Capsazepine is a synthetic analogue of capsaicin

Capsaicin

Capsaicin 2CHCH=CH4CONHCH2C6H3-4--3- ) is the active component of chili peppers, which are plants belonging to the genus Capsicum. It is an irritant for mammals, including humans, and produces a sensation of burning in any tissue with which it comes into contact...

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Pharmacaology

Capsazepine blocks the painful sensation of heat caused by capsaicin (the active ingredient of chilli pepper) which activates the TRPV1

TRPV1

The transient receptor potential cation channel subfamily V member 1 ', also known as the capsaicin receptor and the vanilloid receptor 1, is a protein that, in humans, is encoded by the TRPV1 gene...

 ion channel

Ion channel

Ion channels are pore-forming proteins that help establish and control the small voltage gradient across the plasma membrane of cells by allowing the flow of ions down their electrochemical gradient. They are present in the membranes that surround all biological cells...

. It is therefore considered to be a capsaicin antagonist. The TRPV1 channel functions as a pain and temperature sensor in mammalians. Capsazepine blocks only the activation of TRPV1 channels by chemicals but not by other painful stimuli, like heat. Depending on the pharmacological assay the half maximal inhibitory concentration IC50

IC50

The half maximal inhibitory concentration is a measure of the effectiveness of a compound in inhibiting biological or biochemical function. This quantitative measure indicates how much of a particular drug or other substance is needed to inhibit a given biological process by half...

 is in the nanomolar to low micromolar range. In addition to its effects on TRPV1 channels it was also shown to inhibit the cold activated TRPM8

TRPM8

Transient receptor potential cation channel subfamily M member 8 , also known as the cold and menthol receptor 1 , is a protein that in humans is encoded by the TRPM8 gene.-Function:...

 channel, voltage-activated calcium channels

Voltage-dependent calcium channel

Voltage-dependent calcium channels are a group of voltage-gated ion channels found in excitable cells with a permeability to the ion Ca2+...

 and nicotinic acetylcholine receptor

Nicotinic acetylcholine receptor

Nicotinic acetylcholine receptors, or nAChRs, are cholinergic receptors that form ligand-gated ion channels in the plasma membranes of certain neurons and on the postsynaptic side of the neuromuscular junction...

s. It mainly serves as a tool to study the TRPV1 ion channel.

Development

Capsazepine was discovered by a research group at the Sandoz Institute for Medical Research. Its synthesis and chemical properties were published in 1994. It was found by modification of the chemical backbone of capsaicin.

External links

• Initial Study on PubMed