Posted by Brainbeard on September 25, 2009, at 14:52:41
In reply to Lets discuss cyproheptadine (Periactin)! Linkadge?, posted by ed_uk on June 29, 2005, at 10:32:50
I'm interested in cyproheptadine because of its 5HT2A/C-antagonism, which indirectly boosts dopamine and noradrenaline, as well as promoting deep stage sleep and having anxiolytic effects.
I've been looking on the internet for quite some time to find its binding profile. Eventually, I found this: http://docs.google.com/gview?a=v&q=cache:2UDBSpj0PeQJ:www.lycaeum.org/research/researchpdfs/3722.pdf+Young+binding+profile+of+cyproheptadine&hl=nl&gl=nl&sig=AFQjCNHDjW8WDAk-kS6JbhJpXCF747qf_A
According to this study, cyproheptadine's 5HT2-antagonism is in the same range as its antimuscarinic and antihistaminergic properties, which is roughly a receptor affinity of 5 Ki (the lower the Ki value, the higher the affinity). The Ki for 5HT2A receptors is about 20 times higher than the Ki for 5HT2C receptors (http://www.google.nl/search?hl=nl&safe=active&client=firefox-a&rlz=1R1GGIC_nl___NL345&q=Ki+cyproheptadine+5-HT2A+5-HT2C+receptors%22&btnG=Zoeken&meta=, see text of first search result.)
This would mean that cyproheptadine is a weaker antihistaminergic than amitriptyline, but a stronger 5HT2A-antagonist. Which makes it quite an interesting drug, in my opinion.
poster:Brainbeard
thread:521042
URL: http://www.dr-bob.org/babble/20090921/msgs/918463.html