Opioid analogues analgesic potencies

As briefly reported the synthesis of an ideal analgesic asks for an improvement of both pharmacodynamic and in pharmacokinetic peculiarities. Sometimes if pharmacodynamic properties are improved, the pharmacokinetic characters can be still far from those of a perfect analgesic molecule. The quantities of opioids normally transported into the CNS can be low, and inadequate blood-brain barrier (BBB) permeation can be responsible for not optimized or for the different analgesic potencies among different opioid analogues. Consistently one major avenue of investigation involves the development of opioid analogues that penetrate the blood-brain-barrier (BBB). 

One major avenue of investigation in the field of opioid agonist and antagonist molecules involves the development of opioid analogues that penetrate the blood-brain-barrier (BBB) In fact inadequate blood-brain barrier (BBB) permeation can be responsible for low analgesic potencies. 

Sufentanil, a fentanyl analogue, is a highly lipid-soluble synthetic opioid with high affinity for OP3 (p) opioid receptors and a potency some 5-10 times that of fentanyl. It is a short-acting analgesic. 

---