Hypothetical Drug

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Mode of action
Hypothetical Drug
Transporter zone
Important for clinical effects
Important for clinical effects
Enzyme zone
No interaction
Receptor zone
Contributes to other effects
Contributes to other effects
Important for clinical effects
Contributes to other effects
Ion channel zone
No interaction
Description

In the figure above, the yellow circle around the name indicates that drug is a multimodal drug – i.e. one whose clinical effects are thought to be mediated by actions on two or more different types of targets. Only target interactions that occur at pharmacological concentrations relevant to therapeutic actions are shown.

It has affinity for both noradrenaline and serotonin transporters.

As the noradrenaline symbol is above the serotonin one this tells us that the drug has higher affinity for the noradrenaline transporter. Both symbols are filled which tells us the drug blocks both the serotonin and noradrenaline transporters

The drug also interacts with a number of receptors; the position of these receptors is in order of affinity with histamine H1 receptor the highest at the top. The filled symbol tells us it is an antagonist at this receptor. The dotted line explains that this action is not considered relevant for the antidepressant effect observed in animal models.

The next highest affinity of the drug is at dopamine, and the open circle indicates that it is an agonist, but the dotted lines indicate that this action is not considered relevant for the antidepressant effect observed in animal models.

The drug has affinity at the 5-HT2 receptor, where it is a partial agonist. The solid line tells us that this is considered relevant.

The drug also has lower but still antagonist activity at the acetylcholine muscarinic M1-4 receptors. The dotted line explains that this action is not considered relevant for the antidepressant effect observed in animal models.

In animal models the actions on the noradrenaline and serotonin transporters and the 5-HT2 serotonin receptor subtype may explain the drug effect in animal models of depression.

 

Please notice that Caution should be applied when extrapolating animal data to humans.

Detailed and Approved Information on the clinical use of the compounds can be found at the homepage of EMA or at Martindale.

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