Modyfing the Message Flashcards
Agonism
agonist?
Agonist = chemical that increases effect of a NT
- can result in excitation or inhibition, depending on the type of NT
Besides summation, info transmitted by Neurons can be modified in various ways
That is, variations in any of the functions of NTs and Synapse can affect the message sent
Antagonism
antagonist?
antagonist = chemical that DECREASES EFFECT of a NT
- can result in excitation or inhibition, depending on the type of NT
EX of agonist and antagonist with ACh
ACh broken down in cleft by enzyme Acetylcholinesterase (AChE) into Choline (re-uptaken) & Acetate
- in patients with ACh deficit, can block enzyme so little available ACh repeatedly stimulates Postsyn cell - so such an AChE blocker is an ACh-Agonist
In contrast, a Choline Reuptake-Blocker would prevent re-synthesis of ACh and so is a ACh-Antagonist
EX Agonist vs. Antagonist with Serotonin
- Serotonin typically remains intact, reuptaken whole into Presynaptic cell by Transporter Proteins
- 5-HT - Agonist drugs like Prosac block reuptake of Serotonin, prolonging its effects on Postsynaptic Cell
- 5-HT Antagonist like enzyme MAO converts Serotonin into inactive form that won’t affect Postsyn Cell
Antagonists and Agonist can also operate inside ____________ cell to affect NT release
- Some antagonistic drugs (Reserpine) prevent NTs (Monoamines) from being packaged into vesicles
- some agonists (Black widow spider venom) cause massive release of NT (ACh)
Receptivity Changes
- receptor sites can be BLOCKED BY NT MIMICS that do not readily detach
- e.g. LSD binds to Serotonin sites - Activation of DNA sequences initiated the production of proteins for structural and chemical changes within cell
- receptor sites can increase/decrease in number
- e.g. repeated activity -> more DENDRIDIC SPINES, more receptor sites
availability of NT components
- some NT’s, like Substanc P, are produced in the Neuron’s soma
- others, like ACh, are produce in Terminal and are efficiently recycled from cleft
- can depend on diet for availability of precursors
- a few precursors will pass blood-brain barrier, so can be administered as drugs
Some NTs, like Substance P (PAIN), are produced in Neuron’s soma, and may require hours/days to replenish
- carried by Kinesin molecules (proteins) that ‘walk’ along micro-tubules from soma to terminal
NTs that depend on diet for availability
- Tryptophan in turkey»_space; serotonin
- Choline from milk or synthesized from lecithin»_space; ACh
Examples of precursors that will pass the blood-brain barrier
L-DOPA for Dopamine
Receptors on PRE-synaptic terminal
Auto Receptors
Axoaxonic Synapses
Auto-Receptors
Some AXONS have Receptor Sites for their OWN (usually inhibitory) NT
NT binding with these sites»_space; Negative Feedback Loop via Second Messengers within PRE-synaptic cell
- that is, their own NT prevents them from releasing more NT
EX: by closing own Ca++ gates or blocking reset of Resting Potential by interfering with Na+/K+ Pump
Axoaxonic Synapses
Axon to Axon
Presynaptic Terminal may have Receptor Sites for Inhibitory or Excitatory NT from ANOTHER CELL
Ex: Brain Endorphins stimulate opiate receptors on terminal of pain cell, inhibiting release of Substance P