Shengs slides 1-3-2024 Flashcards
med/chem drug development
what makes up the peripheral nervous system
Autonomic and somatic
what is the definition of medicinal chemistry?
medicinal chemistry concerns with the discovery , the development, the interpretation of the mode of action of biologically active compounds at the molecular level.
[ interest in bioactive compounds and metabolic products]
what makes up the somatic nervous system ?
sensory and motor
what makes up the autonomic nervous system?
sympathetic and parasympathetic
what are 4 different types of receptors ?
- Ion channel
- G protein coupled receptor
- Receptor tyrosine kinase
- Nuclear receptor
what are the excitatory amino acids of ligand gated ion channels?
glutamate and aspartate
what are the inhibitory amino acids of ligand gated ion channels?
GABA
what are 6 antagonist and their matching agonist counterpart in terms of the receptor they act on?
- Atropine and Pilocarpine
2.Naloxone and Fentanyl - Metoclopramide and pergolide
4.Flumazenil and Benzodiazepine
5.Tamsulosin and Phenylephrine - Flutamide and Estradiol
what are the neurotransmitters of catecholamines ?
Dopamine derivatives and epinephrine derivatives
what is the substrate and drug examples for the enzyme acetylcholinesterase ?
- Substrate: Acetylcholine
- Drugs: Acetylcholinesterase inhibitors: Donepezil, rivastigmine, galantamine
what is the substrate and drug examples for the enzyme catechol-o-methyltransferase (COMT)?
- Substrate: Catechols such as levodopa
- Drugs: COMT inhibitors: entacapone
what is the substrate and drug examples for the enzyme cyclooxygenase (COX)?
- Substrate: arachidonic acid
- Drugs: NSAIDS
what is the substrate and drug examples for the enzyme monoamine oxidase (MAO) ?
- catecholamines: DA,NE,EPI, 5-HT
- Drugs: MOA inhibitors: Phenelzine, tranylcypromine, isocarboxazid, selegiline, rasagiline, methylene
which amino acid is the precursor of epinephrine ?
tyrosine
what is the cellular membrane resting potential vm of neurons ?
between -60 mv to -80 mv
which type of cell has measurable membrane potential?
Neurons cells
what are the 3 fiber types of impulse propagation ?
Impulse propagation is all or none
1. A fibers: the largest 5-20 microns and 130m/second, myelinated node for the transmission of the somatic sensory and motor neurons linked to skeletal muscle
2. B fibers: the medium 2-3 microns and 15m/second, myelinated ones for visceral sensory and autonomic preganglionic neurotransmission
3. C fibers: the smallest 0.5-1.5 m/seconds, unmyelinated ones for sensory and autonomic motor transmission
what is oxidation?
- Loss of electrons
- Oxidation number increases
- Loss of hydrogen or gain of oxygen
what is reduction?
- Gain of electrons
- Oxidation number decreases (reduces)
- Gain of H or loss of oxygen
what are the rules of oxidation number states for carbon?
- Carbon-carbon (C-C) bond, the oxidation state for each carbon atom is considered to be 0.
2.C-X, (X is More Electronegative) = -1 per Bond: When carbon is bonded to a more electronegative atom (denoted as X), the carbon is assigned an oxidation number of -1 for each bond.
3.C-H bond, carbon is assigned an oxidation number of +1.
4.To determine the overall oxidation state of carbon in a molecule, you sum up the individual oxidation numbers assigned based on the rules mentioned above for all atoms directly attached to the carbon.
5.Oxygen is Always -2:
6.Oxygen Gas = 0:
What would be the appropriate cytochrome p450 nomenclature for “CYP2G1”
- Family: 2
- Subfamily: 2G
3.Individual isoenzyme number within the CYP subfamily: CYP2G1
