Lecture 5 Flashcards
Targets of psychiatric drugs
G-protein coupled receptors Ligand-gated ion channels Voltage gated ion channels Enzymes 12-transmembrane domain transporteers
Reuptake Pumps
Plasma membrane transporters; transport neurotransmitters from the extracellular space into the cytoplasm of the presynaptic terminals
i.e. SERT, NET, DAT
Vesicular Transporters
Transport neurotransmitters from the cytoplasm to the vesicles.
i.e. Vesicular monoamine transmitter VMAT
Cofactor for reuptake pumps?
Sodium
Fluoxetine
Acts at the SERT
Are not carried into the presynaptic terminal they remain bound to SERT
AChE
Acetylcholinesterase; rapidly breaks fown ACh into choline and acetate . Choline transporter then pumps choline in to the terminal and converted to AChE.
VAChT
Vesicular ACh transporter
GAT
GABA transporter
EAAT
Excitatory amino acid transporter
VGlu
vesicular glutamate transporter
VIAAT
Vesicular inhibitory amino acid transporter
Full Agonist
Completely activate i.e. morphine is a full agonist at mu opioid receptors
Partial agonist
Partial agonists activate signaling to limiting degree
i.e. chantix at nicotinic ACh receptors
Antagonists
Block the ability of neurotransmitters or other agonists to activate but constitutive activity is still present
i.e. naltrexone is a opioid receptor antagonist
Inverse agonist
Stops all GPCR activity
i.e. cetrizine at H1 histamine receptors