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International Union of Basic and Clinical Pharmacology. LXXXIII: Classification of Prostanoid Receptors, Updating 15 Years of Progress
TLDR
The DP2 receptor, also termed CRTH2, has little structural resemblance to DP1 and other receptors described in the original prostanoid receptor classification and is anticipated to lead to novel therapeutic entities. Expand
Cloning of a novel human prostaglandin receptor with characteristics of the pharmacologically defined EP2 subtype.
TLDR
The findings suggest that Hup-4 encodes the pharmacologically defined EP2 receptor, whereas the mouse and human cDNAs previously classified as EP2 may represent another EP receptor subtype or the recently defined EP4 subtype. Expand
6-Isopropoxy-9-oxoxanthene-2-carboxylic acid (AH 6809), a human EP2 receptor antagonist.
TLDR
It is discovered that the putative EP1 receptor antagonist 6-isopropoxy-9-oxoxanthene-2-carboxylic acid (AH 6809) also has affinity for the human EP2 receptor, and behaved as an EP2 receptors antagonist and inhibited prostaglandin E2-stimulated increases in cyclic AMP. Expand
Analgesic actions of N‐arachidonoyl‐serotonin, a fatty acid amide hydrolase inhibitor with antagonistic activity at vanilloid TRPV1 receptors
TLDR
This work investigated if AA‐5‐HT antagonizes the transient receptor potential vanilloid‐1 (TRPV1) channel and, as FAAH and TRPV 1 are targets for analgesic compounds, if it exerts analgesia in rodent models of hyperalgesia. Expand
Finding of endocannabinoids in human eye tissues: implications for glaucoma.
TLDR
In eyes from patients with glaucoma, significantly decreased 2-AG and PEA levels were detected in the ciliary body, an important tissue in the regulation of IOP, suggesting that these endogenous compounds may have a role in this disease. Expand
Cloning of a receptor for prostaglandin F2 alpha from the ovine corpus luteum.
TLDR
The level of messenger RNA encoding the FP receptor is high in the midluteal phase ovine corpus luteum and decreases during luteolysis, whereas the amount of FP receptor message decreased when the progesterone level was low or falling. Expand
EP1 Prostanoid Receptor Coupling to Gi/o Up-Regulates the Expression of Hypoxia-Inducible Factor-1α through Activation of a Phosphoinositide-3 Kinase Signaling Pathway
TLDR
It is shown that PGE2 stimulation of the EP1 receptor up-regulates the expression of hypoxia-inducible factor-1α (HIF-1 α), which can be completely blocked by pertussis toxin, indicating coupling to Gi/o. Expand
Prostaglandin Ethanolamides (Prostamides): In Vitro Pharmacology and Metabolism
TLDR
Prostamides' most prominent pharmacological actions are not due to transformation into prostaglandins, activation of prostanoid receptors, enhancement of AEA levels, or gating of TRPV1 receptors, but possibly to interaction with novel receptors that seem to be functional in the cat iris. Expand
Changes in endocannabinoid and palmitoylethanolamide levels in eye tissues of patients with diabetic retinopathy and age-related macular degeneration.
TLDR
The tissue- and disease-selective nature of the changes observed suggests that the compounds analyzed here may play different roles in the control of eye function under different pathological conditions. Expand
Molecular cloning and expression of human EP3 receptors: evidence of three variants with differing carboxyl termini
TLDR
Transient expression in eukaryotic cells showed that the human EP3 receptor variants had similar but not identical radioligand binding properties and differed in their functional coupling to second messenger pathways. Expand
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