848 ·PMID:21849626

There is considerable ongoing investment in the research and development of selective progesterone receptor (PR) modulators for the treatment of gynecological conditions such as endometriosis. Here, we provide the first report on the clinic…

other 2010
A long-acting tumor necrosis factor alpha-binding protein demonstrates activity in both in vitro and in vivo models of endometriosis
doi:10.1124/jpet.110.166488 ·PMID:20435921

Endometriosis is characterized by the presence of elevated proinflammatory cytokines such as tumor necrosis factor (TNF) alpha in the peritoneal cavity. Blocking interaction of TNFalpha with its receptor by the addition of excess TNFalpha-b…

other 2008
The translational pharmacology of a novel, potent, and selective nonsteroidal progesterone receptor antagonist, 2-[4-(4-cyano-phenoxy)-3,5-dicyclopropyl-1H-pyrazol-1-yl]-N-methylacetamide (PF-02367982)
doi:10.1124/jpet.108.140467 ·PMID:18593954

The progesterone receptor (PR) is an important regulator of endometrial function. Blockade of PR function has been recognized as the potential basis for preventing gynecological conditions such as endometriosis and uterine fibroids. In this…

other 2003
Biological characterization of a novel, orally active small molecule gonadotropin-releasing hormone (GnRH) antagonist using castrated and intact rats
doi:10.1124/jpet.102.046656 ·PMID:12606616

Gonadotropin-releasing hormone (GnRH) receptor antagonists have potential in treating numerous hormone-dependent pathologies including cancers of the prostate, breast, and ovary, endometriosis, and fertility disorders. An unmet clinical nee…

article 1988
One-month release injectable microcapsules of a luteinizing hormone-releasing hormone agonist (leuprolide acetate) for treating experimental endometriosis in rats.
doi:10.1016/s0022-3565(25)24466-4 ·PMID:3126294

Leuprolide acetate is a highly potent analog of luteinizing hormone-releasing hormone. We have prepared 1-month release injectable microcapsules of leuprolide acetate using a biodegradable polymer, poly (dl-lactide-co-glycolide), to treat a…