Introduction to Central Nervous System Pharmacology Flashcards
Explain the differences between voltage-gated and ligand gated ion channels.
voltage gated channels’ confirmation change is triggered by changes in voltage across a membrane
ligand-gated channels require the binding of a specific molecule (ligand) with corresponding shape and charge to bind the receptor to create a confirmation change
List the major chemical and peptide neurotransmitters. (7)
serotonin 5-HT dopamine norpeneiphrine histamine glutamate GABA glycine
Identify neuronal targets for drug action. (8)
membrane conductivity, transmitter biosynthesis, transmitter storage, transmitter release, transmitter uptake, transmitter metabolism and pre- and postsynaptic receptors.
- List the functional classes of CNS drugs
Psychopharmacological agents (cognition) 1. Antidepressants 2. Antipsychotic 3. Sedative and hypnotics 4. Mood stabilizers 5. Psychostimulants 6. psychedelics 7. cannabinoids Anti-seizure drugs Opioids (analgesics) Anesthetic (general and local) Drugs for neurodegenerative disease 1. Cognition enhancers 2. Anti-parkinsonism
Discuss the activity, synthesis, receptors and pertinent neuronal pathways that are important to the biological role of serotonin.
excitatory or inhibitory depending on the type of ion channel or G-protein coupled receptor
synthesized from tryptophan (via TPH and AAAD) and can be metabolized to melatonin (via AANAT and ASMT)
released by axons originating in raphe nuclei, rostral raphe axons ascending to the cerebral cortex, also caudal raphe axons terminating in medulla or descend spinal cord
Discuss the activity, synthesis, receptors and pertinent neuronal pathways that are important to the biological role of dopamine.
excitatory or inhibitory based on receptor type
D1-D5 receptors are G coupled receptors, D1 and D5- adenylyl cyclase; D2-4 inhibit adenylyl cyclase
synthesized from tyrosine (via TH) and then from DOPA (via AAAD)
released via four pathways: substantia nigra to caudate-putamen, VT to mesolimbic forebrain, VT to frontal cortex and tuberoinfundibular system (arcuate nucleus to median eminence
Discuss the activity, synthesis, receptors and pertinent neuronal pathways that are important to the biological role of norepinephrine.
G protein-coupled adrenergic receptors, excitatory via a1 and B1, inhibitory via a2 and B2
synthesized from dopamine (via DBH)
main pathways originate in locus coeruleus (to FC, thalamus, hypothalamus, limbic and cerebellum) and caudal raphe nuclei (to amygdala and descend to the midbrain)
Discuss the activity, receptors and pertinent neuronal pathways that are important to the biological role of histamine.
Function as pacemakers acting at 3 receptor subtypes in brain: H1 Gq (E), H2 Gs (E) and H3 auto-receptors (I); Produces arousal, analgesia, promotes locomotion, learning and memory
pathways originate at tuberomamillary nucleus (very small locus)
Discuss the activity, receptors and pertinent neuronal pathways that are important to the biological role of glutamate.
Excitatory reaction at receptors via ion channels (NMDA, KA, AMPA) and G-coupled receptors
synthesized via normal amino acid synthesis
cortico-cortical pathways, thalamus to cortex and extrapyramidal pathway
Discuss the activity, receptors, synthesis and pertinent neuronal pathways that are important to the biological role of glycine.
inhibitory via Cl- influx in spinal cord and brainstem
synthesis via yin/yang relationship of GABA and glycine (via glutamate decarboxylate)
Discuss the activity, receptors, and pertinent neuronal pathways that are important to the biological role of glycine.
G-coupled receptors change K+ conductance: M1 via increasing IP3 and DAG and M2 via decreasing cAMP for brainstem and cortex cognition and motor control
and
excitatory nicotinic recptors (ion channel) a2B2 configuration is most widely distributed in the substantia nigra and cortex for cognition and motor cortex
pathways in basal forebrain cholinergic complex and pontomesencephalotegmental cholinergic complex
List important peptide neurotransmitters.
CCK, oxytocin, vasopressin, neuropeptide Y (feeding), opioids (endorphins, enkephalins and dynorphin), orexin nad subance P (pain)
(other, non-peptide include nitric oxide and CO)
