醫學二：100題 ( 包括生理學,生化學,藥理學,病理學等科目及其臨床相關知識 )題庫下載題庫

Ans. (A,B)

Clozapine, one of the most effective antipsychotic drugs, has been shown to display moderate affinity for various neurotransmitter receptors, including the dopamine D1 and D2 receptors

Chlorpromazine acts as an antagonist (blocking agent) on different postsynaptic and presynaptic receptors:

Ans. (A,B)

Clozapine, one of the most effective antipsychotic drugs, has been shown to display moderate affinity for various neurotransmitter receptors, including the dopamine D1 and D2 receptors

Chlorpromazine acts as an antagonist (blocking agent) on different postsynaptic and presynaptic receptors:

• Dopamine receptors (subtypes D1, D2, D3 and D4), which account for its different antipsychotic properties on productive and unproductive symptoms, in the mesolimbic dopamine system accounts for the antipsychotic effect whereas the blockade in the nigrostriatal system produces the extrapyramidal effects
• Serotonin receptors (5-HT1 and 5-HT2), with anxiolytic, and antiaggressive properties as well as an attenuation of extrapyramidal side effects, but also leading to weight gain and ejaculation difficulties.
• Histamine receptors (H1 receptors, accounting for sedation, antiemetic effect, vertigo, and weight gain)
• α1- and α2-adrenergic receptors (accounting for sympatholytic properties, lowering of blood pressure, reflex tachycardia, vertigo, sedation, hypersalivation and incontinence as well as sexual dysfunction, but may also attenuate pseudoparkinsonism—controversial. Also associated with weight gain as a result of blockage of the adrenergic alpha 1 receptor)
• M1 and M2 muscarinic acetylcholine receptors (causing anticholinergic symptoms such as dry mouth, blurred vision, constipation, difficulty or inability to urinate, sinus tachycardia, electrocardiographic changes and loss of memory, but the anticholinergic action may attenuate extrapyramidal side effects).

<https://en.wikipedia.org/wiki/Chlorpromazine>

Thioridazine has the following binding profile:[15] 

Haloperidol acts on these receptors: (Ki)

• D1 (silent antagonist) — Unknown efficiency[citation needed]
• D5 (silent antagonist) — Unknown efficiency[citation needed]
• D2 (inverse agonist) — 1.55 nM[44]
• D3 (inverse agonist) — 0.74 nM[45]
• D4 (inverse agonist) — 5–9 nM[46]
• σ1 (irreversible inactivation by haloperidol metabolite HPP+) – 3 nM[47]
• σ2 (agonist): 54 nM[48]
• 5HT1A receptor agonist – 1927 nM[49]
• 5HT2A (silent antagonist) – 53 nM[49]
• 5HT2C (silent antagonist) – 10,000 nM[49]
• 5HT6 (silent antagonist) – 3666 nM[49]
• 5HT7 (irreversible silent antagonist) — 377.2 nM[49]
• H1 (silent antagonist) — 1,800 nM[49]
• M1 (silent antagonist) — 10,000 nM[49]
• α1A (silent antagonist) — 12 nM[49]
• α2A (silent antagonist) — 1130 nM[49]
• α2B (silent antagonist) — 480 nM[49]
• α2C (silent antagonist) — 550 nM[49]
• NR1/NR2B subunit containing NMDA receptor (antagonist; ifenprodil site): IC50 — 2,000 nM[50]

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