Ac-RYYRIK-NH2 is a hexapeptide that has garnered significant attention due to its interaction with the nociceptin/orphanin FQ (N/OFQ) peptide receptor (NOP), a G protein-coupled receptor (GPCR) related to the opioid receptor family. The NOP receptor and its endogenous ligand, nociceptin, are implicated in various physiological processes, including pain modulation, cardiovascular function, and stress response. As such, Ac-RYYRIK-NH2 and its derivatives have been studied for their potential as therapeutic agents in treating conditions such as pain, cardiac dysfunctions, and mood disorders12345678910.
Ac-RYYRIK-NH2 and its derivatives have been explored as potential analgesic and antineuropathic drugs due to their interaction with the NOP receptor6. The peptide library-based antagonist Ac-RYYRIK-NH2 inhibits nociceptin activity mediated through ORL1 but retains a high level of agonist activity6. Structural modifications have led to the development of analogs with enhanced receptor-binding affinity and strong antagonist activity, which could be beneficial in treating pain610.
The ability of Ac-RYYRIK-NH2 to inhibit the chronotropic effect of nociceptin on cardiomyocytes points to its potential application in cardiovascular research1. By modulating the NOP receptor activity, Ac-RYYRIK-NH2 could influence heart rate and rhythm, providing a basis for developing treatments for cardiac dysfunctions.
Ac-RYYRIK-NH2 has been shown to affect behaviors related to mood and stress response. For instance, it can inhibit locomotor activity and stimulate food intake after supraspinal administration in mice3. Additionally, it has been reported to reverse the antidepressant-like effects elicited by NOP receptor selective antagonists in the forced swimming test3. These findings suggest that Ac-RYYRIK-NH2 and its analogs could be useful in studying and potentially treating mood disorders.
Despite its antagonistic properties in other systems, Ac-RYYRIK-NH2 does not antagonize the prolactin secretory activity of nociceptin. Instead, it has been found to increase the magnitude and duration of the prolactin secretory response in female rats, indicating agonist activity in the endocrine system5.
Ac-RYYRIK-NH2 has been characterized as a partial agonist at the NOP receptor when expressed in Chinese hamster ovary (CHO) cells14. It competitively antagonizes the effects of nociceptin in rat brain membranes, inhibiting the stimulation of GTP binding by nociceptin with high affinity and specificity1. This antagonism is not observed with agonists for other opioid receptors, indicating a selective action for the NOP receptor1. Additionally, Ac-RYYRIK-NH2 has been shown to inhibit the chronotropic effects of nociceptin on neonatal rat cardiomyocytes, suggesting a potential role in modulating cardiac function1. However, the peptide also exhibits agonistic properties, as seen by its ability to inhibit spontaneous locomotor activity in mice, an effect additive to that of nociceptin4. The complexity of its pharmacological profile is further highlighted by its variable behavior as an antagonist or agonist depending on the system studied478.
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