Prostanoid receptors

Overview

Prostanoid receptors are activated by the endogenous ligands prostaglandins PGD2, PGE1, PGE2, PGF, PGH2, prostacyclin [PGI2] and thromboxane A2. Differences and similarities between human and rodent prostanoid receptor orthologues, and their specific roles in pathophysiologic conditions are reviewed in [1]. Measurement of the potency of PGI2 and thromboxane A2 is hampered by their instability in physiological salt solution; they are often replaced by cicaprost and U46619, respectively, in receptor characterization studies.

Reference

  1. Norel X, Sugimoto Y, Ozen G, et al. International Union of Basic and Clinical Pharmacology. CIX. Differences and Similarities between Human and Rodent Prostaglandin E2 Receptors (EP1-4) and Prostacyclin Receptor (IP): Specific Roles in Pathophysiologic Conditions. Pharmacol Rev 2020;72:910-968.
Excerpt from IUPHAR/BPS Guide to Pharmacology
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Species
Receptor
Family
Assays
Human
Available
Assay modes:
Agonist
Inverse agonist
Antagonist
PAM
NAM
Panels:
Human non-orphan GPCRs
Hematology
à la carte
Reference agonist:
BW245C
EC50:
380 pM
Human
Available
Assay modes:
Agonist
Inverse agonist
Antagonist
PAM
NAM
Panels:
Human non-orphan GPCRs
Immunology/Infection
Hematology
Respiratory
à la carte
Reference agonist:
(15)‐15‐CH3‐PGD2
EC50:
6.8 nM
Human
Available
Assay modes:
Agonist
Inverse agonist
Antagonist
PAM
NAM
Panels:
Human non-orphan GPCRs
Oncology
Neurology
Dermatology
Urology/Reproduction
à la carte
Reference agonist:
PGE2
EC50:
16 nM
Human
Available
Assay modes:
Agonist
Inverse agonist
Antagonist
PAM
NAM
Panels:
Human non-orphan GPCRs
Immunology/Infection
Respiratory
Urology/Reproduction
à la carte
Reference agonist:
misoprostol
EC50:
62 nM
Human
Available
Assay modes:
Agonist
Inverse agonist
Antagonist
PAM
NAM
Panels:
Human non-orphan GPCRs
à la carte
197_PTGER3
Reference agonist:
PGE2
EC50:
4.5 nM
Human
Available
Assay modes:
Agonist
Inverse agonist
Antagonist
PAM
NAM
Panels:
Human non-orphan GPCRs
Immunology/Infection
Oncology
Hematology
Endocrinology/Metabolism
Ophthalmology
Cardiology
Dermatology
Musculoskeletal
Urology/Reproduction
à la carte
Reference agonist:
PGE2
EC50:
4.0 nM
Human
Available
Assay modes:
Agonist
Inverse agonist
Antagonist
PAM
NAM
Panels:
Human non-orphan GPCRs
Ophthalmology
Respiratory
Urology/Reproduction
à la carte
Reference agonist:
fluprostenol
EC50:
98 pM
Human
Available
Assay modes:
Agonist
Inverse agonist
Antagonist
PAM
NAM
Panels:
Human non-orphan GPCRs
Respiratory
à la carte
Reference agonist:
beraprost
EC50:
130 nM
Human
Assay modes:
-
Panels:
-
Reference agonist:
EC50:
Mouse
Available
Assay modes:
Agonist
Inverse agonist
Antagonist
PAM
NAM
Panels:
Mouse non-orphan GPCRs
à la carte
Reference agonist:
BW245C
EC50:
430 pM
Mouse
Available
Assay modes:
Agonist
Inverse agonist
Antagonist
PAM
NAM
Panels:
Mouse non-orphan GPCRs
à la carte
Reference agonist:
(15)‐15‐CH3‐PGD2
EC50:
4.9 nM
Mouse
Available
Assay modes:
Agonist
Inverse agonist
Antagonist
PAM
NAM
Panels:
Mouse non-orphan GPCRs
à la carte
Reference agonist:
PGE2
EC50:
2.2 nM
Mouse
Available
Assay modes:
Agonist
Inverse agonist
Antagonist
PAM
NAM
Panels:
Mouse non-orphan GPCRs
à la carte
Reference agonist:
misoprostol
EC50:
13 nM
Mouse
Available
Assay modes:
Agonist
Inverse agonist
Antagonist
PAM
NAM
Panels:
Mouse non-orphan GPCRs
à la carte
Mouse Ptger3
Reference agonist:
PGE2
EC50:
1.1 nM
Mouse
Available
Assay modes:
Agonist
Inverse agonist
Antagonist
PAM
NAM
Panels:
Mouse non-orphan GPCRs
à la carte
Reference agonist:
PGE2
EC50:
3.3 nM
Mouse
Available
Assay modes:
Agonist
Inverse agonist
Antagonist
PAM
NAM
Panels:
Mouse non-orphan GPCRs
à la carte
Reference agonist:
EC50:
210 pM
Mouse
Available
Assay modes:
Agonist
Inverse agonist
Antagonist
PAM
NAM
Panels:
Mouse non-orphan GPCRs
à la carte
Reference agonist:
beraprost
EC50: