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For example, in states of anxiety and depression the following presynaptic changes are thought to occur:
For example, in states of anxiety and depression the following presynaptic changes are thought to occur:
{| class="wikitable"
|-
! !! α2-Adr-autoreceptor !! α2-Adr-heteroreceptor !! 5-HT<sub>1A</sub>-autoreceptor
|-
| || Nor-adrenergic neuron || serotonergic neuron || serotonergic neuron
|-
| Depression/Anxiety || ↑ || ↑ || ?
|-
| Clomipramine || ↓ || ↓ || ↓
|}
↓=Downregulation of receptor ↑=Upregulation of receptor
These receptors normally inhibit noradrenaline or serotonin release so down regulation of the receptors increases the release of the neurotransmitters. Postsynaptic changes also occur:
These receptors normally inhibit noradrenaline or serotonin release so down regulation of the receptors increases the release of the neurotransmitters. Postsynaptic changes also occur:
{| class="wikitable"
|-
! !! α1 Ad-R !! 5-HT2A, 2C-R !! 5-HT1A-R !! β1,2,3-R !! 5-HT4,6,7-R
|-
| Depression/Anxiety || ↓ || ↑ || ? || ↑ || ?
|-
| Clompipramine || ↑ || ↓ || ? || ↓ || ?
|}
↓=Downregulation of receptor ↑=Upregulation of receptor
The effect of these postsynaptic receptor number changes is an increase in the levels of two crucial compounds, C-amp Response Element Binding Protein (CREB) and Brain Derived Neurotropic Factor (BDNF). The end results of these presynaptic and postsynaptic changes are:
Changes in receptor numbers take several days to occur. The effect of these postsynaptic receptor number changes is an increase in the levels of two crucial compounds, C-amp Response Element Binding Protein (CREB) and Brain Derived Neurotropic Factor (BDNF). The end results of these presynaptic and postsynaptic changes are:
*Increase in serotonin in the synaptic cleft.
*Increase in serotonin in the synaptic cleft.
==Comparison of Effects and Adverse Effects for Clomipramine and Related Drugs==
==Comparison of Effects and Adverse Effects for Clomipramine and Related Drugs==
{| class="wikitable"
|-
! Drug !! Class !! 5-HT:NorAdrenaline Blocking ratio !! H<sub>1</sub> !! Ach (Muscarinic) Blockade
|-
| Amitriptyline || TCA || 1:4 || +++ || +++
|-
| Clomipramine || TCA || 5:1 || ++ || ++
|-
| Fluoxetine || SSRI || 15:1 || || +
|-
| Fluvoxamine || SSRI || 150:1 || || +
|-
| Sertraline || SSRI || 150:1 || || +
|}