Opioid receptors are a subtype of GPCRs and play a crucial role in the human body's reaction to various neurotransmitters, hormones, and medications. Currently, there are five known kinds of opioid receptors: MOR, KOR, DOR, NOR, and ZOR. Moreover, the various types of opioid receptors selectively bind to their corresponding agonist molecules. Notably, opioid receptors have been linked to a variety of disorders, including immunological dysfunction, endocrine abnormalities, and so on. Consequently, identifying the opioid receptors is beneficial for drug development.
Fig.1 The role of opioid receptors in physiology and addiction.1
Innovatively, Creative Biolabs succeeded in developing Magic™ in vitro cell-based opioid receptor functional assay service. Through examining the accumulation of second messengers like cAMP, ion flux in cellular, and internalization of opioid receptors, our Magic™ in vitro cell-based opioid receptor functional assay service has the ability to identify candidate samples and their capacity to regulate opioid receptors. Our assay incorporates the highlights of cell-based in vitro assay, which will rapidly and dependably achieve the desirable outcomes for global customers. Besides, we provide comprehensive customized services to ensure each project is implemented smoothly. Cordially welcome global customers to inquire and order.
Fig.2 Opioid receptors in neurotransmission regulation.2
Background: KOR antagonists provide new insights into the treatment of neurological illnesses. Although Compound A, the novel scaffold opioid ligand, initially was demonstrated to be an antagonist of the MOR, its binding, selectivity, and activation profile at the DOR and KOR are yet a mystery.
Methods: In order to identify Compound A as a KOR antagonist, an in vitro radioligand competitive binding assay, in vivo activity assays in mice, and in silico research were carried out.
Results: The results of functional in vitro assays indicated that Compound A shows an advantageous KOR selectivity profile. The results of in vivo assay and in silico research demonstrated that Compound A was identified as a new KOR antagonist.
Fig.3 Compound A's in vitro activity profile at the human KOR.3
Background: Safer analgesics may be found by the manipulation of opioid receptor functional selectivity profiles, however, it is not yet clear which structural variables are responsible for this.
Methods: Crystal structures of opioid receptors, including MP1104, MP1207, and MP1208, were utilized to rationally construct new combined MOR and KOR agonists with decreased arrestin activity and verify them.
Results: The findings support a new approach that takes inspiration from the structure of molecules to achieve positive effects on pain relief in living organisms. This could be accomplished through various mechanisms, such as bias, partial agonism, and the activation of both MOR and KOR receptors.
Fig.4 For cAMP inhibition, MP1104 is a complete agonist at hMOR.4
Continuously, in light of valuable input from our global customers, Creative Biolabs remains dedicated to advancing and revolutionizing our cutting-edge technological breakthroughs. If you are attracted by our Magic™ in vitro cell-based opioid receptor functional assay service, please feel free to contact us.
References
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