MOR - Micro Receptor (OP3)
(Ligands: endomorphin, enkephalin, DAMGO)
u1 - analgesia in the brain, euphoria, excitement, psycho-dependence
u2 - analgesia in the spine, sedation, anxiolysis, respiratory depression, constipation, itching, physical dependence, tolerance
u3 - unknown
2 subtypes have been characterized. A 3rd subtype has been theorized based on the analgesia produced by morphine 6-substituted analogues in mu1 and 2 knockout subjects. This third subtype interacts with opioid alkaloid compounds and not opioid peptides; only certain compounds are believed to interact with this subtype - specifically, morphine analogues with C-6 substitutions such as morphine-6-glucuronide, 6-acetylmorphine, heterocodeine, and possibly fentanyl.
KOR - Kappa Receptor (OP2)
(Ligands: dynorphin, enadoline, ketocyclazocine)
spinal analgesia, dysphoria, miosis, sedation, diuresis (increased urination), psychotomimesis, anti-itching, counteraction of mu-agonist effects, anti-addictive effect, dopamine inhibition, mu & dopamine receptor upregulation
At least 2 subtypes of kappa receptor have been characterized. Kappa is the endogenous dynorphin receptor.
DOR - Delta Receptor (OP1)
(Ligands: enkephalin, deltorphin, DPDPE)
anxiolysis, antidepressant properties, respiratory stimulation or depression, upregulation of brain-derived neurotrophic hormone, cardioprotection, potentiation of mu analgesia
2 subtypes of delta receptor have been characterized.
ORL1 - Orphan Receptor, Opioid-Like-Receptor 1 (OP4)
(Ligand: nociceptin)
hyperalgesia (pain), anxiety, counteraction of mu-agonist effects, anorexia or hunger
Endogenous receptor for nociceptin, the neurotransmitter implicated in transduction of pain signals.
0 comments:
Post a Comment