Salvinorin-A

Agonist of OPRK1

Structure

Information

Protein target names: OPRK1

Mechanism of action: Agonist

In Vitro Validations

Uniprot ID: P41145
Target Class: GPCR
Target SubClass: Opioid receptor
Potency: Ki
Potency Value: 16 nM
PDB ID for probe-target interaction (3D structure): --
Target aliases:
Kappa-type opioid receptor, OPRK, OPRK1, OPRK_HUMA ...

In Cell Validations

In Vivo Data

No in Vivo Validations

Reagent authentication certificate: PDF image

I have extra information to add

SERP ratings and comments


SERP Ratings

In Cell Rating
In Model Organisms

Comments:

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 receptor ligands.

(last updated: 31 May 2016 )

SERP Ratings

In Cell Rating
In Model Organisms

Comments:

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 recommended doses/concentrations.

(last updated: 3 Jun 2016 )

SERP Ratings

In Cell Rating
In Model Organisms

Comments:

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 other more suitable ligands to choose from which are available, selective and stable.

(last updated: 23 Jun 2016 )