CYP2D9 Inibidores

Os inibidores comuns da CYP2D9 incluem, entre outros, a quinidina CAS 56-54-2, a fluoxetina CAS 54910-89-3, a paroxetina CAS 61869-08-7, a amiodarona CAS 1951-25-3 e o haloperidol CAS 52-86-8.

The chemical inhibitors of CYP2D9 have a series of mechanisms by which they directly bind to and inhibit the enzyme's activity. Quinidine, for example, is a stereoisomer that targets the active site of CYP2D9, effectively preventing the metabolism of the enzyme's substrates by binding to the site where these reactions normally take place. Similarly, the antidepressant fluoxetine has a competitive inhibition with CYP2D9, occupying the active site and competing with the enzyme's natural substrates, thus reducing the enzyme's ability to process these substrates. Paroxetine, another antidepressant, binds to the same critical active site on CYP2D9, leading to a decrease in the enzyme's metabolic activity by blocking the site required for enzyme function.

The impact of other inhibitors, such as ajmalicine, an alkaloid, also involves the CYP2D9 active site, where it binds and prevents the enzyme from metabolizing its substrates. Amiodarone inhibits CYP2D9 by a similar mechanism, targeting the active site and thus interfering with the enzyme's normal function. Haloperidol, an antipsychotic, and ritonavir, a compound with antiviral properties, both inhibit CYP2D9 through direct interaction with the enzyme's active site, which in turn prevents the metabolic processing for which CYP2D9 is responsible. Antihistamines, such as diphenhydramine and chlorpheniramine, inhibit CYP2D9 by binding to the active site and reducing the enzyme's ability to carry out its normal metabolic processes. On the other hand, bupropion and sertraline, both antidepressants, directly inhibit CYP2D9 by occupying its active site, thus hindering the enzyme's metabolic activity. Finally, methadone, an opiate analgesic, binds to the active site of CYP2D9, acting as a blocker and thus inhibiting the metabolic activity that would normally be facilitated by this enzyme. Among these chemicals, each has a specific inhibitory action on CYP2D9, interacting directly with the enzyme's active site, which is essential for its metabolic function.