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The First Orally Active Low Molecular Weight Agonists for the LH Receptor: Thienopyr(im)idines with Therapeutic Potential for Ovulation Induction
Author(s) -
van Straten N. C. R.,
SchoonusGerritsma G. G.,
van Someren R. G.,
Draaijer J.,
Adang A. E. P.,
Timmers C. M.,
Hanssen R. G. J. M.,
van Boeckel C. A. A.
Publication year - 2002
Publication title -
chembiochem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.05
H-Index - 126
eISSN - 1439-7633
pISSN - 1439-4227
DOI - 10.1002/1439-7633(20021004)3:10<1023::aid-cbic1023>3.0.co;2-9
Subject(s) - ovulation , luteinizing hormone , pharmacology , endogeny , receptor , in vivo , chemistry , ovulation induction , agonist , hormone , oral administration , mode of action , orally active , endocrinology , medicine , biology , biochemistry , microbiology and biotechnology
Pregnancy in pill form? The identification of low molecular weight (LMW) agonists for receptors normally triggered by high molecular weight (HMW) endogenous ligands is a great challenge for medicinal chemists. Thienopyrimidines and thienopyridines of general structures 1 and 2 , respectively, are the first orally active LMW agonists for the G‐protein‐coupled luteinizing hormone receptor, which is responsible for ovulation induction. The LMW agonists display micromolar to nanomolar potencies and in vivo ovulation induction could be demonstrated in mice after oral administration. Thus, these compounds mimic the mode of action of the endogenous HMW glycopeptidic luteinizing hormone.