Shengs slides 1-3-2024 Flashcards

med/chem drug development

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1
Q

what makes up the peripheral nervous system

A

Autonomic and somatic

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2
Q

what is the definition of medicinal chemistry?

A

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]

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3
Q

what makes up the somatic nervous system ?

A

sensory and motor

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4
Q

what makes up the autonomic nervous system?

A

sympathetic and parasympathetic

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5
Q

what are 4 different types of receptors ?

A
  1. Ion channel
  2. G protein coupled receptor
  3. Receptor tyrosine kinase
  4. Nuclear receptor
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6
Q

what are the excitatory amino acids of ligand gated ion channels?

A

glutamate and aspartate

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7
Q

what are the inhibitory amino acids of ligand gated ion channels?

A

GABA

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8
Q

what are 6 antagonist and their matching agonist counterpart in terms of the receptor they act on?

A
  1. Atropine and Pilocarpine
    2.Naloxone and Fentanyl
  2. Metoclopramide and pergolide
    4.Flumazenil and Benzodiazepine
    5.Tamsulosin and Phenylephrine
  3. Flutamide and Estradiol
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9
Q

what are the neurotransmitters of catecholamines ?

A

Dopamine derivatives and epinephrine derivatives

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10
Q

what is the substrate and drug examples for the enzyme acetylcholinesterase ?

A
  1. Substrate: Acetylcholine
  2. Drugs: Acetylcholinesterase inhibitors: Donepezil, rivastigmine, galantamine
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11
Q

what is the substrate and drug examples for the enzyme catechol-o-methyltransferase (COMT)?

A
  1. Substrate: Catechols such as levodopa
  2. Drugs: COMT inhibitors: entacapone
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12
Q

what is the substrate and drug examples for the enzyme cyclooxygenase (COX)?

A
  1. Substrate: arachidonic acid
  2. Drugs: NSAIDS
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13
Q

what is the substrate and drug examples for the enzyme monoamine oxidase (MAO) ?

A
  1. catecholamines: DA,NE,EPI, 5-HT
  2. Drugs: MOA inhibitors: Phenelzine, tranylcypromine, isocarboxazid, selegiline, rasagiline, methylene
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14
Q

which amino acid is the precursor of epinephrine ?

A

tyrosine

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15
Q

what is the cellular membrane resting potential vm of neurons ?

A

between -60 mv to -80 mv

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16
Q

which type of cell has measurable membrane potential?

A

Neurons cells

17
Q

what are the 3 fiber types of impulse propagation ?

A

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

18
Q

what is oxidation?

A
  1. Loss of electrons
  2. Oxidation number increases
  3. Loss of hydrogen or gain of oxygen
19
Q

what is reduction?

A
  1. Gain of electrons
  2. Oxidation number decreases (reduces)
  3. Gain of H or loss of oxygen
20
Q

what are the rules of oxidation number states for carbon?

A
  1. 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:
21
Q

What would be the appropriate cytochrome p450 nomenclature for “CYP2G1”

A
  1. Family: 2
  2. Subfamily: 2G
    3.Individual isoenzyme number within the CYP subfamily: CYP2G1