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Salvinorin-A | Agonist of OPRK1
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (3 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
OPRK1
  • Ki:16 nM
  • EC50:235 nM
Agonist
Up to 10 nM

Selectivity

In Vitro Selectivity Assessment

Potency: Ki - Mu opioid receptor >10,000 nM, Delta opioid receptor >10,000 nM

Selectivity Assessment Description:
In a screen of GPCRs (50), 10 uM of Salvinorin A was active only against OPRK1.

Potency
Cellular
In Vitro

OPRK1

Mode of Action: Agonist

Structure-Activity-Relationship data available? No

Orthogonal Probes def

ICI-199441

Chemical Information

Molecular Formula C23H28O8
SMILEs COC(=O)[C@@H]1C[C@H](OC(C)=O)C(=O)[C@H]2[C@@]1(C)CC[C@H]1C(=O)O[C@H](c3ccoc3)C[C@]21C
InChI InChI=1S/C23H28O8/c1-12(24)30-16-9-15(20(26)28-4)22(2)7-5-14-21(27)31-17(13-6-8-29-11-13)10-23(14,3)19(22)18(16)25/h6,8,11,14-17,19H,5,7,9-10H2,1-4H3/t14-,15-,16-,17-,19-,22-,23-/m0/s1
Molecular weight 432.18 Da
AlogP 0.0
HBond acceptors 8
HBond donors --
Atoms 59

References

Publications

    Cross References

    canSARChEMBLBindingDB

    Vendors

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    Expert Reviews

    by SERP
    (on 31 May 2016 )
    Cellular Use Rating
    In Model Organisms
    This is a structurally unique probe for kappa opioid receptors. It is highly selective, poorly soluble, and rapidly metabolized. Literature suggests it has clear differences from other kappa opioid...
    by SERP
    (on 3 Jun 2016 )
    Cellular Use Rating
    In Model Organisms
    This is an extremely potent and selective probe. It has activity at the CB1 receptor at 200 nM, but this should not interfere with interpretations of biological activity when the probe is used at the...
    by SERP
    (on 23 Jun 2016 )
    Cellular Use Rating
    In Model Organisms
    The compound is a diester and, additionally, a lactone. It is highly lipophilic. The potential for intracellular esterase inactivation of the probe is high. Since the probe is for KOR, there are many...
    Note: The Chemical Probes Portal only endorses compounds as chemical probes for use as specific and selective modulators of the proposed target if they receive three or more (3-4) stars. Read more about our evaluation criteria