GTS-21/DMXB-A
3AlarmLampscooter 08 Jul 2013
Safety, pharmacokinetics, and effects on cognitive function of multiple doses of GTS-21 in healthy, male volunteers. (PMID:12629535)
This study was designed to determine the safety, tolerability, pharmacokinetics and effects on cognitive function of GTS-21 in healthy, male volunteers. A total of 18 subjects were randomized to GTS-21 (25, 75 and 150 mg) or placebo administered three times daily (first 4 days, once on Day 5) for three, 5-day sessions. GTS-21 was well tolerated up to doses of 450 mg/day, with no clinically significant safety findings. C(max) and the area under the plasma concentration of GTS-21 and the metabolite 4-OH-GTS-21 increased in a dose-related fashion; although considerable intersubject variability occurred, it decreased with continued dosing. GTS-21 showed statistically significant enhancement of three measures of cognitive function (attention, working memory, episodic secondary memory) compared to placebo. A relationship between exposure to GTS-21 and the magnitude of the cognitive response was apparent, with maximal effect approached for doses between 75 and 150 mg three times a day. These data indicate that GTS-21 may represent a novel treatment for dementia.
Attached Files
Edited by 3AlarmLampscooter, 08 July 2013 - 04:50 AM.
Reformed-Redan 08 Jul 2013
WAY-317,538
GTS-21:
PRL-8-53
Only problem is that these seem to be partial or full agonists leading to potential downregulation or tolerance.
telight 08 Jul 2013
Yup quite interesting. Nootropic effects should be prominent as with PRL-8-53. Compare these structures:
WAY-317,538
GTS-21:
PRL-8-53
Only problem is that these seem to be partial or full agonists leading to potential downregulation or tolerance.
These structures are completely different.
3AlarmLampscooter 05 Sep 2013
I've been quoted $12,500 for a 100g synth. Works out to $3.13 to $18.75 a dose from the 25-150mg range used in clinical trials. Pricey, but I'm still possibly inclined to proceed. I'll do a bit more shopping around. That, and maybe start looking at some more simple nicotinic agonists as alternatives.
I may try sourcing some quotes for WAY-317,538, as it is supposedly "easy to synthesize", and thus probably cheap(er)
Edited by 3AlarmLampscooter, 05 September 2013 - 08:12 AM.
3AlarmLampscooter 21 Dec 2013
Anyone wanna submit quotes to their favorite labs?
formergenius 21 Dec 2013
3AlarmLampscooter 21 Dec 2013
I believe there were a few alpha7nAChR agonist requests, so perhaps you'll draw more people when you explain that this is its primary MoA.
Hah! Never even hit me that I didn't mention this in the OP! Derp.
GTS-21 = α7 Nicotinic Receptor Agonist
Also, a new paper has come out expanding on pathways of the anti-inflammatory properties of this class of drugs: http://www.ncbi.nlm....les/PMC3817544/
Overman 22 Dec 2013
Reformed-Redan 29 Dec 2013
Sry, here is the link:
http://journals.prou...064020&p_IsPs=N
Edited by yadayada, 29 December 2013 - 06:48 PM.
Reformed-Redan 29 Dec 2013
More info:
http://link.springer...1007/BF02480382
and derivatives of anabaseine:
http://pubs.acs.org/....1021/ml400278r
megatron 29 Dec 2013
Edited by Megatrone, 29 December 2013 - 10:12 PM.
scibor1 30 Dec 2013
My supplier indicated that pure anabaseine, which is the backbone of GTS-21, could more readily be provided. It's a potent agonist at the nicotinic receptors and would be maybe worth a trial?
More info:
http://link.springer...1007/BF02480382
and derivatives of anabaseine:
http://pubs.acs.org/....1021/ml400278r
Yes, yes, yes...
Beautiful information
Flex 30 Dec 2013
Here is a picture of most a7n agonists or partial agonists. If anyone could get tthrough the paywall that would be nice and label some of the compounds there. Like 19, 23. 19 looks interesting.
Sry, here is the link:
http://journals.prou...064020&p_IsPs=N
Lol, Where's Wally
Edited by Flex, 30 December 2013 - 05:25 PM.
megatron 30 Dec 2013
My supplier indicated that pure anabaseine, which is the backbone of GTS-21, could more readily be provided. It's a potent agonist at the nicotinic receptors and would be maybe worth a trial?
More info:
http://link.springer...1007/BF02480382
and derivatives of anabaseine:
http://pubs.acs.org/....1021/ml400278r
Did you get a quote for GTS-21?
What also greatly triggers my interest in this drug is that these effects were seen in humans, not just rats.
Edited by Megatrone, 30 December 2013 - 07:41 PM.
3AlarmLampscooter 31 Dec 2013
Here's the fulltext on another review that cites it, which I had access to: http://ge.tt/3UpgQvB1/v/0
There are plenty more and newer agonists/PAMs also.
Of the ones you mentioned, compound 19 is 3-{[2-(pyridin-3-yl)-3,4,5,6-tetrahydropyridin-3-ylidene]methyl}-1H-indol-1-yl and has no pubchem entry, 23 is 2,3-Dihydroindol-5-ol and looks to be a pretty potent dopamine agonist also.
Edited by 3AlarmLampscooter, 31 December 2013 - 07:14 PM.
Reformed-Redan 01 Jan 2014
http://jpet.aspetjou...jpet.113.206623
formergenius 06 Jan 2014
There's no wiki on it, but it has been tested in humans, see here. I believe YoungS is going to participate in a trial as well.
edit: If I'm not mistaken, it's also much more potent (2mg), hence even if a gram is around the aforementioned price, it would be more bang for you buck.
Edited by formergenius, 06 January 2014 - 02:22 AM.
megatron 06 Jan 2014
Edited by Megatrone, 06 January 2014 - 01:59 PM.
formergenius 07 Jan 2014
What about TC-5619?
Edited by formergenius, 07 January 2014 - 02:09 PM.