borohydride
08-09-2011, 04:56 PM
The book 'Pain: current understanding, emerging therapies, and novel approaches to Treatment' by By Chas Bountra, Rajesh Munglani et al discusses a potent opioid now undergoing trial.
It's Ki at the Mu receptor is 3.3 (morphine is 19.3) & it has greater Mu:Delta:Sigma selectivity.
Sounds great. Sadly, it's a peripheral acting opioid that is being researched for the treatment of burns & similar trauma via topical administration.
Oh, it has an old name - loperamide.
This just goes to show that if only loperamide could be convinced to cross the BBB, it would be a very potent opioid. The central receptors are slightly different & won't like the -Cl & the reason it won't pass the BBB is that bare hydroxyl....
If these two features are resolved, then it only remains to find a cheap supply of multi-gram quantities of loperamide & of you go!
It's Ki at the Mu receptor is 3.3 (morphine is 19.3) & it has greater Mu:Delta:Sigma selectivity.
Sounds great. Sadly, it's a peripheral acting opioid that is being researched for the treatment of burns & similar trauma via topical administration.
Oh, it has an old name - loperamide.
This just goes to show that if only loperamide could be convinced to cross the BBB, it would be a very potent opioid. The central receptors are slightly different & won't like the -Cl & the reason it won't pass the BBB is that bare hydroxyl....
If these two features are resolved, then it only remains to find a cheap supply of multi-gram quantities of loperamide & of you go!