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Summary Chapter 2 Stahl Notes
Summary of the content in chapter 2 of stahls psychopharmacology, including important figures and tables.
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Chapter 2: Transporters, Receptors and Enzymes as Targets of Psychopharmacological DrugAction
o Sites of action for therapeutic agents
o Transporters for neurotransmitters (33%)
o Receptors coupled to G proteins (33%)
o Enzymes (10%)
Nomenclature for Medications
o Moving from traditionally naming medications for their therapeutic indications
Antidepressant, antipsychotic, etc.
So called antipsychotics being used for depression shows how
ineffective the current nomenclature is
Changing to nomenclature based on neuroscience
Serotonin transport inhibitor
Dopamine D2 and serotonin 5HT2A antagonist
o Genetic Variation
o Moving towards understanding gene variations and how those impacts whether the
patient responds to the drug or not
Pharmacogenomics
Neurotransmitter Transporters as Targets of Drug Action
o 12-transmembrane-region proteins
o Utilized by presynaptic reuptake and vesicular storage
o Cross the membrane 12 times
Plasma Membrane Transporters
Some are presynaptic and others are on glial membranes
o Solute carrier SLC6 gene family
Includes transporters for the monoamines:
Serotonin, norepinephrine, dopamine
Neurotransmitter GABA
Amino acid glycine
o Solute carrier SLC1 gene family
High affinity glutamate transporters
Intracellular synaptic vesicle transporters
SLC18 gene family
o Vesicular monoamine transporters (VMATs) for:
Serotonin, norepinephrine, dopamine and histamine
o Vesicular acetylcholine transporter (VAChT)
SLC32 gene family
o Vesicular inhibitory amino acid transporters (VIAATs)
SLC17 gene family
o Vesicular glutamate transporters
vGluT1-3
SLC6 Gene Family as Targets of Psychotropic Drugs
o Monoamines use unique presynaptic transporters (each different)
o Serotonin: SERT
o Norepinephrine: NET
, o Dopamine: DAT
They still have affinity for the other receptors
If other transportable neurotransmitters or drugs are in the area they
can also be transported into the presynaptic neuron
o NET also has high affinity for dopamine transport
o DAT has high affinity for transport of amphetamines as well as
dopamine
o SERT has high affinity for MDMA transport
o Same vesicular transporter in the synaptic vesicle membranes of all three monoamines
plus histamine
o Vesicular monoamine transporter 2: VMAT2
o Energy
o Transporters in the SLC6 gene family couple the “downhill” transport of sodium with
the “uphill” transport of the monoamines
Up a concentration gradient
Sodium dependent cotransporters (sodium-potassium ATPase) sodium
pump
Usually also involves additional cotransport of chloride
In some cases, also the counter transport of potassium
o Binding sites
o One site for the monoamine to bind
o Binding sites for 2 sodium ions
Dimer
The concept that these transporters may exist as 2 copies working
together with each other
Monamines are believed to exist as dimers
o SSRIs
o Drug binds to the transporter and inhibits the reuptake of monoamines
They do NOT bind to the substrate site they bind to allosteric site
Substrate site: where the monoamine itself binds to the transporter
o Designed for unipolar depression
Act at SERT, NET and DAT or some combination of these
o “Antidepressant” is misnomer
o Good for treating GAD, social phobia and other anxiety forms
o They help with neuropathic pain and post herpetic neuralgia
o Can improve eating disorders, OCD, trauma and stress related disorders
o We do NOT use agents that block monoamine transporters in bipolar or mixed
states
SLC6 and SLC1 Gene Family as Targets of Psychotropic Drugs
o GABA
o Transported by the GAT1-4
GAT1-4 is selectively blocked by the anticonvulsant: Tiagabine
Increases synaptic GABA concentrations
o therapeutic actions in anxiety, sleep disorders
No other inhibitors of this transport system are available for clinical use
o Glycine
o Belong to the SLC6 gene family
No drugs on the market to block glycine transporters
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