Hammilton
Bluelighter
- Joined
- Sep 2, 2008
- Messages
- 3,435
I've meant to start this thread for a long time, because there have been a lot of threads on various old depressants, but they're all either in singles or doubles- and I don't think we've remotely run out of old depressants to discuss.
Of course, though, limiting yourself to discussion of the old drug isn't good, but discussions of LOGICAL variants of the old drugs should be in here too.
To start the discussion, I want to talk about a drug called propanidid, which was taken off the market because of allergic reactions, though today it is believe to have been due to a component of the product, not propanidid itself.
The structure reminds me dimethocaine, actually. Too short acting to have any da reuptake inhibiting effects, though. A strange symmetry, too. It's interesting that it has analgesic effects too. Most GABAergic depressants don't reduce pain, and many actually produce hyperalgesia, which makes this so interesting.
I know it has effects on the GABA-A receptor, but I don't know where it binds.
This is very interesting, but I don't know what to make of it. I wouldn't and still don't think that opioid receptors are very involved in the sedation produced by GABAergics, but apparently, at least in the transfer from consciousness to unconsciousness, for some, they are. I don't understand why drugs effecting the same receptor would have different downstream effects. I mean, they both cause the chloride channel to stay open longer or open more frequently, and there's no obvious split between those that cause it to open more often and those that cause it to stay open longer.
Any explanation?
I think the biggest goal with propanidid would be to produce a longer acting analogue. I believe it has a plasma halflife of .2 hours, or 12 minutes. That seems in line with it's ultra-short effect. Great for anaesthesia where you want the person to come out quickly, not so great for abuse. Depressant crack sounds interesting, but it's a bad idea.
I think at least a 30 minute half life would be required, but 60 minutes would probably be best. At least, imho, anyway. I like a depressant that hits rapidly and is over in 1.5 or 2 hours. A 60 minute half life should be good for that. It's hard to predict though.
Of course, though, limiting yourself to discussion of the old drug isn't good, but discussions of LOGICAL variants of the old drugs should be in here too.
To start the discussion, I want to talk about a drug called propanidid, which was taken off the market because of allergic reactions, though today it is believe to have been due to a component of the product, not propanidid itself.
The structure reminds me dimethocaine, actually. Too short acting to have any da reuptake inhibiting effects, though. A strange symmetry, too. It's interesting that it has analgesic effects too. Most GABAergic depressants don't reduce pain, and many actually produce hyperalgesia, which makes this so interesting.
I know it has effects on the GABA-A receptor, but I don't know where it binds.
This is very interesting, but I don't know what to make of it. I wouldn't and still don't think that opioid receptors are very involved in the sedation produced by GABAergics, but apparently, at least in the transfer from consciousness to unconsciousness, for some, they are. I don't understand why drugs effecting the same receptor would have different downstream effects. I mean, they both cause the chloride channel to stay open longer or open more frequently, and there's no obvious split between those that cause it to open more often and those that cause it to stay open longer.
Any explanation?
I think the biggest goal with propanidid would be to produce a longer acting analogue. I believe it has a plasma halflife of .2 hours, or 12 minutes. That seems in line with it's ultra-short effect. Great for anaesthesia where you want the person to come out quickly, not so great for abuse. Depressant crack sounds interesting, but it's a bad idea.
I think at least a 30 minute half life would be required, but 60 minutes would probably be best. At least, imho, anyway. I like a depressant that hits rapidly and is over in 1.5 or 2 hours. A 60 minute half life should be good for that. It's hard to predict though.
