Noradrenergic and specific serotonergic antidepressant
Encyclopedia
Antidepressant
An antidepressant is a psychiatric medication used to alleviate mood disorders, such as major depression and dysthymia and anxiety disorders such as social anxiety disorder. According to Gelder, Mayou &*Geddes people with a depressive illness will experience a therapeutic effect to their mood;...
s. They act by antagonizing
Receptor antagonist
A receptor antagonist is a type of receptor ligand or drug that does not provoke a biological response itself upon binding to a receptor, but blocks or dampens agonist-mediated responses...
various adrenergic
Adrenergic
An adrenergic agent is a drug, or other substance, which has effects similar to, or the same as, epinephrine . Thus, it is a kind of sympathomimetic agent...
and serotonin receptors, of which typically consist of α1-adrenergic and α2-adrenergic, and 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...
, 5-HT2C
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 5-HT3
5-HT3 receptor
The 5-HT3 receptor is a member of the superfamily of ligand-gated ion channels, a superfamily that also includes the neuronal nicotinic acetylcholine receptors , and the inhibitory neurotransmitter receptors for GABA and glycine...
, respectively. By blocking α2-adrenergic autoreceptor
Autoreceptor
An autoreceptor is a receptor located on presynaptic nerve cell membranes and serves as a part of a feedback loop in signal transduction. It is sensitive only to those neurotransmitters or hormones that are released by the neuron in whose membrane the autoreceptor sits.Canonically, a presynaptic...
s and heteroreceptor
Heteroreceptor
A heteroreceptor is a receptor regulating the synthesis and/or the release of mediators other than its own ligand.Heteroreceptors are presynaptic receptors that respond to neurotransmitters, neuromodulators, or neurohormones released from adjacent neurons or cells...
s, NaSSAs enhance adrenergic
Adrenergic
An adrenergic agent is a drug, or other substance, which has effects similar to, or the same as, epinephrine . Thus, it is a kind of sympathomimetic agent...
and serotonergic
Serotonergic
Serotonergic or serotoninergic means "related to the neurotransmitter serotonin". A synapse is serotonergic if it uses serotonin as its neurotransmitter...
neurotransmission
Neurotransmission
Neurotransmission , also called synaptic transmission, is the process by which signaling molecules called neurotransmitters are released by a neuron , and bind to and activate the receptors of another neuron...
, notably 5-HT1A
5-HT1A receptor
The 5-HT1A 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 Gi/Go and mediates inhibitory neurotransmission...
-mediated transmission. Unlike many common antidepressants, the NaSSAs have no efficacy as serotonin reuptake inhibitors.
List of NaSSAs
The NaSSAs include the following agents:- AptazapineAptazapineAptazapine is a tetracyclic antidepressant which was assayed in clinical trials for the treatment of depression in the 1980s but was never marketed...
(CGS-7525A) - EsmirtazapineEsmirtazapineEsmirtazapine is a drug which is under development by Organon for the treatment of insomnia and vasomotor symptoms associated with menopause. As of 2009 it is in phase III clinical trials...
(ORG-50,081) - MianserinMianserinMianserin is a psychoactive drug of the tetracyclic antidepressant chemical class which is classified as a noradrenergic and specific serotonergic antidepressant and has antidepressant, anxiolytic, hypnotic, antiemetic, orexigenic, and antihistamine effects...
(Bolvidon, Norval, Tolvon) - MirtazapineMirtazapineMirtazapine is a tetracyclic antidepressant used primarily in the treatment of depression. It is also sometimes used as a hypnotic, antiemetic, and appetite stimulant, and for the treatment of anxiety, among other indications...
(Remeron, Avanza, Zispin) - SetiptilineSetiptilineSetiptiline , also known as teciptiline, is a tetracyclic antidepressant which acts as a noradrenergic and specific serotonergic antidepressant...
(Tecipul)
Notably, all of these compounds are also classified as tetracyclic antidepressant
Tetracyclic antidepressant
Tetracyclic antidepressants are a class of drugs used primarily as antidepressants that were first introduced in the 1970s. They are named after their chemical structure which contains four rings of atoms and are closely related to the tricyclic antidepressants which contain three rings of...
s (TeCAs).
See also
- Norepinephrine-dopamine disinhibitorNorepinephrine-dopamine disinhibitorNorepinephrine-dopamine disinhibitors are a class of psychoactive drugs used as antidepressants and anxiolytics. They act by antagonizing the serotonin 5-HT2C receptor which normally acts to inhibit norepinephrine and dopamine release, thereby promoting outflow of these neurotransmitters.The only...
(NDDI) - Serotonin antagonist and reuptake inhibitorSerotonin antagonist and reuptake inhibitorSerotonin antagonist and reuptake inhibitors are a class of drugs used mainly as antidepressants, but also as anxiolytics and hypnotics. They act by antagonizing serotonin receptors such as 5-HT2A and inhibiting the reuptake of serotonin, norepinephrine, and/or dopamine. Additionally, most also...
(SARI)