NPB 168 Lecture Notes - Lecture 5: Periaqueductal Gray, Area Postrema, Nippon Professional Baseball
27 Apr 2016
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Potency as muscle relaxant vs. potency as analgesic, moderate positive correlation. Endogenous opiates: pro-peptides: pro-opiomelanocortin (binds to mu and delta) Our heroin that is released when we exercise. Used for modulating pain: proenkephalin (binds to mu and delta) Neuromodulators: prodynorphin (binds to kappa, endomorphin (binds to mu) Endogenous opiate receptors: au g-protein coupled receptors (metabatropic, mu receptors. Opiates bind most strongly to this receptor, probably creating the rush or high: delta receptors. Motor integration (motor cortex, striatum, substantia nigra) Hormonal control (temp. , water balance, food intake hypothalamus and pituitary) Cellular mechanisms: open k channels (postsynaptic inhibition) leading to hyperpolarization. Mu and delta receptors: close ca channels (axoaxonic inhibition) drop in neurotransmitter release. Mu, delta, and kappa: reduce transmitter release (presynaptic autoreceptors) presynaptic cell has autoreceptor so inhibiting neurotransmitter release. Opiates: cross-tolerance occurs and appears to be receptor dependent (pharmacodynamics) Physical dependence: withdrawal symptoms (opposite of acute symptoms, abstinence symptoms for opiates is not fun.
