1256921-77-3Relevant articles and documents
Design and synthesis of KNT-127, a δ-opioid receptor agonist effective by systemic administration
Nagase, Hiroshi,Nemoto, Toru,Matsubara, Ayaka,Saito, Manabu,Yamamoto, Naoshi,Osa, Yumiko,Hirayama, Shigeto,Nakajima, Mayumi,Nakao, Kaoru,Mochizuki, Hidenori,Fujii, Hideaki
, p. 6302 - 6305 (2010)
We have reported previously the novel δ-opioid agonist, SN-28, which was more potent in in vitro assays than the prototype δ-agonists, TAN-67 and SNC-80. However, when administered by subcutaneous injection, this compound showed no analgesic effect at dosages greater than 30 mg/kg in the acetic acid writhing test. We speculated that SN-28 was not effective in the test because the presence of the charged ammonium groups prevented its penetration through the blood-brain barrier. On the basis of our proposal, we designed the novel δ-agonist, KNT-127, which was effective with systemic administration.