Date published: 2025-9-21

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D5DR Activators

The chemical class of D5DR Activators primarily includes compounds that modulate the dopaminergic system, either by directly activating dopamine receptors or by increasing the availability of dopamine in the synaptic cleft. This class is characterized by a diverse range of mechanisms, each contributing to the enhancement of dopamine receptor activity, including D5DR. Dopamine precursors like L-DOPA and levodopa are foundational in this class, as they are metabolized into dopamine, subsequently increasing the activation potential of D5DR. Dopamine agonists such as bromocriptine, ropinirole, pramipexole, and apomorphine directly interact with dopamine receptors, with potential cross-reactivity or indirect effects on D5DR. These agonists vary in their selectivity, with some showing higher affinity for D2/D3 receptors but still capable of influencing D5DR through overall enhanced dopaminergic signaling. Additionally, compounds that inhibit dopamine breakdown or reuptake, such as amantadine, selegiline, rasagiline, entacapone, and tolcapone, play a crucial role. By increasing the availability of dopamine, they indirectly potentiate D5DR activation. These inhibitors work by targeting enzymes like monoamine oxidase B (MAO-B) or catechol-O-methyltransferase (COMT), crucial in the catabolism of dopamine.

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