Open AccessInteractions between Prostaglandin Analogues and a Receptor in Bovine Corpora lutea
Author(s) -
POWELL William S.,
HAMMARSTRÖM Sven,
SAMUELSSON Bengt,
MILLER William L.,
SUN Frank F.,
FRIED Josef,
LIN Chu Hong,
JARABAK Joseph
Publication year - 1975
Publication title -
european journal of biochemistry
Language(s) - English
Resource type - Journals
eISSN - 1432-1033
pISSN - 0014-2956
DOI - 10.1111/j.1432-1033.1975.tb02451.x
Subject(s) - prostaglandin f2alpha , chemistry , potency , in vivo , dissociation constant , medicine , receptor , prostaglandin , endocrinology , corpus luteum , biochemistry , biology , hormone , in vitro , microbiology and biotechnology
The dissociation constants for the interactions between some prostaglandin analogues and a prostaglandin F 2α receptor in bovine corpora lutea were determined. These values were compared to the antifertility potencies of these compounds in hamsters and the rates of metabolism by 15‐hydroxyprostaglandin dehydrogenase. The most active analogues with regard to both affinity for the receptor and luteolytic potency were 17‐phenyl‐18,19,20‐trinorprostaglandin F 2α , 15‐methyl‐17‐phenyl‐18,19,20‐trinorprostaglandin F 2α and 15‐methylprostaglandin F 2α . The alkyl side chain of prostaglandins could be modified considerably without altering the affinity for the receptor. In this way metabolism by 15‐hydroxyprostaglandin dehydrogenase could be blocked. Some of these compounds had greatly increased luteolytic effects. Substitution of a phenyl group for the 3 terminal carbon units of the alkyl side chain of prostaglandins increased both the affinity for the receptor and the luteolytic activity in vivo . 7‐oxa‐13‐prostynoic acid, an antagonist of the luteolytic effect of prostaglandin F 2α in vivo was a weak competitive inhibitor of the interaction between prostaglandin F 2α and the receptor.