BCH 261 Lecture Notes - Lecture 2: Covalent Bond, Gtpase, Morphine

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30 Nov 2020
Lecture 2
What makes fentanyl and other opioids so good at binding mu-opioid receptors?
Fentanyl and other opioids bind to μ-opioid receptors by non-covalent
interactions (in brain cells, but also elsewhere in the body)
Fentayl binding to μ-opioid receptors causes receptor activation
which activates GTPase proteins that in turn lead to changes in
neurons where the end result is a reduction in the sensation of pain.
Why is fentanyl so dangerous?
It binds more tightly to mu-opioid receptors than morphine and much, much
more tightly than natural brain hormones
So, very low doses of fentanyl cause maximal binding to mu-opioid receptor Mu-
opioid receptors not only control pain sensation, but also things like
breathing, cardiac function - > too much Mu-opioid receptor activation ->
cardiac or respiratory arrest (overdose)
- Cells with only covalent bonds = dead
- Used to fixate cells
- Molecular Interactions are attractive forces b/w molecules & between non-
bonded atoms
- Molecular interactions are NOT bonds
- Bonds hold atoms together within molecule
- Non-covalent interactions act in range that is limited by their packing
radius (van der Waals radius)
Water & its properties
- Water is polarized
- Up to 4 H bonds per water molecule
- High boiling & melting temperature
- Universal solvent of polar solutes
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