Neuropharmacology Flashcards
Amino Acid NT =
Serotonin and GABA
Catecholamine NT =
NE, dopamine, EPI
Synaptic Neurotransmission Process
AP leads to calcium influx which causes exocytosis of NT vesicles that can act on ionotropic, metabotropic or presynaptic receptors
They then get reuptaken/metabolized, membranes get recycled, dense core granules with neuropeptides come out to release neuropeptides
NT that are reuptaken =
Dopamine, NE, GABA
NT that are metabolized =
ACh and peptides
NT that are reuptaken by glial cells =
Glutamate
Excitatory NT
propagates signal farther to have more action potentials down the line
Inhibitory NT
hyperpolarization and signal will not be propagated any further
Important for drug binding a specific receptor
Hydrophobicity
pKa
Conformation
Spatial arrangement
Ionotropic receptors =
ligand gated ion channels
Define Ionotropic receptors
Release NT causes electrical effects on postsynaptic neuron by opening a specific ion channel
Complex
Metabotropic receptors =
G-protein coupled receptors
Define Metabotropic receptors
Single subunit
Conformation change which activates this family
Serotonin!!!
Glutamate is synthesized from
Glutamine is released by glial cells and broken down via presynaptic terminals
Glutamate is what type of NT
Fast EXCITATORY
Ionotropic glutamate receptors Non-NMDA
Fast depolarization (AMPA and kainate)
Ionotropic glutamate receptors NMDA
Learning/memory
GABA is synthesized from
Glutamate
GABA is what type of NT
Inhibitory
GABA purpose is
Prevent neurons from firing too often and too easily
Low GABA =
anxiety, seizures, PARKINSON’s
GABA(A) =
ionotropic
Modulator of barbiturates and BZD
Antagonists for flumazenil
GABA(B) =
Metabotropic GPCR
Agonist baclofen
GABA(C)/GABA(A)-rho =
Ionotropic
Brain and retina
GABA(A) drugs
Benzo Barbiturates Anesthetics Neurosteroids Alcohol ANTAGONISTS- picrotoxin AGONIST - muscimol
ACh synthesized from
acetyl CoA and choline via choline acetyltransferase
ACh is brokendown by
AChE
Butyrylcholinesterase
ACh acts on
Nicotinic and muscarinic receptors
Nicotinic Receptors + ACh
Ionotropic
Excitatory
**Muscarinic Receptors + ACh
Metabotropic
Excitatory at M1, M3, M5
Inhibitory at M2 and M4
**Catecholamine synthesis
Tyrosine to DOPA via tyrosine hydroxylase (RATE LIMITING)
DOPA to Dopamine via DOPA decarboxylase
Dopamine to NE via dopamine beta hydroxylase
NE NT
Inhibitory via beta receptors in the brain
some excitatory through alpha or beta
NE Functions
Arousal
BP regulation
Control of mood (big in depression)
NE Termination =
reuptake into noradrenergic nerve endings
Uses for alpha adrenoreceptors agonists
(a1) Symptomatic relief of nasal congestion
(a2) BP lowering
Uses of beta adrenoreceptors agonists
(b2) asthma
Inhibitors of NE reuptake (prolong effects)
TCA
Cocaine
Drugs affecting NE synthesis
Carbidopa, methyldopa
Drugs affecting NE release and storage
Reserpine
Drugs inhibiting metabolism
MAOIs
Not enough dopamine =
Parkinson’s!!! (in nigrostriatal pathway)
Schizo, ADD, drug addiction
Dopamine is broken down by
COMT and MAO
Dopamine is what type of NT
Metabrotropic
Excitatory in D1 and D5
Inhibitory in D2, D3, D4
Dopamine functions
Motor control (D2) Endocrine control (prolactin - inhibitory) Behavioral (D1; pleasure, addiction, correct thinkin)
Dopamine precursors =
Levodopa
Dopamine receptor agonists =
Bromocriptine, pergolide
MAO-B inhibitors =
Selegiline/rasagiline
Dopamine receptor blockers =
Antipsychotic effects (D2) for schizo
Serotonin is what type of NT
Metabotropic
Serotonin Types and Metabolism
7 types mainly in CNS
Metabolized by MAO
Serotonin Functions
Hallucinations/behavior
Sleep/wakefulness/mood
Feeding (appetite)
