BreakingBad89
Greenlighter
- Joined
- Jul 2, 2012
- Messages
- 4
Hello to all ... I often read on this and other forums that 5HT2A/2C receptors are down-regulated by both agonists and neutral antagonists. I was then looking for a neutral antagonist, but I see that the only is agomelatine and i'm not like it because it is an agonist of melatonin.
Still trying to find, however, the studies that collide with the fact of the downregulation and upregulation by antagonists and inverse agonists regard, the 5-HT2c receptor.
for example the fact that the mianserin is an inverse agonist and the antagonist eltoprazine is silent, but in chronic the first downregulates the 5-HT2C receptors (on anxiolytic action) and the second upregulates them.
http://www.ncbi.nlm.nih.gov/pubmed/7813563
then find that the sertindole (inverse agonist) decreases the affinity for agonists but not antagonists
http://www.ncbi.nlm.nih.gov/pubmed/11594443
and finally I find this study, which states that the inverse agonists under-regulate the receptor, whereas antagonists do not!
http://www.ncbi.nlm.nih.gov/pubmed/7909313
clarification? I wondered also if the mirtazapine also has the effect of reducing the 5-HT2C receptors ... on paper it looks perfect for my purposes except for the question that may upregulate the 5-HT2C receptors (which is not a good thing for me). about the mianserin have confirmation that it decreases the 5-HT2C receptors?
Still trying to find, however, the studies that collide with the fact of the downregulation and upregulation by antagonists and inverse agonists regard, the 5-HT2c receptor.
for example the fact that the mianserin is an inverse agonist and the antagonist eltoprazine is silent, but in chronic the first downregulates the 5-HT2C receptors (on anxiolytic action) and the second upregulates them.
http://www.ncbi.nlm.nih.gov/pubmed/7813563
then find that the sertindole (inverse agonist) decreases the affinity for agonists but not antagonists
http://www.ncbi.nlm.nih.gov/pubmed/11594443
and finally I find this study, which states that the inverse agonists under-regulate the receptor, whereas antagonists do not!
http://www.ncbi.nlm.nih.gov/pubmed/7909313
clarification? I wondered also if the mirtazapine also has the effect of reducing the 5-HT2C receptors ... on paper it looks perfect for my purposes except for the question that may upregulate the 5-HT2C receptors (which is not a good thing for me). about the mianserin have confirmation that it decreases the 5-HT2C receptors?
