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L14 Medicinal Chemistry

Deleted user 11 questions Updated 26 May 2019

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Questions in this quiz (11)

  1. 1“Nor” means desmethyl/minus a methyl group, so noradrenaline is structurally the same as the catecholamine adrenaline, without a methyl group.
    1. ATrue
    2. BFalse
  2. 2Adrenaline is [blank_start]non[blank_end]-selective for adrenoceptor subtypes and [blank_start]short[blank_end] acting. Drugs designed from adrenaline, noradrenaline as a starting point, were designed with:
    – Improved receptor type/subtype [blank_start]selectivity[blank_end]
    – Longer duration of [blank_start]action[blank_end]
    – Improved [blank_start]stability[blank_end] to metabolism
    1. Anon
    2. Bshort
    3. Cselectivity
    4. Daction
    5. Estability
  3. 3Catecholamines have a catechol and an amine group.
    Catechols (two OH groups adjacent on a ring) are extensively [blank_start]metabolised[blank_end] by COMT (catechol-O methyltransferase), so we can change the catechol to make the drug last [blank_start]longer[blank_end].
    We can add an extended chain to the amine, which [blank_start]reduces[blank_end] metabolism by MAO (monoamine oxidase). It can also change molecule structure to [blank_start]match[blank_end] with unique receptor subtype binding pocket shape i.e. we can tune selectivity or [blank_start]affinity[blank_end] for ARs. Adding an extended lipophilic chain gives [blank_start]beta 2[blank_end] AR selectivity and we can tune the duration of action; the longer the [blank_start]lipophilic chain[blank_end] the longer it stays.
    1. Ametabolised
    2. Blonger
    3. Creduces
    4. Dmatch
    5. Eaffinity
    6. Fbeta 2
    7. Glipophilic chain
  4. 4 SABAs – Short Acting Beta Agonists, are selective for beta-ARs over alpha-ARs, and more selective for [blank_start]beta 2[blank_end] ARs than [blank_start]beta 1[blank_end] ARs.
    They have a fast [blank_start]onset[blank_end] of action, and a duration of action [blank_start]4-6[blank_end] hours, which is longer than endogenous agonists.
    – Catechol group no longer there, reduces [blank_start]COMT metabolism[blank_end]
    – Bulky N-alkyl group, reduces [blank_start]MAO metabolism[blank_end]
    Most marketed drugs targeting β-AR are a [blank_start]racemic[blank_end] mixture.
    1. Abeta 2
    2. Bbeta 1
    3. Conset
    4. D4-6
    5. ECOMT metabolism
    6. FMAO metabolism
    7. Gracemic
  5. 5 LABAs – Long Acting Beta Agonists, e.g. [blank_start]salmeterol[blank_end], have a long chain/lipophilic N-substituent which [blank_start]associates[blank_end] with membrane. The drug is ‘anchored’ close to orthosteric [blank_start]binding[blank_end] site, giving a longer [blank_start]duration of action[blank_end].
    Since LABAs are more lipophilic than SABAs their [blank_start]clogP[blank_end] is higher.
    1. Asalmeterol
    2. Bassociates
    3. Cbinding
    4. Dduration of action
    5. EclogP
  6. 6Beta agonists have an amine that would be [blank_start]ionised[blank_end] at physiological pH, and therefore are formulated as [blank_start]salts[blank_end].
    E.g. Terbutaline and salbutamol as sulfate salt, formoterol as fumarate dihydrate salt, salmeterol as the xinafoate salt.
    These salts are more [blank_start]lipophilic[blank_end] than salts like HCl, and have better [blank_start]membrane[blank_end] retention.
    1. Aionised
    2. Bsalts
    3. Clipophilic
    4. Dmembrane
  7. 7There are 5 muscarinic GPCR subtypes – M1, M2, M3, M4, M5, also known as ‘muscarinic acetylcholine receptors’ or ‘mAChRs'. The endogenous agonist is [blank_start]acetylcholine[blank_end] (ACh).
    ACh and acts directly at mAChRs on airway [blank_start]smooth[blank_end] muscle to cause
    [blank_start]bronchoconstriction[blank_end] (in particular via [blank_start]M1, M2, M3[blank_end] subtypes). For asthma, bronchodilation can be provided by using an [blank_start]antagonist[blank_end] drug to block effects of [blank_start]endogenous[blank_end] ACh.
    1. Aacetylcholine
    2. Bsmooth
    3. Cbronchoconstriction
    4. DM1, M2, M3
    5. EM4, M5
    6. Fantagonist
    7. Gendogenous
  8. 8Atropine is a typical antimuscarinic, but is not selective and has side effects.
    1. ATrue
    2. BFalse
  9. 9 SAMAs – Short Acting Muscarinic Antagonists, are [blank_start]non-selective[blank_end] across
    M receptor subtypes. They have a quick, [blank_start]15[blank_end] min onset, a duration less than [blank_start]4[blank_end] hours, and provide [blank_start]short term[blank_end] relief. An example is ipratropium bromide.
    IB systemic exposure is very [blank_start]limited[blank_end] due the drug’s physicochemical properties. A permanent [blank_start]positive[blank_end] charge limits its diffusion across [blank_start]membranes[blank_end] and into systemic circulation(this also means it has poor [blank_start]oral[blank_end] bioavailability, but when administering to the airways this is not a big problem).
    1. Anon-selective
    2. B15
    3. C4
    4. Dshort term
    5. Elimited
    6. Fpositive
    7. Gmembranes
    8. Horal
  10. 10LAMAs, Long Acting Muscarinic Antagonists, are long acting for [blank_start]kinetic[blank_end] reasons. They have very slow [blank_start]off binding[blank_end] from the M receptor, in particular the M3 subtype. Their clogPs are [blank_start]similar[blank_end] to SAMAs and their systemic exposure is limited due to a permanently [blank_start]positively[blank_end] charged nitrogen.
    1. Akinetic
    2. Boff binding
    3. Csimilar
    4. Dpositively

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User has deleted their subject information Quiz on L14 Medicinal Chemistry, created by Deleted user on 14/04/2019.
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Created on 14 Apr 2019 · updated on 26 May 2019
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