Deramciclane
Encyclopedia
Deramciclane is a drug
which acts as an antagonist at the 5-HT2A
receptor
, as an inverse agonist
at the 5-HT2C receptor
, and as a GABA reuptake inhibitor
.
In 2003 Orion Pharma of Finland and partner Pharmacia discontinued the development of deramciclane for generalized anxiety disorder, owing to a lack of efficacy in the combined results of the Phase III trials of the agent.
Drug
A drug, broadly speaking, is any substance that, when absorbed into the body of a living organism, alters normal bodily function. There is no single, precise definition, as there are different meanings in drug control law, government regulations, medicine, and colloquial usage.In pharmacology, a...
which acts as an antagonist at the 5-HT2A
5-HT2A receptor
The mammalian 5-HT2A receptor is a subtype of the 5-HT2 receptor that belongs to the serotonin receptor family and is a G protein-coupled receptor . This is the main excitatory receptor subtype among the GPCRs for serotonin , although 5-HT2A may also have an inhibitory effect on certain areas such...
receptor
Receptor (biochemistry)
In biochemistry, a receptor is a molecule found on the surface of a cell, which receives specific chemical signals from neighbouring cells or the wider environment within an organism...
, as an inverse agonist
Inverse agonist
In the field of pharmacology, an inverse agonist is an agent that binds to the same receptor as an agonist but induces a pharmacological response opposite to that agonist....
at the 5-HT2C receptor
5-HT2C receptor
The 5-HT2C receptor is a subtype of 5-HT receptor that binds the endogenous neurotransmitter serotonin . It is a G protein-coupled receptor that is coupled to Gq/G11 and mediates excitatory neurotransmission. HTR2C denotes the human gene encoding for the receptor, that in humans is located at the...
, and as a GABA reuptake inhibitor
GABA reuptake inhibitor
A GABA reuptake inhibitor is a type of drug which acts as a reuptake inhibitor for the neurotransmitter gamma-Aminobutyric acid by blocking the action of the gamma-Aminobutyric acid transporters...
.
In 2003 Orion Pharma of Finland and partner Pharmacia discontinued the development of deramciclane for generalized anxiety disorder, owing to a lack of efficacy in the combined results of the Phase III trials of the agent.