Fertile
Bluelighter
- Joined
- Mar 31, 2022
- Messages
- 1,627
I found a source for the EC50 of fentanyl and (±) beta hydroxy fentanyl.
Wild-type μ-opioid receptor in vitro (EC50s = 38.1 and 64.9 nM, respectively).
Now in 'Opiates' by Lenz et al they state that the gamma -OH doesn't increase affinity BUT it improves transport to the receptor with (S) phenoperidine having a duration some x7 the (R). I got to wondering - with such short duration opioids, will those really short durations seemingly affect potency simply because the drug isn't transported? The (S) isomer if beta hydroxyfentanyl is the more potent (whereas it's the (R) isomer of aMP.
SO I wondered if anyone had other sources for the effects of a beta (or gamma) hydroxy on the potency of opioids. I briefly used to talk to Robojunkie and he sent Superjunky's route to alpha methyl fenttanyl. Lab notes - not huge amounts of detail, nothing unexpected BUT Robojunky said they usually made plain vanilla and when they tried the beta hydroxy, it was MUCH more potent.
I forget the dose he mentioned, but it was some silly large figure. I knew they were in deep.
I'm just keen to know if and by how much that (S) beta hydroxy has on the potency of fentanyl. I should add that beta hydroxy fentanyl and beta hydroxy thiofentanyl have both turned up in Russia killing many.
Wild-type μ-opioid receptor in vitro (EC50s = 38.1 and 64.9 nM, respectively).
Now in 'Opiates' by Lenz et al they state that the gamma -OH doesn't increase affinity BUT it improves transport to the receptor with (S) phenoperidine having a duration some x7 the (R). I got to wondering - with such short duration opioids, will those really short durations seemingly affect potency simply because the drug isn't transported? The (S) isomer if beta hydroxyfentanyl is the more potent (whereas it's the (R) isomer of aMP.
SO I wondered if anyone had other sources for the effects of a beta (or gamma) hydroxy on the potency of opioids. I briefly used to talk to Robojunkie and he sent Superjunky's route to alpha methyl fenttanyl. Lab notes - not huge amounts of detail, nothing unexpected BUT Robojunky said they usually made plain vanilla and when they tried the beta hydroxy, it was MUCH more potent.
I forget the dose he mentioned, but it was some silly large figure. I knew they were in deep.
I'm just keen to know if and by how much that (S) beta hydroxy has on the potency of fentanyl. I should add that beta hydroxy fentanyl and beta hydroxy thiofentanyl have both turned up in Russia killing many.
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