ArticleBritish journal of pharmacology1999
Prostaglandin DP receptors positively coupled to adenylyl cyclase in embryonic bovine tracheal (EBTr) cells: pharmacological characterization using agonists and antagonists.
Article in British journal of pharmacology, 1999. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.
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Who cites it
17 citing papers in PubMed, 53 citations in OpenAlex.
- Prostaglandins in the Inflamed Central Nervous System: Potential Therapeutic Targets.Current drug targets · 2024Review
- Role of epigenetics and the transcription factor Sp1 in the expression of the D prostanoid receptor 1 in human cartilage.Frontiers in cell and developmental biology · 2023Article
- Therapeutic Drugs and Devices for Tackling Ocular Hypertension and Glaucoma, and Need for Neuroprotection and Cytoprotective Therapies.Frontiers in pharmacology · 2021Review
- Discovery to Launch of Anti-allergy (Emadine; Patanol/Pataday/Pazeo) and Anti-glaucoma (Travatan; Simbrinza) Ocular Drugs, and Generation of Novel Pharmacological Tools Such as AL-8810.ACS pharmacology & translational science · 2020Article
- Physiological and Pathological Roles of 15-Deoxy-ΔMolecular neurobiology · 2018Review
- Excitotoxicity-induced prostaglandin DJournal of lipid research · 2017Article
- Prostaglandin D2 toxicity in primary neurons is mediated through its bioactive cyclopentenone metabolites.Neurotoxicology · 2013Article
- Inverse agonist and pharmacochaperone properties of MK-0524 on the prostanoid DP1 receptor.PloS one · 2013Article
- Prostanoid receptor antagonists: development strategies and therapeutic applications.British journal of pharmacology · 2009Review
- The P2Y12 antagonists, 2-methylthioadenosine 5'-monophosphate triethylammonium salt and cangrelor (ARC69931MX), can inhibit human platelet aggregation through a Gi-independent increase in cAMP levels.The Journal of biological chemistry · 2009Article
- Inhibition of interleukin-1beta-induced matrix metalloproteinases 1 and 13 production in human osteoarthritic chondrocytes by prostaglandin D2.Arthritis and rheumatism · 2008Article
- PGD(2) DP1 receptor protects brain from ischemia-reperfusion injury.The European journal of neuroscience · 2007Article
- Cerebral arachidonate cascade in dementia: Alzheimer's disease and vascular dementia.Current neuropharmacology · 2006Article
- Prostaglandin D2 induces nuclear import of the sex-determining factor SOX9 via its cAMP-PKA phosphorylation.The EMBO journal · 2005Article
- Expression of functional prostaglandin D (DP) receptors in human corpus cavernosum smooth muscle.International journal of impotence research · 2002Article
- Article
- Pharmacology and autoradiography of human DP prostanoid receptors using [(3)H]-BWA868C, a DP receptor-selective antagonist radioligand.British journal of pharmacology · 2000Article
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Authors and funding
3 authors at 1 institution in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Various prostaglandin agonists representing various classes of receptor subtypes were evaluated for their ability to stimulate adenylyl cyclase via the endogenous DP receptor in embryonic bovine tracheal (EBTr) cells. Two antagonists were used to block the agonist-induced cyclic AMP production. ZK118182 (EC50 = 16+/-4 nM), RS-93520 (EC50 = 23+/- 4 nM), SQ27986 (EC50 = 33+/-9 nM), ZK110841 (EC50 = 33+/-5 nM), BW245C (EC50 = 59+/-19 nM) and PGD2 (EC50=101+/-10 nM) (n = 4-70) were the most potent agonists. Whilst most compounds were full agonists (Emax = 100% relative to PGD2), BW245C was significantly more efficacious than PGD2 (Emax = 121+/-3%; P<0.001) and RS-93520 appeared to be a partial agonist (Emax = 64+/-9%; P<0.001). Agonists from the EP (e.g. enprostil; misoprostol; butaprost), FP (e.g. cloprostenol; fluprostenol; PHXA85), IP (iloprost; PGI2) and TP (U46619) prostanoid receptor classes were weak agonists or inactive in the EBTr cell assay system. The DP-receptor antagonist, BWA868C, showed a competitive antagonist profile with pA2 values of 8.00+/-0.02 and 8.14+/-0.13 in Schild analyses with two structurally different agonists, BW245C and ZK118182, respectively (n = 3). AH6809, another purported DP-receptor antagonist, weakly inhibited PGD2- and ZK 18182-induced cyclic AMP production (K(i)s = 808+/-193 nM and 782+/-178 nM, respectively). The current studies have characterized the DP receptor positively coupled to adenylyl cyclase in EBTr cells using a wide range of agonist and antagonist prostaglandins. These data support the utility of the EBTr cell line as a useful tool for the evaluation of DP receptor agonists and antagonists and for profiling other classes of prostaglandins.
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