Phase II depression

of abuse, while not enough means that the agent is essentially an SNRI. Perhaps the desirable profile is the robust inhibition of SERT and the substantial inhibition of NET, like the known SNRIs, plus the addition of 10-25% inhibition of DAT. Some testing suggests that dopamine reuptake inhibition also increases acetylcholine release, so TRIs may modulate a fourth neurotransmitter system and act as multitransmitter modulators (Stahl 2008a). Further testing will determine whether TRIs will represent an advance over SSRIs or SNRIs in the treatment of depression.

Novel Serotonin Targets (Serotonin Agonists and Antagonists)

A large number of novel serotonin targets are in testing and are listed in Table 2 (Stahl 2008a). One particularly interesting novel serotonin target is the 5HT2C receptor. Blockade of 5HT2C receptors causes the release of both norepinephrine and dopamine, which is why these agents can be called norepinephrine dopamine disinhibitors (NDDIs). The novel antidepressant ► agomelatine combines this property of 5HT2C antagonism with additional agonist actions at ► melatonin receptors (MT1 and

Antidepressants: Recent Developments. Table 3. Antidepressants in development: novel sites of action.

Novel mechanism


Development stage

Beta 3 agonism


Phase III discontinued

Neurokinin (NK) 2 antagonism

Saredutant (SR48968)

Phase III discontinued

NK2 antagonism

Was this article helpful?

0 0
Anxiety and Depression 101

Anxiety and Depression 101

Everything you ever wanted to know about. We have been discussing depression and anxiety and how different information that is out on the market only seems to target one particular cure for these two common conditions that seem to walk hand in hand.

Get My Free Ebook

Post a comment