Yeah, I want to avoid any IV. Not so eager to go down that route which would inevitably lead me back to H and or actually die this time. Having said that, I'll be back to report on the plugging experience w/ my N's. Know about crushing 'em and eating them? Wouldn't breaking the coating make it administer in the functionality of an IR as opposed to a SR? I don't want to be wasteful, so I figured if anyone knew, I would save me the experimental phase. Many Thanks Sekio!
Oh, just found this on another board, going to do a lil more research to prove it, in the mean time...anyway, the receptor sites are plentiful; dirty lil feller.
"...and then Tapentadol comes in the form of it's hydrochloride addition salt, freely soluble in water at physiological pH. Apparently the low bioavailability (32% fasting condition, 32% fed conditions) is due to extensive first-pass metabolism by the liver. MOR - 0.2-0-23 μM
Norepinephrine - 0.6-0.62 μM. It also apparently binds to the β1-adrenergic, 5-HT2a, 5-HT transport, σ2 & the PCP-site of the glutamate receptor. It's MoR : Other-opioid receptor selectivity is about 10. This is a bit of a mix, not very nice at all, I suspect. More worrying is the different effaciacy depending on ROA. In mouse studies the MED50 are 21mg/kg oral but 1mg/kg IV. In rats it was 68.1 oral, 0.464 IV. This is a MASSIVE difference..." (credits to borohydride)