Benzazepine Stimulants, eg. 6-Br-APB, SKF-81,297, SKF-82,958

[matthewmillett]

I've been searching for information about the use of these Benzazepine Stimulants in humans but so far have been unable to find anything.

I am interested in these 3, 6-Br-APB, SKF-81,297, SKF-82,958

They are all legal and here is an excerpt from wiki,

"(R)-6-Br-APB and similar D1-selective full agonists like SKF-81,297 and SKF-82,958 produce characteristic anorectic effects, stereotyped behaviour and self-administration in animals, with a similar but not identical profile to that of dopaminergic stimulants such as amphetamine."

From what I have read, 6-Br-APB, well atleast the (R)-enantiomer is a D1-selective full agonist, while both SKF-81,297 and SKF-82,958 are selective D1/D5 receptor full agonists.

Do those who have knowledge, think these could make for suitable stimulants for humans?

6-Br-APB

SKF-81,297

SKF-82,958

 

[effie]

I am going to move this to advanced drug discussion - hope that is okay.

BDD > ADD

(ADD mods - let me know if this is not appropriate for your forum!)

 

[atrollappears]

I think DA agonists are not used recreationally because they can cause intense nausea. I don't know which receptors mediate that though.
Update: Looks like it's D2, so these compounds could be pretty interesting.

 

[sekio]

As far as I know these are not used anywhere but research.

I expect these drugs would be comparable to the strong pure DRI's - more of a compulsion/psychosis inducer than a functional stimulant.

I remember Jamshyd did a trial on bromocriptine, a D1/2 agonist, and found it was less than desireable as a stimulant.

Play carefully with these, kids.

 

[matthewmillett]

could you make any comparision to say methamphetamine? would you say same ball park?

I understand if it is not possible to answer such a question

Thanks everyone for their reply's too

 

[sekio]

This class of drugs is so far away from amphetamines... it's not even close.

The analogy would be (for the serotonin system): compare LSD (direct receptor agonist) to citalopram (reuptake inhibitor) or MDMA (release agent) ... the three drugs are totally different in terms of their effects and do not neccesarily substitute for each other.

The benzazepines are basically the "LSD of stimulants" - they tickle the recptors directly by mimicking dopamine. Most known stimulants to date (methylphenidate, cocaine, amphetamines) instead work by increasing the levels of natural dopamine which then goes on to stimulate receptors.

I have not ever seen human trials of these, and I expect that they wouldn't share the same effects as "traditional" stimulants.

 

[atrollappears]

The analogy would be (for the serotonin system): compare LSD (direct receptor agonist) to citalopram (reuptake inhibitor) or MDMA (release agent) ... the three drugs are totally different in terms of their effects and do not neccesarily substitute for each other.

That's not necessarily a fair comparison. The effect of LSD which is not mimicked by serotonin releasing agents/reuptake inhibitors is caused by activation of the arachidonic acid signaling pathway through the 5-HT2A receptor, which is not activated by serotonin. Conversely, serotonin activates the inositol triphosphate signaling pathway which is not activated by LSD. The D1 receptor does display functional selectivity, but whether or not these compounds activate the receptor similarly to dopamine is up in the air.

I expect these drugs would be comparable to the strong pure DRI's - more of a compulsion/psychosis inducer than a functional stimulant.

I remember Jamshyd did a trial on bromocriptine, a D1/2 agonist, and found it was less than desireable as a stimulant.

Is it possible that D2 activation limits the recreational potential of these? IIRC the D2 receptor is the one associated with psychosis.

 

[atrollappears]

ketamin is a d2-agonists, and its highly recreational.

Is it? Learn something new every day
But still, that's a way different method of action, and a way different desired effect. The psychotomimetic effect of the D2 receptor might even add to the desired effect of ketamine.
Clearly D2 activation doesn't immediately extinguish the recreational potential of any substance (or else coke and amph would be pretty lame), I was just noting the possibility that it puts a damper on the effects of selective D1 activation, in which case these compounds might be viable stimulants, and the data from animal studies would be more easily explained.

 

[Epsilon Alpha]

ketamine is dirty as all hell in what it does, but recreational.

Fixed
But, with virtually every drug that is recreational it does a lot more than selectively increase a random monoamine or bind to a single receptor. There's generally a bizarrely complex interplay going on along side it to prime the brain for "hey this is f*cking awesome" mode.

Of course some pathways trigger downstream pathways that leads to the indirect activation of these "priming" pathways, but there's a very interesting changes in them with "tolerance"
I'll keep the science rant downplayed till I uber-bump the amp thread I've got going.

Needless to say, ketamine does a lot of indirect stuff to make itself recreational. Which is also why it has such a fucked up tolerance profile from what I've read.
But, keeping my "half a flat of rockstar" fueled rant on topic: these drugs aren't too well characterized so who knows everything they'll do in vivo

 

[matthewmillett]

This is interesting,

"Rhesus monkeys with chronic intravenous catheters lever pressed on a fixed-ratio 10 schedule maintained by a base-line cocaine dose of 0.03 mg/kg/inj in daily 1-hr sessions. Periodically, D1 agonists were substituted for the cocaine base-line. All monkeys (n = 4) self-administered the high-efficacy D1 agonists SKF 81297, SKF 82958 and R(+) 6-Br-APB at rates above those maintained by vehicle; therefore, each of these compounds functioned as a positive reinforcer (maxima: SKF 81297: 55-172 inj/hr, 0.01 mg/kg/inj; R(+) 6-Br-APB:103-165 inj/hr, 0.001 mg/kg/inj; SKF 82958: 110-149 inj/hr, 0.01 mg/kg/inj)." (Pharmacol Exp Ther December 1995 275:1367-1374)

It looks like i'll be testing 6-Br-APB on myself first, as it's the most easily available. Any advice on how I should go about this is welcomed.

 

[matthewmillett]

Substitution for methamphetamine also was observed with the D1 receptor agonists, SKF 81297, SKF 82958 and dihydrexidine, and the D2 receptor agonist, (+)-PHNO in the majority of monkeys. (PMID: 9618419)

 

[sekio]

Just because a drug produces self-administration doesn't mean it's any good... e.g. MDPV.

Be careful. You shouldn't have access to the drug if you're the one testing it, esp. if the major effect is a compulsion to take more..

 

[atrollappears]

Substitution for methamphetamine also was observed with the D1 receptor agonists, SKF 81297, SKF 82958 and dihydrexidine, and the D2 receptor agonist, (+)-PHNO in the majority of monkeys. (PMID: 9618419)

Interesting. I thought most of the cue for amphetamines was actually produced by NE release.

Just because a drug produces self-administration doesn't mean it's any good... e.g. MDPV.

Be careful. You shouldn't have access to the drug if you're the one testing it, esp. if the major effect is a compulsion to take more..

This is definitely true. If you do this, realize that you are being a guinea pig.

Are you getting are you getting R, S, or racemate?

 

[matthewmillett]

I have decided not to pursue this anymore, I've decided even if I can get legal substaces I don't want to be using drugs

Thanks everyone for their reply's btw