SSRI selectively blocked the reuptake of 5HT through their
inhibiting effects on the Na+/K+ adenosine triphosphatase
(ATPase) dependant carrier in presynaptic neurons.
A standard TCA such as amitriptyline, which has about an
equal tendency to block neuronal reuptake of 5HT and
norepinephrine, Fluoxetine in 200 times more selective in
blocking the reuptake of 5HT than of norepinephrine. Florentine
is approximately 4 times as potent as 5-HT reuptake inhibitor in
vito as is amitriptyline and paroxetine is approximately 80
times as potent an inhibitor as amitriplyline.
Of the five available SSRI's, paroxetine and citalopram
appear to be the most potent 5HT uptake blockers. The reuptake
blocking properties of the SSRI's enhance general serotonergic
tone in at least two distinct steps. Initially the SSRI's
contribute to a significant increase in the availability of 5HT
in the synaptic cleft.
Serotonin (5HT) interacts with multiple brain receptors.
Three receptors subtype to influences a wide range of behaviors.
There main families of 5HT receptors (5HT, 5HT2, 5HT3) have been
described which differ in their binding affinity for selective
ligands their receptor effectors coupling mechanism and the
behavioral processes they regulate. Manipulation of several
different %HT receptor subtypes (5HT1A, 5HTIC, 5HT2 and may
produce anxiolytic effects; 5HTIA and 5HT2 receptors maybe
involved in the etiology of major depression and the therapeutic
effects of antidepressants treatment. 5HT3 receptors have been
linked to reward mechanisms and cognitive processes. These
advances offer therapeutic possibilities, the ...
... middle of paper ...
...ogy. By: PJ, Coen. National Library of Medicine
Pub Med. Br. J Psychiatry Suppliment, Sept1991, Vol. 12, p7-14.
Effects of Fluoxetine on Dpoamine D2 receptors in the human
brain: a positron emission topography study with [11c] recopied.
By: Aalto J; Hietala J; Hirvonen J; Illonen T; Kajander J;
Nagren K; Penttila J; Syvalahti E. National Library of Medicine
Pub Med. Int J. Neuropsychopharmacol, Dec7,2004, Vol. 4, p431-
Systemic Uptake inhibition Decreases Serotonin release via
Somatodendritic Autoreceptor Activation. By: Auerbach, Sidney B;
Gundalah, Christine; Rutter, John J. M. Wiley Inter Science on-
line, 1995, Vol.20, Issue 3, p225 to 233.
Fluoxetine: an update of its use in major depressive
disorder in Adults. By: Gourion, D; Perrin, E; Quintin, P.
National Library of Medicine Pub Med. Encephale, 2004Jul Aug30;
4: p392 to 399.
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