·k(kappa)receptor Sedation Analgesia(spinal level) -Miosis(瞳孔缩小)
• κ(kappa) receptor – Sedation – Analgesia (spinal level) – Miosis （瞳孔缩小）
·δ(delta)receptor - analgesia (spinal supraspinal) release of growth hormone ·o(sigma)receptor -dysphoria (opposite of euphoria) hallucination (both visual auditory) respiratory and vasomotor stimulation -mydriasis(瞳孔散大)
• δ (delta) receptor – analgesia (spinal & supraspinal) – release of growth hormone • σ (sigma) receptor – dysphoria (opposite of euphoria) – hallucination (both visual & auditory) – respiratory and vasomotor stimulation – mydriasis （瞳孔散大）
Opioid receptors and lignads Receptor endogenous ligands receptor subtypes μ β-endorphin μ1，μ2 K dynorphin K1)K2)K3 6 enkephalins 81 62 O
Opioid receptors and lignads __________________________________________________________ Receptor endogenous ligands receptor subtypes __________________________________________________________ μ β-endorphin μ1 , μ 2 κ dynorphin κ1 , κ2 , κ 3 δ enkephalins δ1 , δ 2 σ ? ________________________________________________
Proopiomelanocortin Proenkephalin Morphine CH3 6000000o000a00000000000000 B-Lipotropin 00000 6 000000000o0o0o0000 o00o0 HO OH O0000 000000000000000000 O00o0 Q0000 Enkephalin B-Endorphin Opioid receptors CH2-CH=CH2 K+-permeability↑ Ca2+-influx↓ Excitability↓ Release of transmitters↓ HO HO O Naloxone Cellular actions of opioid receptor agonists(ligangs)and antagonist
Cellular actions of opioid receptor agonists (ligangs) and antagonist
Distribution of opioid receptors CNS distribution is not uniform. ● Areas concerned with pain. Receptor locations beginning with highest concentration areas 1.cerebral cortex 0o0o0oooo0ooaoooooooooNH2 Extracellular 2.amygdala 3.septum 4.thalamus 00 5.hypothalamus 6.midbrain 7.spinal cord Cytoplasmic HOOC 0000000000000000000000000f
Distribution of opioid receptors • CNS distribution is not uniform. • Areas concerned with pain. • Receptor locations beginning with highest concentration areas 1. cerebral cortex 2. amygdala 3. septum 4. thalamus 5. hypothalamus 6. midbrain 7. spinal cord Extracellular Cytoplasmic NH 2 HOOC