Capsazepine is a synthetic
antagonist of
capsaicin.
It is used as a biochemical tool in the study of
TRPV ion channel
Ion channels are pore-forming membrane proteins that allow ions to pass through the channel pore. Their functions include establishing a resting membrane potential, shaping action potentials and other electrical signals by gating the flow of ...
s.
Pharmacology
Capsazepine blocks the painful sensation of heat caused by capsaicin (the active ingredient of
chilli pepper) which activates the
TRPV1 ion channel. Capsazepine is therefore considered to be a TRPV1
antagonist. The TRPV1 channel functions as a pain and temperature sensor in
mammalians. Capsazepine blocks the activation of TRPV1 channels by other chemicals, but not by other painful stimuli such as heat. Depending on the pharmacological assay, the
IC50 is in the
nanomolar
Molar concentration (also called molarity, amount concentration or substance concentration) is a measure of the concentration of a chemical species, in particular of a solute in a solution, in terms of amount of substance per unit volume of solut ...
to low
micromolar
Molar concentration (also called molarity, amount concentration or substance concentration) is a measure of the concentration of a chemical species, in particular of a solute in a solution, in terms of amount of substance per unit volume of ...
range. In addition to its effects on TRPV1 channels, it was also shown to activate the noxious chemical sensor
TRPA1 channel,
inhibit the cold activated
TRPM8 channel,
and
nicotinic acetylcholine receptors.
It mainly serves as a tool to study the TRPV1 ion channel.
Development
Capsazepine was discovered by a research group working for
Novartis
Novartis AG is a Swiss-American multinational pharmaceutical corporation based in Basel, Switzerland and
Cambridge, Massachusetts, United States (global research).name="novartis.com">https://www.novartis.com/research-development/research-loc ...
.
[ Its synthesis and chemical properties were published in 1994. It was found by modification of the chemical backbone of capsaicin.]
Use in biotechnology
By incorporation of an azobenzene unit, a photoswitchable version of capsazepine (AC4) was developed in 2013 that allows for optical control of TRPV1 channels with light.
LMU Munich, 07/25/2013
See also
*
Discovery and development of TRPV1 antagonists
*
Menthol
*
Herkinorin
*
JWH-133
JWH-133 (Dimethylbutyl-deoxy-Delta-8-THC) is a potent selective CB2 receptor agonist with a Ki of 3.4nM and selectivity of around 200x for CB2 over CB1 receptors. It was discovered by and named after, John W. Huffman.
It's important to note t ...
References
{{Transient receptor potential channel modulators
Capsaicinoids
Catechols
Benzazepines
Chlorobenzenes
Thioureas