Any way to tell what, if any, in vivo activity something will have?

[fastandbulbous]

^ Is it? I never noticed any opioid effect in my days of abusing it (fencamfamine - courstesy of Aldrich, when they would still deal with me), just plain (well actually special!) stimulation

 

[vecktor]

^ Is it? I never noticed any opioid effect in my days of abusing it (fencamfamine - courstesy of Aldrich, when they would still deal with me), just plain (well actually special!) stimulation

I didn't note any subjective opioid effects either, so I am guessing that it must be a downstream effect, I haven't got affinity data at mu for it, but it isn't a million miles from the required structure,

Pharmacol Biochem Behav. 1995 Jan;50(1):35-40. Related Articles, Links
Click here to read
Reinforcing properties of fencamfamine: involvement of dopamine and opioid receptors.

Planeta Cda S, Aizenstein ML, DeLucia R.

Departamento de Principios Ativos Naturais e Toxicologia, Faculdade de Ciências Farmacêuticas, UNESP, Araraquara, Brazil.

Fencamfamine (FCF) is a psychostimulant classified as an indirect dopamine agonist. The conditioning place preference (CPP) paradigm was used to investigate the reinforcing properties of FCF. After initial preferences had been determined, animals were conditioned with FCF (1.75, 3.5, or 7.0 mg/kg; IP). Only at the dose of 3.5 mg/kg FCF produced a significant place preference. Pretreatment with SCH23390 (0.05 mg/kg; SC) or naloxone (1.0 mg/kg; SC) 10 min before FCF (3.5 mg/kg, IP) blocked both FCF-induced hyperactivity and CPP. Pretreatment with metoclopramide (10.0 mg/kg; IP) or pimozide (1.0 mg/kg, IP), respectively, 30 min or 4 h before FCF (3.5 mg/kg; IP), which blocked the FCF-induced locomotor activity, failed to influence place conditioning produced by FCF. In conclusion, the present study suggests that dopamine D1 and opioid receptors are related to FCF reinforcing effect, while dopamine D2 subtype receptor was ineffective in modifying FCF-induced CPP.

http://www.ncbi.nlm.nih.gov/sites/entrez?cmd=Retrieve&db=PubMed&list_uids=7700952&dopt=Citation

 

[hussness]

^I'm currently searching for a pharmacological mechanism to explain these findings. Is it possible that naloxone has affinity for non-opioid receptor systems which could have blocked the FCF locomotor activity and CPP?
I read the study and unless I missed something, it doesn't state whether or not rats continued to self-administer FCF under conditions that block hyperactivity and CPP. Is self-administration equivocated to CPP in this case?

 

[LuxEtVeritas]

The effect of naloxone on spontaneous and evoked dopamine release in the central and peripheral nervous systems
Authors: Feigenbaum J.J.; Howard S.G.

Source: Life Sciences, Volume 59, Number 24, 8 November 1996 , pp. 2009-2019(11)

Publisher: Elsevier

A number of studies have reported that the opiate antagonist naloxone (NX) inhibits behaviors dependent upon central dopamine (DA) release.

 

[blase deviant]

I've always wondered how Shulgin knew how much to dose when he was dealing with a completely new chemical.

 

[LuxEtVeritas]

i believe he usually would go off a SAR relationship hypothesis and then start well below even the low end of what the theoretical range should be

that is really the only way to play it, though even with such one can potentially get in trouble

 

[bigmac74]

i believe he usually would go off a SAR relationship hypothesis and then start well below even the low end of what the theoretical range should be

that is really the only way to play it, though even with such one can potentially get in trouble

Yes, I have heard Ann say that he would always start with an extremely small dose and work his way up... Although arguably he didn't go high enough with some of the compounds and their activity is still a mystery to many of us.

 

[Aidan of TCC]

I've always wondered how Shulgin knew how much to dose when he was dealing with a completely new chemical.

It used to amaze me, too, but if you have the right kind of mind (I'd hate to be an organic chemist who wasn't a visual thinker), then you start picking up on the patterns after a while.

I'd go so far as to say being an intuitive visual thinker is more important than formal knowledge of chemistry. If that's how you think, then just devote a lot of time to analyzing the chemical structure of psychoactives and the receptors they act on. You'll start to see the patterns.

 

[hussness]

^Chemical similarity is only a starting point for inferring a possible pharmacological relationship between drugs. Equivocating the two can be very dangerous. I would even go as far as to say that Shulgin's self-experimentation is not particularly smart in relation to preservation of health. However, the guy is almost 80 years old. If I was of that age I would much more readily take certain risks -- you have to go sometime.

The effect of naloxone on spontaneous and evoked dopamine release in the central and peripheral nervous systems
Authors: Feigenbaum J.J.; Howard S.G.

Source: Life Sciences, Volume 59, Number 24, 8 November 1996 , pp. 2009-2019(11)

Publisher: Elsevier

A number of studies have reported that the opiate antagonist naloxone (NX) inhibits behaviors dependent upon central dopamine (DA) release.

If you have access to this article could you pm me?

 

[fastandbulbous]

i believe he usually would go off a SAR relationship hypothesis and then start well below even the low end of what the theoretical range should be

that is really the only way to play it, though even with such one can potentially get in trouble

See the entry on DOT/Aleph-1 and not what the first dose of it he took was compared with it's eventual active dose.

Better safe than sorry (as Albert Hoffman found out, thinking 250ug of LSD would be a mild/threshold dose!)