Principles of Pharmacology 1
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AFFINITY
refers to the strength of the drug-receptor interaction
what type of biomolecules are receptors
proteins
how many types of receptors do we have, name them
4 Ligand-gated ion channel (ionotropic) receptors G-protein coupled (metabotropic) receptors Kinase-linked receptors Nuclear receptors
Lipophobic Lipophilic
substances or molecules that are not soluble in or repel lipids (fats and oils) substances or molecules that are soluble in lipids and tend to interact with fats and oils
which receptors in the cell do lipophilic signal molecules bind to
these molecules diffuse through the cell and bind to cytosolic or nuclear receptors
which receptors in the cell can lipophobic and lipophilic signal molecules bind to
receptors on the cell membrane
hormones
Molecules Released from one cell into extracellular space/circulation to travel to a new site of action where they provoke a specific response
in which neurons are neurotransmitters synthesized
in the pre-synaptic neuron
exocytosis
Exocytosis is a cellular process that involves the release of substances from a cell by the fusion of membrane-bound vesicles with the cell membrane (plasma membrane)
name 5 types of neurotransmitters
acetylcholine monoamines (noradrenaline, dopamine) amino acids neuropeptides (endorphins) purines soluble gases (nitric oxide)
name some amino acids that can act as neurotransmitters
GABA and Glutamate
which types of molecules act as the major inhibitory and excitatory neurotransmitters in the CNS
amino acids
Neurotransmitters cannot stay in the synapse for too long. what happens to neurotransmitters after they have carried out their function?
they are reabsorbed by transporter proteins on the pre-synaptic membrane. once reabsorbed they can be repackaged for reuse or broken down. Some neurotransmitters simply diffuse away from the synaptic cleft and are absorbed by nearby cells or the bloodstream. Some neurotransmitters are broken down by enzymes present in the synaptic cleft. The most well-known example of this process involves acetylcholine, which is broken down by the enzyme acetylcholinesterase. (enzymatic degradation)
why are some neurotransmitters broken down in the synaptic cleft
prevents the continued stimulation of the postsynaptic neuron.
which amino acid constitutes 40% of inhibitory transmission which amino acid constitutes 50% of excitatory transmission
GABA Glutamate
how many types of extra-cellular receptors are there, name them name the intra-cellular receptor present in human cells
3 ligand-gated channel receptors kinase-linked(tyrosine kinase) receptors G-protein coupled receptors nuclear receptors
what kind of drugs are extracellular receptors for
hydrophilic(lipophobic) and large drugs
what kind of drugs are intracellular receptors for
hydrophobic(lipophilic) and small drugs
drugs with high affinity have high potency, true or false
Not necessarily true, so false