PHRM 311 Lecture Notes - Lecture 13: Hyperprolactinaemia, Structural Analog, Weight Gain
Document Summary
Acts as an antagonist with greatest affinity toward 5-ht2a, 5-ht2c, 5-ht6, 5-ht7, a1, muscarinic, & h1 gpcrs . First atypical antipsychotic drug with minimal extrapyramidal side effects. Its success provided impetus to target receptors other than or in addition to. Weight gain due to h1 & 5-ht2c gpcr interactions. Similar structurally & functionally to clozapine (i. e. similar gpcr binding profile) to clozapine. Higher d2 & 5-ht2a gpcr affinity than clozapine. Exhibits a similar gpcr binding profile as clozapine with some exceptions. Selectivity toward m1 vs other muscarinic receptors, overall low. Selectivity toward 5-ht2a versus 5-ht2c intermediate weight gain compared to others. High affinity for 5-ht2a, h1, alpha-1 gpcrs. No affinity toward muscarinic receptors , modest affinity toward 5-ht2c. 5-ht1a partial agonist activity, and no affinity toward muscarinic receptors. Despite affinity toward 5-ht2c & h1 gpcrs, low propensity for weight gain. Lack muscarinic receptor affinity (like risperidone & ziprasidone)
