What is EC50
The concentration of a drug that gives a half maximal response
- only in agonists
- has to do w efficacy
What is the Hill Langmuir equation (Breustedt)
pAR = [A] / [K] + Ka
-50% occupancy when [A] = Ka
Biotransformation: phase 1
Introduce/recover reactionary groups
- oxidation
- reduction
- hydrolysis
- hydratization
Biotransformation: phase 2
Conjugation reaction
- glucuronation
- sulfatation
- methylation
- acetylation
What is Kd?
Drug concentration where half of the binding sites are occupied
-dissoc constant
Lower order biomolecules
- sugars (carbohydrates)
- peptides
- lipids
- heterocylic compounds
Medium order biomolecules
- nucleotides
- peptides (opiates)
Higher order biomolecules
- proteins
- DNA,RNA
Purinergic synapse
- ATP —> activates P2Y (coupled to Gq) and P2X (excitatory)
- Adenosine —> activates A1 and A2 —> cAMP pathway
Glutamate…
Metabolism:
- from alpha-ketoglutarate or glutamine
- enzymes: amino transferase or PAG
Storage:
vGluT
-gets energy from mostly electrochemical gradient
Inactivation:
EAAT
Recycling:
-direct or via Glia-Gln shuttle
GABA…
Synthesis:
-from glutamate/glutamine —> GABA via enzymes GAD65 and 67
Storage:
VIAAT
-driven by equally electrochemical and pH gradient
Inactivation:
GAT1-3 (in neurons and glia)
GHB - agonist of GABAbR
ACh…
Synthesis:
- from choline and Acetyl CoA —> ACh via enzyme choline acetyl transferase
- degraded by enzyme acetylcholinesterase
Storage:
VAT (VMAT and VAChT)
-driven by pH gradient (H+ antiport)
Inactivation:
enzyme Acetylcholinesterase
Recycling:
Choline
Catecholamines…
Metabolism:
-enzyme TH
L tyrosine —> LDOPA —> DA —> NE —> EPi
Storage:
VMAT
Reuptake:
DAT
NET
Inactivation:
MAO and COMT
5HT…
Synthesis:
-enzymes: TPH(TrypOHase) and LAADC
Storage:
VMAT
Inactivation:
MAO and COMT
