PF-4840154 is a
pyrimidine derivative discovered by
Pfizer at its
Sandwich, Kent research center. The compound is a potent, selective activator of both the human (EC50 = 23 nM) and rat (EC50 = 97 nM)
TRPA1 channels.[1] This compound elicits
nociception in a mouse model through
TRPA1 activation. PF-4840154 is used as a reference
agonist of the
TRPA1 channel for
in-vitrohigh-throughput screening purposes, and is superior to
allyl isothiocyanate for this use.[2] The
TRPA1 channel is considered an attractive pain target based on the fact that
TRPA1 knockout mice showed near complete attenuation of pain behaviors in some
pre-clinical development models.[3][4]
PF-4840154 is a
pyrimidine derivative discovered by
Pfizer at its
Sandwich, Kent research center. The compound is a potent, selective activator of both the human (EC50 = 23 nM) and rat (EC50 = 97 nM)
TRPA1 channels.[1] This compound elicits
nociception in a mouse model through
TRPA1 activation. PF-4840154 is used as a reference
agonist of the
TRPA1 channel for
in-vitrohigh-throughput screening purposes, and is superior to
allyl isothiocyanate for this use.[2] The
TRPA1 channel is considered an attractive pain target based on the fact that
TRPA1 knockout mice showed near complete attenuation of pain behaviors in some
pre-clinical development models.[3][4]