Never actually tried it, (IDRA-21) but I can tell you a few things about it.
AFAIK its of moderate potency at the biological target. It is an AMPAkine, a benzothiadiazine derivative,..now where have I heard that before. Ahh yes. Cyclothiazide. One of the thiazide diuretics. They later discovered it was a noncompetitive GABAa antagonist and an AMPAkine, acting on AMPAr desensitization (AMPAkines act via more than one mechanism at AMPARs, some reduce desensitization and some affect channel open time or open frequency)
I don't know if IDRA-21 has any GABAa antagonist activity though. But...I do wonder if it passes the BBB. I contemplated cyclothiazide myself as a potential fix/aid for my memory/cognitive issues, until I found out that it doesn't cross the BBB in humans, and in any case if it did, it would have aforementioned GABA antagonist effects.
hxxp://molpharm.aspetjournals.org/content/62/3/566.long
Effects of 5?-Alkyl-Benzothiadiazides on (R,S)-?-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid (AMPA) Receptor Biophysics and Synaptic Responses
doi: 10.1124/mol.62.3.566
Molecular Pharmacology September 1, 2002 vol. 62 no. 3 566-577
This has relevance to the pharmacology of AMPAkines as a whole, and in particular, benzothiadiazide derivatives.
IDRA-21, according to this paper lacks the peripheral effects (read, diuretic etc.) and hasn't shown neurotoxic properties in vivo in animals.
Some analogs of IDRA-21 are discussed, with a view to attaining higher potency and other such things, and it appears that in some at least, there is more than one mode of action present as regards potentiation of fluorowillardiine activation of AMPARs (5-halowillardiine derivatives are glutamate direct agonists at the ionotropic receptor types, E.g the fluorinated derivative targets AMPA receptors, IIRC the iodo-substituted willardiine , the halogen substituent present has very significant effects in determining the receptor target and selectivity over other ionotropic glutamate receptors, NMDA, AMPA and kainate. AFAIK they either do not effect either delta1, delta2 or chi-1 type iGLuRs or have not been tested. (not sure if chi-type ionotropic glutamate receptors are expressed in humans, they are expressed in rats, and appear to be present mainly during development)
Seemingly currents are prolonged by a means other than blockade of desensitization by some IDRA-21 analogs, which whilst not explicitly stated in that paper, could be the case for IDRA-21 itself.
IDRA-21 IS active in vivo in the rat at least. But that does not mean that it will be in humano. Cyclothiazide is a potent convulsant in several animal species, but in humans can be safely used as a diuretic, because of its lack of BBB permeability.
Gah..I could do with some right now, at least, if it does pass the human BBB. Thanks to the filth stealing my pramiracetam, my memory function has gone straight down the pan. Was looking at the structure of cyclothiazide and IDRA-21 in two seperate wiki pages, and couldn't hold the structure in memory long enough to be able to compare the differences, even just the skeletal structure diagram.
Wish I could get some help with it, but nobody will do anything, seen memory specialists, and all they are willing to do is keep re-testing memory function. I already fucking KNOW it doesn't work and that my executive functioning is shot to shit. Couldn't remember the greek letter prefix for the ionotropic glutamate receptor type with 2 known subtypes, had to go through the greek alphabet letter by letter searching, excluding a few I knew were not right. Fucking fed up of this. So, so SO fucking fed the fuck up.
If it wasn't for the fact that other than stealing my pramiracetam, they also stole his propionyl chloride, benzoyl chloride and threw the piperazine on the floor, then he would have got off his arse, executive difficulties or no, and likely had one of the most potent of the AMPAkine drugs, sunifiram, within a few days at most, sunifiram/DM-235. (1-propionyl-4-benzoylpiperazine)
Not as if the pigs have the intelligence to realize that those three reagents were the ones needed for that particular synthesis, but it does seem selective. Unless of course, they went through his literature either while he was in the pig shop, or during previous search/burglaries when his computer was stolen by them.
