KOR agonist 6

KOR agonist 6 is a KOR agonist (Ki = 0.25 pM) . KOR agonist 6 shows agonistic activity at MOR and DOR in CHO cells and inhibits Forskolin (HY-15371) -stimulated cAMP accumulation. KOR agonist 6 stimulates KOR-mediated [35S]GTPγS binding and inhibits cAMP accumulation in KOR-expressing HEK293 cells with potent agonistic activity, while showing lower β-arrestin recruitment potency. KOR agonist 6 demonstrates anti-nociceptive efficacy in mice. KOR agonist 6 can be used for the study of analgesics with reduced central nervous system (CNS) side effects[1].

Product Specifications

UNSPSC

12352005

Target

Opioid Receptor

Related Pathways

GPCR/G Protein; Neuronal Signaling

Field of Research

Neurological Disease

Smiles

O=C(NC1=CC=C([C@H]2C[C@@]34CC[C@]2(OC)[C@H]5[C@]36C7=C(C(OC)=CC=C7CC4N(CC6)CC8CC8)O5)C=C1)C9=NN(C=C9)C

Molecular Formula

C35H40N4O4

Molecular Weight

580.72

References & Citations

[1]Kong L, et al. Structure-Activity Relationship of N-Cyclopropylmethyl-7α-[para- (arylcarboxamido) phenyl]-6,14-endoethano-tetrahydronorthebaines as Potent and Selective Kappa Opioid Receptor Agonists. J Med Chem. 2025 Aug 14;68 (15) :15889-15909.