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4hydroxyNdesmethyltamoxifen

4-hydroxy-N-desmethyl is a shorthand designation that may refer to a metabolite derived from a parent amine-containing drug. The full name and structure depend on the parent compound, but the descriptor indicates two common biotransformations: N-demethylation (removal of a methyl group from the nitrogen atom) and 4-hydroxylation (addition of a hydroxy group at the fourth position of an aromatic or other ring system). As such, "4-hydroxy-N-desmethyl" describes a class of related metabolites rather than a single, fixed molecule.

These metabolites are typically produced by hepatic enzymes in phase I metabolism, often involving cytochrome P450

The pharmacological activity of 4-hydroxy-N-desmethyl metabolites depends on the parent compound. Some retain partial receptor activity

Analytically, these metabolites are detected in biological samples by LC-MS/MS in pharmacokinetic and toxicology studies. Understanding

isoforms
(for
example,
CYP3A4
and
CYP2D6).
They
may
be
formed
sequentially
or
via
parallel
pathways.
Depending
on
the
parent
drug,
the
metabolite
may
be
further
processed
by
phase
II
conjugation
(glucuronidation
or
sulfation),
increasing
water
solubility
for
excretion.
The
exact
structure
and
prevalence
vary
by
species
and
individual
genotype.
or
contribute
to
therapeutic
effect
or
adverse
effects;
others
are
largely
inactive.
Genetic
polymorphisms
in
metabolizing
enzymes
and
drug
interactions
can
influence
their
levels
and
clinical
impact.
their
formation
aids
interpretation
of
drug
exposure,
efficacy,
and
safety,
and
informs
drug
development
and
monitoring.