Thyroid receptor ligands. 6. A high affinity "direct antagonist" selective for the thyroid hormone receptor.
A new high-affinity thyroid hormone antagonist 6 with druglike properties was designed and synthesized. The compound behaved as an antagonist in a cell transactivation assay, and in a first in vivo experiment in rats.
Koehler
Konrad
K
Karo Bio AB, Novum, Huddinge SE-141 57, Sweden.
Gordon
Sandra
S
Brandt
Peter
P
Carlsson
Bo
B
Bäcksbro-Saeidi
Anna
A
Apelqvist
Theresa
T
Agback
Peter
P
Grover
Gary J
GJ
Nelson
William
W
Grynfarb
Marlena
M
Färnegårdh
Mathias
M
Rehnmark
Stefan
S
Malm
Johan
J
D000818:Animals; D016466:CHO Cells; D006224:Cricetinae; D003412:Cricetulus; D006801:Humans; D008024:Ligands; D008958:Models, Molecular; D010666:Phenylpropionates / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D011725:Pyridines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D051381:Rats; D011988:Receptors, Thyroid Hormone / Q000037:antagonists & inhibitors*; D037021:Thyroid Hormone Receptors alpha / Q000037:antagonists & inhibitors; D037042:Thyroid Hormone Receptors beta / Q000037:antagonists & inhibitors / Q000737:chemistry; D015533:Transcriptional Activation / Q000187:drug effects
C516213:3-(3,5-dibromo-4-(4-hydroxy-3-isopropyl-5-(2-pyridin-4-ylvinyl)phenoxy)phenyl)propionic acid; D008024:Ligands; D010666:Phenylpropionates; D011725:Pyridines; D011988:Receptors, Thyroid Hormone; D037021:Thyroid Hormone Receptors alpha; D037042:Thyroid Hormone Receptors beta