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Ligand Binding Methods- subtyping |
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Definition
(using a radioactive labelled ligand) this is a Method of classifing Drugs by Identifing their receptor and location . E.g. Morphine Binds to receptor which decreases pain sensation- same receptor and location as the Opiod Neurotransmitters *** New research in the US, focusing on the pharmacological aspects of smoking marijuana, are closer to understanding how the drugs active ingredients exert its effects, paving the way for drugs that selectively bind and block subtypes of cannabinoid receptors on one type of cell but not another. |
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Endorphins are "endogenous" which means they are a.produced inside body
These endorphins make effects when they attach to which (clue: Morphine-like effects) NT receptors? |
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Antagonist opiod receptors have this effect |
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occupies the receptor without opiod analgesic effects. |
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A neuropeptide that is a type of endorphin. (CNS)Neurons containing the enkephalins are even more widely distributed in the central nervous system. Levels are particularly high in the dorsal horn of the spinal cord, a region that contains opiate receptors and is involved in the transmission of pain (see Chap. 11). Enkephalins may act at this location to inhibit pain transmission by sensory nerves |
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agonis antagonist nicotine Ach curare msucarnic Ach atropine |
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Glutamate vs. (AMPA and NMDA) |
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Definition
can bind to any channel vs. receptor specific |
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Norepinephrine Alpha= Norepineprhine Beta= |
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Definition
To assess the postsynaptic actions of a neurotransmitter candidate e.g. ionophoretic application 1. electrophysiological changes 2. Determine if it mimics effect of transmitter Criteria: localization, synthesis and release |
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localize MRNA transcripts through applying radioactive label probes |
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various receptors, various effects |
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4 transmitter 3 receptors one effector |
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Definition
2 receptors mix into 5 effectors |
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The fucnction of signal cascades |
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Definition
Signal amplification by G-Protein coupled second messenger cascades |
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Term
The function of signal cascades |
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Definition
Signal amplification by G-Protein coupled second messenger cascades |
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Definition
Kinase driven- provides- a confirmational change |
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Term
long term depression vs. long term potentiation |
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Definition
depends on prestimulus and amount of Ca+2 released |
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at high extraculluar concentrations- causing an increase in Ca2+ pathological high Ca2+ activates proteases and destroys neurons |
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Heart attack, blocks glutamate- for Ca+2 extra cellular- |
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slow synaptic transmission |
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specific NT- confirmational change- it binds |
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integral membrane protein (expands membrane) NT binding sites- then what? |
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Definition
binding changes shape, g-protein- inside of the membrane- NO NT, NO G-PROTEIN |
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Definition
alpha beta gamma subunits anchored to membrane- |
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binding site GDP bound when activated |
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Term
when it bound by G-protein- NTs, loses affinity for GDP neucleotide, fall off and now has a high affinity for GTP |
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Definition
activation of the G-Protein- binds to an activated receptor - a receptor with a NT bound to it |
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