N&PD Moderators: Skorpio
Benzomorphans arn't too weak
haribo1
Ex-Bluelighter
the trans-5,9-diCH3 (beta) isomer is where most of the potency lies.
Metazocine X=CH3 , Y=OH = 1/5 x morphine
Pentazocine X=allyl , Y=OH = 1/5 x morphine
Phenazocine X=phenylethyl. Y=OH = 4 x morphine
Thiazocine X=2 thienylethyl Y=OH = 8 x morphine
Cyclazocine X=methyl cyclopropyl Y=OH = 10 x morphin
8-CAC X=methyl cyclopro Y=CONH2 = 12 x morphine
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Jabberwocky
Frumious Bandersnatch
man haribo this hobby of yours is time consuming, isn't it?
Ham-milton
Bluelighter
Maybe not weak, but are any of those listed pure mu agonists? How many are stronger kappa agonists than mu?
fastandbulbous
Bluelight Crew
^ Those potencies are just from Straub tail flicck analgesic testing. What pentazocine: 1/5th morphine potency doesn't tell you is that it's possible to get lost in your own bathroom (and it's not a nice feeling by any stretch of the imagination).
About the only one I'd touch with a 10' pole is metazocine as all the others have too much of the weirdness factor about them (mostly due to kappa agonism, but some go for the sigma and/or NMDA receptor as well)
theWorldWithin
Bluelighter
psychedelic opiates perhaps, sounds like a group of winners to me. Could this manifest itself as a non-dysphoric property or are we talking a bad getting lost kappa agonism?
Swerlz
Bluelight Crew
everytime i hear kappa agonism.. Salvia comes to mind and instantly say fuck that
Jabberwocky
Frumious Bandersnatch
^ isn't salvia just an agonist to one type of kappa receptor?
Ham-milton
Bluelighter
I can't thinhk of any kappa agonists that don't result in getting lost or mind-fucked.
negrogesic
Bluelight Crew
I would imagine that a number of these benzomorphans have at least a weak affinity to the sigma receptor, which when combined with kappa affinity, certainly makes dysphoria a very real possibility...
8-CAC is probably the most promising of these; it has a significantly lower affinity to the kappa receptor than cyclazocine yet a higher affinity for the MOR...
But of course we all know that potency does not = potential...
I never enjoyed talwin.
haribo1
Ex-Bluelighter
phenazocine has been used medically. It's much more selective to the mu receptor so an active dose has no sigma/delta effects.
I would guess the N 2-thienylethyl would be the best of the lot, it's 20x morphine and not controlled. If normetazocine (or whatever the N-H version is called) then it should be makable...
Ya, I also have never heard of a kappa agonist opioid being enoyable to the majority of people.
Wont these also be mixed agonist/atagonists as well, thus being more or less useless to people who are dependent on opioids because of the risk of precipitated w/d? I know Pentazocine is ussually mixed w/ naloxone, but I think it is a mixed agonist antagonist by itself also.
(Edit:missed holy_cow's post mentioning this)
haribo1
Ex-Bluelighter
The kappa agonism of phenazocine is also very low. I would venture to sat that the amide on 8-CAC can make this class much more mu specific. I'm looking for the papers right now, but some people managed to make the amide version of phenazocine and it was a full agonist 80x morphine, i.e. fentanyl potency. Also, in the UK, only metazocine, pentazocine & phenazocine are legally controlled...
getreal
Bluelighter
You're telling me!!
samadhi_smiles said:
morphiquet
Bluelighter
the above structure of benzomorphans has 2 mistakes:
the y-substituent is in the wrong position and the bond between the n-atom and the tetraline-skeleton is also in wrong position.
besides that, the amido-version has caught my attention, it remembers me of another class of mu-agonists which are derived by dealkylating some delta-receptor-agonists ( e.g. RWJ-394674 )
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haribo1
Ex-Bluelighter
^Whoops, my bad. I drew it from memory... from memory.... errmmmmm.....
Yes, the amido versions contain some plenty powerful members. I remember that they tried doing the same to the 3 -OH in morphine. In that case it turned out to be a total loser. Apparently the -OH is the main place that morphans and benzomorphans are metabolized, so the amido solves the problem. I seem to remember that they got phenazocine from 3-4 hours up to 12 hours +...
I also clearly remember that in the benzomorphan class (and many others) replacing the -OH for an -NO2 increases activity. I will look for some examples right now...
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fastandbulbous
Bluelight Crew
CH3CH2OH said:
I actually like the effects salvia produces as lomg as you don't smoke a massive dose. Pentazocine on the other hand, I've never found pleasurable. When it comes to anything other than the 4-phenylpiperidine based opioids, I personally have severe misgivings about anything attached to the heterocyclic nitrogen other than a methyl or arylethyl group (anything with a cyclopropyl ring or a double bond - which you can imagine as a two membered ring - I will avoid like the plague!)
lysergication
Bluelighter
Sorry if it's a bit offtopic, but there some things I don't really understand about the properties of effects linked with the KOR agonists :
Is the weirdness of salvinorin a a "classical weirdness" of the KOR agonists (the same kind you'll experience if you take (-)-pentazocine) that makes it not enjoyable for the majority of people ?
I mean if someone find salvinorin a very interesting, is there a chance that he will enjoy other KOR agonist as well (the kind that is not enjoyable by the majority) ?
Also, when researchers speak about dysphoria mediated by the KOR agonism, are they speaking about this weirdness or it's pure dysphoria (opposite to euphoria) and if it is, why don't we experience this dysphoria with salvinorin a ?
F&B, if you don't enjoy large dose of salvinorin a, what makes you think you'll enjoy metazocine ?
