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tricyclic antidepressants
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Tricyclic antidepressants and mood stabilisers have a different mechanism of action. The mechanisms can be classified according to the action of tricyclic and mode therapeutic action.
Mechanisms of action
Tricyclic antidepressants and mood stabilisers act upon the central and/or peripheral mechanisms of action for many different psychoactive substances, including amphetamines, phencyclidine (PCP), MDMA, ketamine and cannabis.
The binding of tricyclic antidepressants and mood stabilisers to the serotonin and norepinephrine transporters (5-HT NE respectively) is the main mechanism for their action on central and peripheral pathways. These receptors are found mainly in the brain, including cerebellum and spinal cord.
Tricyclic antidepressants are also known to bind some of the other serotonin, norepinephrine, noradrenaline, epinephrine, dopamine transporters (DAT and NET respectively) may
diazepam 10 mg tablet mylan also have some activity through antagonism of these receptor sites. It is believed that tricyclic antidepressants bind directly to the receptors without activating enzymes which catalyse the subsequent reactions.
Mechanisms of action tricyclic antidepressants and mood stabilisers are discussed briefly below.
Monoamine transporters
A monoamine transporter (MT) is the major involved in transporters from central and peripheral brain monoamines to the extracellular space. Tricyclic antidepressants are known to inhibit the transport of serotonin and dopamine in the extracellular space.
Neurotransmitters
Tricyclic antidepressants and mood stabilisers are selective inhibitors of the transport monoamines to and from the synaptic cleft. This action is attributed to:
disruption of serotonin and norepinephrine (5-HT) transporters, which would cause depletion of the monoamines in synaptic cleft
inhibition of the monoamine transporter, catecholamine transporters, which would cause accumulation of monoamines in the synaptic cleft
decrease in the receptor-binding affinity for monoamines in the synaptic cleft.
The decrease in receptor-binding affinity is due to the binding of tricyclic antidepressants to serotonergic receptors. Monoamine transporter (5-HT, noradrenaline and dopamine) receptors are known to be targets for tricyclic antidepressants and mood stabilisers.
The monoamine transporter (5-HT, norepinephrine and dopamine) receptors are also responsible for inhibiting the uptake of monoamines by presynaptic monoamine transporter (NET) system which is a critical component of the monoamine transporter system.
Catecholamine transporters
A catecholamine transporter (CAT) has also been implicated in the binding of tricyclic antidepressants and mood stabilisers possibly other monoamines to the central and/or peripheral monoamine transporters.
Norepinephrine (NE) and dopamine (Dopamine) transporters are known to be targets for tricyclic antidepressants and mood stabilisers. stabilisers bind to the norepinephrine and dopamine transporters, respectively. It is suspected that the activation of these transporter systems modifies their specific binding sites and thus modulates the transporters activities.
All these monoamine transporters are modulated by specific receptor-binding sites on the transporters and by activities of enzymes which catalyze the subsequent reactions. In particular, catecholamine transporter system is a sensitive target for tricyclic antidepressants and mood stabilisers. This system has been shown to be a site of action for some tricyclic antidepressants and may also be the site of action some novel compounds.
Dopamine transporters
The dopamine transporters are an important site of action for some novel compounds that bind to the dopamine transporter. action of tricyclic antidepressants on these transporters may be related to their ability reduce.
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