Most selective 5HT2 antagonist

[LuxEtVeritas]

what substance is the cleanest, most selective antagonist of 5HT2?
Most seem to act on dopamine and/or other pathways (antipsychotic class)

from what i have gleaned thusfar Ketanserin seems to be the most selective

...what is a typical dose of this agent>?

Pizotifen and Ciproheptadine seem fairly selective as well though aer notable antihistaminergic agents

the more obscure LY53857 and derivative seem pretty selective

 

[MattPsy]

Look toward superpotent 5-HT2A ligands that were designed as agonists but turned out not to be, maybe.
AFAIK some N-benzyl tryptamines fit this.

 

[hussness]

Are you looking for a clean way to kill a trip or doing schizophrenic research?

 

[LuxEtVeritas]

research which entails solely excising the 5HT2 component of specific molecules

i have found some interesting relatively pure antagonists after posting

 

[dorothyperkins]

Sorry its kind of a different topic but whats the most selective agonist? DO(I) maybe? I looked but couldn't find any info, would be nice to see data at several receptors for different phens/tryptamines and try and correlate it with experience reports.

Edit: ^^ cool, how do you work out the dose to exactly balance it though? sounds hard.

 

[LuxEtVeritas]

DOI is highly selective of 5HT2 over other serotonin receptors but I am not sure how selective it is in regards to other NT pathways such as DA

there also likely in the literature is more selective agents, though again many are expressed for the selective of 5HT2 over other SE receptor types

ie.,
http://pubs.acs.org/cgi-bin/abstract.cgi/jmcmar/2003/46/i19/abs/jm030205t.html

 

[Smyth]

Try looking at M1009007, although that is 5-HT2(A) receptor.

This site started by Bryan Roth is supposed to contain the Ki infomation for all psychoactive compounds: PDSP

 

[dorothyperkins]

Yeah i saw that one on google, Lux, is it much better than a,O-DMS? Possibly more evidence against the psych unified receptor theory, since the oxygen lone pair points in the other direction to that in the FLY's.

Smyth, thats pretty cool but can you get a program to parse the txt document, its impossible to read like that!

 

[LuxEtVeritas]

Try looking at M1009007, although that is 5-HT2(A) receptor.

This site started by Bryan Roth is supposed to contain the Ki infomation for all psychoactive compounds: PDSP

that compound i had looked at

the database though i did not know of so props for that link

though to note one example of something seemingly amiss is the ritanserin 5HT2 values are absent what i see as the dominant value quoted about at 0.39 (or thereabouts) with all values being given 10-fold weaker and over

(curious to the selectivity of RIT relative to its Ki at 5HT2 to what i belieev is its next highest affinity receptor D2)....

 

[Ham-milton]

that's one of those imidazolines, right?

 

[dorothyperkins]

Yeah i saw that one on google, Lux, is it much better than a,O-DMS? Possibly more evidence against the psych unified receptor theory, since the oxygen lone pair points in the other direction to that in the FLY's.

Smyth, thats pretty cool but can you get a program to parse the txt document, its impossible to read like that!

Bump! If someone can give me a list of fields in that Ki text ill have a play with getting it into access or something.

 

[Smyth]

I'm sure some of you have seen my Wikipedia files that I have been working on over the last 10 months.

The Bryan Roth paper is referenced there in the "SNDRI" section. He's actually closely allied with Kozikowski who started Acenta Discovery. Read the BR paper to get some further infos or PM me with your email if you are having difficulties accessing it.

Indeed, if somebody can get me this document then that would be a great help also.