What is GHB and how does it work? Flashcards
(35 cards)
What is GHB?
A drug that is used as a date rape
What kind of receptor is GABAb?
A GPCR
How does the GABAb system work?
As a dimer (i.e. you need two of them activated to create an effect)
What are the two halves of the dimer that are required to carry out a signal?
- GABAb1
2. GABAb2
What is the function of the GABAb1 receptor?
The activator
What is the function of the GABAb2 receptor?
the signaller
Describe the cascade of GABAb?
GABAb acts on NMDA receptors
- Alpha subunit cleaves; the beta-gamma subunit goes on to negatively influence voltage-gated Ca2+ channels
- alpha subunit acts on Gi pathway (inhibits adenylyl cylcase from making cAMP from ATP)
- NMDA receptor has to be phosphorylated by protein kinase a to be activated
How does the GABAb receptor inhibit the NMDA receptor?
By preventing phosphorylation (therefore it inhibits the excitatory response)
What do presynaptic GABAb receptors prevent?
Ca2+ from causing vesicle to dock and release NTs
What does GHB stand for?
gamma hydroxybuterate
What is GHB synthesized from?
GABA
Describe the synthesis of GHB?
succinic semialdehide makes GHB from GABA
What does a low dose of GHB produce?
Excitement and euphoria (with some memory problems)
What is liquid X?
GHB at low doses (is paired with other club drugs)
What do moderate doses of GHB produce?
More memory problems and sedation
What do high doses of GHB produce?
coma and/or death
Why is GHB effective as a memory impairer in date rape situations (exam question)?
Because the LTP in NMDA receptors is blocked by the GABAb receptor cascade
What is an orphan receptor?
Proteins that act like receptors, but with no known ligand that specifically binds to it
What property can GHB have when it comes to neurotransmission (other than the possibility of it being its own neurotransmitter)?
GHB could be a GABAb co-signaller
What are monoamine neurotransmitters?
They are a class of compounds that have a single amine
What are the two classifications of monoamines?
Catecholamines and 5HTs
What are the catecholamine NTs?
- Dopamine (DA)
- Norepinephrine (NE)
- Epinephrine (Epi)
Is serotonin a catecholamine?
No, but it is a monoamine
What is the technical difference between epinephrine and adrenaline?
Epinephrine is used when referring to the effects in the CNS (i.e. in the brain) and adrenaline is used when referring to the effects in the PNS (i.e. in heart rate, pupil dilation, etc)