Posted by CrAzYmEd on May 28, 2010, at 16:22:21
In reply to 5HT2A-antagonism + 5HT2C-agonism Would Be Ideal, posted by Brainbeard on May 28, 2010, at 15:17:55
"There is a consesnus based on clinical evidence that 5HT2A-agonism opposes the beneficial effects of unspecific 5HT-activation through serotonin reuptake inhibition (SRI)."
The opposing powers! There's allways a bad boy around counteracting the benefits of mr good guy, but then again there's mr good guy counteracting the problems the bad boys are causing!
It seems that when other receptors are either activated or inhibited, the effects of agonism of a differend receptor could be completely differend, like you say that 5HT2C antagonism could counteract the benefits of 5HT2A antagonism. So id say it depends on the situation wheter 5HT2A antagonism is good.
About your experience with SSRI's, 5HT2A agonism plays a big role in the mushroom experience too , so i wouldnt only point to 5HT2C agonism, its the whole mix, and suprisingly the pharmacological profile of mushrooms is very simular to that of lisuride except that mushrooms seem to be a strong D1 agonist too.
I'm still convinced that 5HT2A agonism is better then 5HT2A antagonism tough (in some situations atleast), 5HT2A can facilate dopamine release togheter with the 5-HT1A, 5-HT1B, 5-HT3 and 5-HT4 receptors. 5HT2A is also crucial for the dopamine release by amphetamine's and opiates while 5HT2C can inhibit it (its a weird one)
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Pharmacol Ther. 2007 Feb;113(2):296-320. Epub 2006 Oct 17.
Pharmacologic mechanisms of serotonergic regulation of dopamine neurotransmission.
Alex KD, Pehek EA.Department of Neurosciences, Case Western Reserve School of Medicine, Cleveland, OH 44106, USA.
Abstract
The neurotransmitter dopamine (DA) has a long association with normal functions such as motor control, cognition, and reward, as well as a number of syndromes including drug abuse, schizophrenia, and Parkinson's disease. Studies show that serotonin (5-HT) acts through several 5-HT receptors in the brain to modulate DA neurons in all 3 major dopaminergic pathways. There are at least fourteen 5-HT receptor subtypes, many of which have been shown to play some role in mediating 5-HT/DA interactions. Several subtypes, including the 5-HT1A, 5-HT1B, 5-HT2A, 5-HT3 and 5-HT4 receptors, act to facilitate DA release, while the 5-HT2C receptor mediates an inhibitory effect of 5-HT on DA release. Most 5-HT receptor subtypes only modulate DA release when 5-HT and/or DA neurons are stimulated, but the 5-HT2C receptor, characterized by high levels of constitutive activity, inhibits tonic as well as evoked DA release. This review summarizes the anatomical evidence for the presence of each 5-HT receptor subtype in dopaminergic regions of the brain and the neuropharmacological evidence demonstrating regulation of each DA pathway. The relevance of 5-HT receptor modulation of DA systems to the development of therapeutics used to treat schizophrenia, depression, and drug abuse is discussed. Lastly, areas are highlighted in which future research would be maximally beneficial to the treatment of these disorders.--------------------------------
I should take a look at the full paper of that study.
Will take a better look at your post tomorrow, have to get up early today, morgen weer gaan werken:p.
poster:CrAzYmEd
thread:948688
URL: http://www.dr-bob.org/babble/neuro/20100223/msgs/949290.html