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Fig. 1 | Arthritis Research & Therapy

Fig. 1

From: Pharmacological characterisation of CR6086, a potent prostaglandin E2 receptor 4 antagonist, as a new potential disease-modifying anti-rheumatic drug

Fig. 1

Biochemical characterisation of CR6086 activity on prostaglandin E2 receptor 4 (EP4) receptors. a Effect of CR6086 on prostaglandin E2 (PGE2) binding to EP4 receptor. Membranes from human embryonic kidney cells 293 (HEK293) cells transfected with human EP4 receptor were incubated with [3H]PGE2 and CR6086 (range 1–3000 nM). The results are expressed as percentage inhibition of specific binding. Data are representative of five independent experiments. b Effect of CR6086 on cyclic adenosine monophosphate (cAMP) release from membranes of HEK293 cells transfected with human EP4 receptor and stimulated with 3 nM PGE2 in the presence of CR6086 (range 3–300 nM). Data are representative of three independent experiments. c CR6086 inhibition affinity constant [Ki], and [3H]PGE2 dissociation constant [Kd] towards human and rodent EP4 receptors

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Arthritis Research & Therapy

ISSN: 1478-6362

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