Salvinorin-A

Agonist of OPRK1

Structure

SERP Rating

In Cells

(3 ratings)

In Model Organisms

(3 ratings)

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.

Information

OPRK1

Agonist

DOI - 10.1073/pnas.182234399

Probe Availability:

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

Off-Target Selectivity Assesments

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

Probe Selectivity in Vitro:

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

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SERP ratings and comments

SERP Ratings

In Cell Rating

In Model Organisms

SERP 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

SERP 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

SERP 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 )