Kdem said:
Lorne??? said:
Kdem said:
Lorne??? said:
Kdem said:
I'm sorry about dropping off the thread, to be honest,(and between you and I) I ran out of my own K-pins, so I was out of action for a while. I've had the back for a week, but it takes me a couple of days to regain my strength, and even then I just want to eat and sleep for a few days.
I have looked though, but my internets off, so having to use phone. I'll get back to ya, if I find anything. So far, nothing particularly useful, except most of the more "scientific" sources still list it as low-intermediate, despite the numbers.
Is clono the only Benz you are interested in???
Hi. My response is a bit late, isn't it ? I'm not used to logging in frequently, I tend to watch the threads.
I'm mostly interested in clonazepam. Although, if you have some comparative information about other benzodiazepines (diazepam for example) vs. clonazepam and their relative affinity for the GABAA subunits or affinity for areas of the brain (for example, diazepam seems to accumulate in particular in the thalamus and a few other areas source:drug(s?)bank.ca )that would be nice !
It is an old drug, in my country introduced in the early 1970s. I even emailed the local Roche affiliate. They had very little information. 'the drops are absorbed slightly faster than the tablets'. That's about all they got.
And how does clonazepam distribute in the body ? I found some data, mostly animals/post mortem.
I had a full response but my inbox was full...
Anyway, check this link:
http://www.grindfactor.com/Forum/sh...-to-talk-about-Pharmacology&p=42236#post42236
It contains binding affinities for several benzodiazepines, both common and uncommon(like flunitro and Etiz). Of course, Clono has the highest affinity at 1.8. But some of the numbers don't add up, I mean alprazolam at 20nm??? But it is certainly worth checking out.
Hi, do you have a source for that ?
Alprazolam, that doesn't seem right.
And according to that, diazepam would be four times more potent than clonazepam. Simply not true.
I have seen 'potency' values fo triazolam and clonazepam that were nearly equal.
I don't know if that was Ki. Sometimes other values are used. Like 'mu' (where do I find those greek letters on my keyboard...) 'mu'mol on this forum.
Yeah, Alrazolam at 22nm(presumably) makes little sense, Clonazepam at 1.2 seems about perfect. But remember, it is far more complicated than Ki values. Morphine's affinity is at least 5x higher than oxycodone, yet it is maybe slightly more potent IV.(oral is different, Oxy has a better oral BA, at least under normal circumstances. And Valium has a low affinity, Lorazepam's was actually pretty, IIRC, and I think Nitrazepam was in between.
But Xanax has better solubility, and penetrates the BBB faster. Just like oxycodone, which has much better solubility than morphine, so it's faster acting.
In terms of subunits, ClonaZepam binds tightly of course, but I'm fairly certain it has some selectively for the Alpha 3 and (?) 1 subunits. Explaining it's very powerful anti convulsant effects. Diazepam is very fast acting, but has a modest affinity, and short duration, despite it and K-pins having about the same T1/2.
Distibution, Klonopin has poor to intermediate lipid solubility, lending it a delayed onset, but an extended duration of action. But it typically takes 2-3 days for it to reach max effect.
Sorry for long delay, I've had seizures, and a serious problem w/ benzodiazepines myself. I thought I found a copy with 5 binding affinities and basic info, but eh.
I'm here though, this kind of thing fascinates me, and I can explain at least some oddities
(Example, Clono and Lorazepam have the poorest lipid solubility among the common benzodiazepines, hence delayed onset and extended duration.)
But I want to convince the mods to lower Oxy's BA, multiple studies put it at or around 50%, the "Mega-Thread" info is outdated.
But please, text if you/can want to, sorry again for the delay
