title: Prostanoid action on the human pulmonary vascular system.
abstract: 1. Four types of prostanoid receptor are present on pulmonary arterial vessels of man. Thromboxane (TP) receptors mediate constriction and are blocked by antagonists such as BAY u-3405, GR 32,191 and EP 169. Prostaglandin (PG) EP3 receptors also mediate constriction, the agonist potency ranking being SC 46,275 > sulprostone > misoprostol > or = PGE2; this action needs to be borne in mind when PGE analogues are used therapeutically. 2. Prostaglandin E2 causes relaxation in a few pulmonary artery preparations: an EP2 receptor may be involved. Prostacyclin, acting through i.p. receptors, consistently produces relaxation and studies are in progress to determine the contribution made by K(+)-channel opening. Agonist potencies of stable prostacyclin analogues and non-prostanoid prostacyclin mimetics, such as BMY 45,778 and the novel diphenylindole CU 23, on human pulmonary artery and platelets are well correlated. Interestingly, the non-prostanoid mimetics show persistent relaxant effects in vitro, which may be related to their high lipophilicities. 3. Prostacyclin and iloprost are being used to treat severe pulmonary hypertension; further study of the pharmacodynamic and pharmacokinetic properties of other i.p. receptor agonists could produce improved therapy.
authors.affiliation: Department of Pharmacology, Chinese University of Hong Kong, Shatin, Hong Kong SAR.
authors.forename: R L
authors.initials: RL
authors.lastname: Jones
authors.forename: Y
authors.initials: Y
authors.lastname: Qian
authors.forename: H N
authors.initials: HN
authors.lastname: Wong
authors.forename: H
authors.initials: H
authors.lastname: Chan
authors.forename: A P
authors.initials: AP
authors.lastname: Yim
mesh_terms: D006801:Humans; D011453:Prostaglandins / Q000494:pharmacology*; D011651:Pulmonary Artery / Q000187:drug effects* / Q000502:physiology / Q000648:ultrastructure; D011667:Pulmonary Veins / Q000187:drug effects* / Q000502:physiology / Q000648:ultrastructure; D011982:Receptors, Prostaglandin / Q000037:antagonists & inhibitors / Q000187:drug effects / Q000502:physiology
chemical_list: D011453:Prostaglandins; D011982:Receptors, Prostaglandin