L7 Flashcards
Meyer-Overton rule
Predicts ‘penetration of drugs/anaesthetics’
What can penetrate the lipid bilayer?
Hydrophobic molecules –> High P (lipids & gases)
Small, uncharged polar –> modest P (H2O)
Large, uncharged polar –> LOW glucose & amino acids
IONS –> NONE
Cocaine
weak base
What is membrane solubility proportional to?
oil
biological membrane permeability- when do they become permable?
simple diffusion = linear
protein mediate = curve that plateaus
ion channels become permeable at >160mM
integral membrane proteins
amino acids adjacent to lipid bilayer = lipophilic
hydrophilic pore region lined with charged amino acid –> route of permeation!
ion pumps
one or more substrate transported (at least one against gradient)
pumps have enzymatic activity (ATPase) to hydrolyse ATP to release energy for ion transport (primary AT)
Solute carriers
one or more substrate transported (at least one DOWN gradient)
V diverse, >400 genes in 66 carriers. 2nd most diverse group
what do SLC’s use
- facilitated diffusion
- Co-transporters/symporters
- Exchangers/antiport
What drugs in the brian target SLCs?
Amphetamines and SSRI’s