κ Opioid Receptors

The κ opioid receptor, (also known as OP2, KOP, KOR), is a member of the opioid family of G-protein-coupled receptors that also includes μ, δ and NOP receptors. Three variants of the receptor (designated κ1, κ2, and κ3) have been characterized.

Products
Background
Literature
Gene Data

Agonists

Cat No Product Name / Activity
0699 BRL 52537 hydrochloride
Potent and selective κ agonist
3195 Dynorphin A
Endogenous κ agonist
3196 Dynorphin B
Endogenous κ agonist
2962 6'-GNTI dihydrochloride
Selective κ/δ opioid heterodimer receptor agonist
1483 GR 89696 fumarate
Subtype-selective κ agonist
0778 ICI 199,441 hydrochloride
Potent κ agonist
0822 ICI 204,448 hydrochloride
κ agonist, acts peripherally
0783 N-MPPP Hydrochloride
Selective κ agonist
5519 (-)-Pentazocine
κ-agonist; antinociceptive
2134 Salvinorin A
Highly potent and selective κ agonist
0471 (+)-U-50488 hydrochloride
Standard selective κ agonist. Less active enantiomer of (±)-U-50488 (Cat. No. 0495)
0495 (±)-U-50488 hydrochloride
Standard selective κ agonist
0496 (-)-U-50488 hydrochloride
Standard selective κ agonist. More active enantiomer of (±)-U-50488 (Cat. No. 0495)
0498 U-54494A hydrochloride
κ agonist

Antagonists

Cat No Product Name / Activity
0347 nor-Binaltorphimine dihydrochloride
Standard κ selective antagonist
0794 DIPPA hydrochloride
Selective irreversible κ antagonist
1282 GNTI dihydrochloride
Potent, selective κ antagonist
4866 ML 190
Selective κ opioid receptor antagonist

Other

Cat No Product Name / Activity
5611 Salvinorin B
Activates the κ-opioid DREADD (KORD)

The κ opioid receptor, (also known as OP2, KOP, KOR), is a member of the opioid family of G-protein-coupled receptors that also includes μ, δ and NOP receptors. Three variants of the receptor (designated κ1, κ2, and κ3) have been characterized. However only one cDNA clone has been identified, hence these receptor subtypes are likely to arise from interaction of one κ-opioid receptor protein with other membrane associated proteins.

κ Opioid receptors are located predominantly in the cerebral cortex, nucleus accumbens, claustrum and hypothalamus and have been implicated in the regulation of nociception, diuresis, feeding and neuroendocrine secretions. Dynorphins A and B and α-neoendorphin appear to be the endogenous ligands. The human gene encoding the κ opioid receptor has been localized to chromosome 8 (8q11.2).

External sources of pharmacological information for κ Opioid Receptors :

Literature for κ Opioid Receptors

GPCR

GPCR Product Listing

A collection of over 450 products for G protein-coupled receptors, the listing includes research tools for the study of:

  • Rhodopsin-like Receptors
  • Secretin-like Receptors
  • Glutamate Receptors
  • Frizzled Receptors
  • GPCR Signaling
Pain

Pain Research Product Guide

A collection of over 250 products for pain research, the guide includes research tools for the study of:

  • Nociception
  • Ion Channels
  • G-Protein-Coupled Receptors
  • Intracellular Signaling
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Peptides Involved in Appetite Modulation Scientific Review

Written by Sonia Tucci, Lynsay Kobelis and Tim Kirkham, this review provides a synopsis of the increasing number of peptides that have been implicated in appetite regulation and energy homeostasis; putative roles of the major peptides are outlined and compounds available from Tocris are listed.

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Addiction Poster

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Pain Poster

Peripheral sensitization is the reduction in the threshold of excitability of sensory neurons that results in an augmented response to a given external stimulus. This poster outlines the excitatory and inhibitory signaling pathways involved in modulation of peripheral sensitization. The role of ion channels, GPCRs, neurotrophins, and cytokines in sensory neurons are also described.

κ Opioid Receptor Gene Data

Species Gene Symbol Gene Accession No. Protein Accession No.
Human OPRK1 NM_000912 P41145
Mouse Oprk1 NM_011011 P33534
Rat Oprk1 NM_017167 P34975