Date published: 2025-9-13

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OR4X1 Inhibitors

OR4X1 inhibitors encompass a diverse group of compounds that indirectly influence the functional activity of the OR4X1 receptor through various cellular and molecular mechanisms. These compounds do not target OR4X1 directly but rather modulate the signaling pathways and cellular conditions that are essential for OR4X1's functional activity. For instance, caffeine and forskolin both influence the levels of cAMP, a pivotal second messenger in GPCR signaling, but with opposite immediate effects; caffeine reduces cAMP by blocking adenosine receptors, while forskolin increases it by activating adenylyl cyclase. However, both can lead to changes in PKA activity, which can phosphorylate and desensitize GPCRs like OR4X1. Chloroquine's effect, by altering endosomal and lysosomal pH, can impact the maturation and transport of GPCRs, potentially leading to a decreased presence of OR4X1 at the cell surface where it would typically encounter its ligands. Ibuprofen, through its anti-inflammatory action, might indirectly affect OR4X1 signaling by reducing the levels of prostaglandins that can modulate GPCR functionality. Diazepam, through enhancement of GABAergic signaling, contributes to a more inhibited neuronal state, which could indirectly reduce the responsiveness of OR4X1 due to a generally higher threshold for activation of sensory neurons.

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