The kappa opioid receptor is associated
with the perception of visceral
pain
by
Black D, Trevethick M
Department of Molecular Pharmacology and Discovery Biology,
Pfizer Central
Research, Sandwich, Kent, UK.
Gut 1998 Sep; 43(3):312-3
ABSTRACT
Mu-, delta- and kappa-opioid receptors are widely expressed in the central
nervous system where they mediate the strong analgesic and mood-altering actions
of opioids, and modulate numerous endogenous functions. To investigate the
contribution of the kappa-opioid receptor (KOR) to opioid function in vivo, we
have generated KOR-deficient mice by gene targeting. We show that absence of KOR
does not modify expression of the other components of the opioid system, and
behavioural tests indicate that spontaneous activity is not altered in mutant
mice. The analysis of responses to various nociceptive stimuli suggests that the
KOR gene product is implicated in the perception of visceral chemical pain. We
further demonstrate that KOR is critical to mediate the hypolocomotor, analgesic
and aversive actions of the prototypic kappa-agonist U-50,488H. Finally, our
results indicate that this receptor does not contribute to morphine analgesia
and reward, but participates in the expression of morphine abstinence. Together,
our data demonstrate that the KOR-encoded receptor plays a modulatory role in
specific aspects of opioid function.
Pain
Morphine
Tramadol
Tolerance
Endomorphins
Buprenorphine
Fentanyl and ketamine
Kappa upregulation and addiction

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