(''R'',''R'')-Tetrahydrochrysene ((''R'',''R'')-THC) is a
drug used to study the
estrogen receptor
Estrogen receptors (ERs) are a group of proteins found inside cells. They are receptors that are activated by the hormone estrogen (17β-estradiol). Two classes of ER exist: nuclear estrogen receptors ( ERα and ERβ), which are members of the ...
s (ERs) in
scientific research
The scientific method is an empirical method for acquiring knowledge that has characterized the development of science since at least the 17th century (with notable practitioners in previous centuries; see the article history of scientific m ...
. It is an
ERβ
Estrogen receptor beta (ERβ) also known as NR3A2 (nuclear receptor subfamily 3, group A, member 2) is one of two main types of estrogen receptor—a nuclear receptor which is activated by the sex hormone estrogen. In humans ERβ is encoded by ...
antagonist and an
ERα
Estrogen receptor alpha (ERα), also known as NR3A1 (nuclear receptor subfamily 3, group A, member 1), is one of two main types of estrogen receptor, a nuclear receptor (mainly found as a chromatin-binding protein)
that is activated by the sex h ...
agonist with 10-fold higher
affinity
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for ERβ relative to ERα.
(''R'',''R'')-THC is a
silent antagonist
A receptor antagonist is a type of receptor ligand or drug that blocks or dampens a biological response by binding to and blocking a receptor rather than activating it like an agonist. Antagonist drugs interfere in the natural operation of recep ...
of ERβ,
and, uniquely relative to other known ERβ antagonists, a
passive antagonist of the receptor.
((''S'',''S'')-THC) also binds to the ERs, but in contrast to (''R'',''R'')-THC, (''S'',''S'')-THC is an agonist of both ERα and ERβ and has 20-fold lower affinity for ERβ relative to (''R'',''R'')-THC.
See also
*
Propylpyrazoletriol
Propylpyrazoletriol (PPT) is a synthetic, nonsteroidal agonist of ERα with 400-fold selectivity over ERβ that is used widely in scientific research to study the function of ERα. Though originally thought to be highly selective for ERα, P ...
(PPT)
*
PHTPP
*
Methylpiperidinopyrazole
Methylpiperidinopyrazole (MPP) is a synthetic, nonsteroidal, and highly selective antagonist of ERα that is used in scientific research to study the function of this receptor. It has 200-fold selectivity for ERα over ERβ and 1000-fold sele ...
(MPP)
*
Diarylpropionitrile (DPN)
*
Prinaberel (ERB-041)
*
Liquiritigenin
Liquiritigenin is a flavanone that was isolated from ''Glycyrrhiza uralensis'', and is found in a variety of plants, including ''Glycyrrhiza glabra'' (licorice). It is an estrogenic compound which acts as a selective agonist of the ERβ subtype ...
*
Menerba
*
2,8-DHHHC
*
Chrysene
References
Estrogens
Antiestrogens
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