* To be completed throughout the course and submitted in Week
8*
Neuro Receptor Location/Function/Effects Distribution Drug classes that Specific medications that target
transmitter Subtype /symptoms of excess (ie: CNS/PNS, target this this neurotransmitter or receptor
or deficit if GI, vascular) neurotransmitter or
applicable receptor
Glutamate AMPA Reside post-synoptically CNS (spinal AMPA antagonist Anticonvulsant: Lamotrigine and
but are in much more of cord, brain) Propagating seizures Topiramate.
a state of flux than NMDA Anticonvulsant drugs AMPA antagonists are drugs used to
receptors. The average treat seizures (unusual electrical
half-life for an AMPA activity in the brain causing changes
receptor in the post- in behavior, movement, or feelings) in
synaptic membrane is 15 adults and children.
minutes.
The Hippocampus, outer
layer of the cortex, basal
ganglia, olfactory regions,
lateral septum, and
amygdala of the CNS are
all enriched with GluA1,
GluA2, and GluA3
subunits.
MNDA The NMDA receptor CNS NDMA antagonist Anesthetic: Nitrous oxide
likely serves a frankly Cognitive processes Dissociative hallucinogens: ketamine
structural role in addition such as and phencyclidine induce dream-like
to its function as a ligand- consciousness, mentation with distortion of sight
gated ion channel, while thought, and memory. and
the AMPA receptor is Hallucinogens, sound.
more Alcohol, anesthetic Alcohol binds to NMDA
peripherally. Clinically
, significant for the
involvement in the
variety of drugs that are
involved in the cognitive
process.
GABA GABA a Brain and Spinal cord, CNS (spinal Benzodiazepines, Benzodiazepines
Producing a calming cord, brain) GABA(A) receptor is Lorazepam, Clonazepam,
effect. an ion channel Diazepam,
GABA (A) is linked to ligan- composed of five Triazolam
gated ion channels subunits with many Anesthetic dugs
Lack of GABA leads to the binding sites. The Zolpidem (sedative),
conditions like epilepsy, Benzodiazepines bind Zaleplon(hypnotic)CNS, Zopiclone,
seizures, and mood to some preferential Eszopiclone, Allopregnanolone -
disorders. subunits. Neuroactive steroids
Excess GABA leads to
hypersomnia.
Sedative and analgesic
properties
GABA b Agonist, therapeutic CNS Agonist, Arbaclofen Placarbil investigated
action: sleepiness in Therapeutic actions: for treatment of spasticity in
narcolepsy, pain cataplexy, sleepiness multiple sclerosis, acute back
reduction in chronic pain in narcolepsy, possible spasms, and GERD.
and fibromyalgia; possible enhanced slow-wave Baclofen agonist used to manage
use for alcohol sleep, possible utility severe spasticity of cerebral or spinal
withdrawal. for alcohol. origin in adults and pediatric
GABA b receptors are G patients.
protein receptors that
may be coupled with
calcium
or potassium channels.
Serotonin 5HT 1a The 5-HT1A receptors are CNS: raphe partial 5-HT1A-R Anxiolytics/antidepressants
5HT G-protein coupled nuclei, agonists Buspirone, and Tandospirone (also
receptors that exert their hippocampus, has beneficial effect in tx of other
effects through Gi/o PNS: cholinergic CNS disorders like Alzheimer’s
proteins to inhibit heteroreceptors
adenylyl in myenteric
cyclase, as well as other