Oxytocin GPCR Assays
Background of Oxytocin Receptor (OTR)
The OTR is a class A G protein-coupled receptor (GPCR) that is a key receptor system for childbirth and breastfeeding. It is activated by its endogenous ligand oxytocin (OT). The OT/OTR signaling system is widely distributed that regulates many aspects of mammalian reproduction. In addition, OT/OTR regulation has many implications for complex social behaviors such as parenting.
Fig.1 OTR analogues activate single G protein subtypes. (Busnelli, 2017)
Crucial Roles of OTR
OTR is closely associated with a variety of different physiological responses, including lactation, stress, luteolysis, uterine contractions, smooth muscle cell contraction, and cardiovascular homeostasis. In addition, studies discovered that OTR is involved in the regulation of social, reproductive, and aggressive behaviors. Notably, Emerging evidence points to the significant role of OTR in breast cancer development. and thus, OTR is also a promising target for cancer therapy.
OTR Related Mechanisms
To date, only one OTR has been identified. The main mechanisms and related pathways of OTR are summarized in the table below.
| Receptor | Gene | Mechanism | Agonists | Antagonists |
| Oxytocin Receptor | OXTR |
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Assay List of Oxytocin Receptor
Creative Biolabs can provide a range of assays of oxytocin receptor. You can choose the assay in the list or contact us for more information:
Published Data
| Paper Title |
A Nonpeptide Oxytocin Receptor Agonist for a Durable Relief of Inflammatory Pain |
| Journal |
Scientific reports |
| Published | 2020 |
| Abstract |
Oxytocin has a variety of physiological and social functions, especially analgesia, through binding to OTR. However, oxytocin has the disadvantages of a short half-life, poor specificity, and extremely poor oral absorption and distribution, so oxytocin is usually not used for pain treatment. Recently, a low molecular weight non-peptide full agonist of the OTR (LIT-001) has been synthesized, which promotes social interaction after peripheral administration. This study proposed that a single intraperitoneal administration of LIT-001 in a rat model can effectively alleviate the symptoms of hyperalgesia caused by inflammatory pain, providing a new idea for the development of original drugs for pain treatment. |
| Result |
Studies have demonstrated that LIT-001 is a specific OTR agonist with significant and durable antihyperalgesic effects on both mechanical and thermal sensitivity. Second, LIT-001 played a positive role in enhancing social interaction in a mouse model of autism. In addition, the researchers demonstrated that LIT-001 can cross the blood-brain barrier and exert effects on the central nervous system. Notably, LIT-001 does not accumulate in the body and is excreted through the urine. In conclusion, LIT-001 is a very promising probe that plays a crucial role in validating the OTR as a target for the treatment of pain.
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Fig.2 Dose-response of the analgesic properties of LIT-001 on CFA-induced inflammatory pain model. (Hilfiger, 2020)
References
- Busnelli, M.; Chini, B. Molecular basis of oxytocin receptor signaling in the brain: what we know and what we need to know. Behavioral Pharmacology of Neuropeptides: Oxytocin. 2017: 3-29.
- Hilfiger, L.; et al. A Nonpeptide Oxytocin Receptor Agonist for a Durable Relief of Inflammatory Pain. Scientific reports. 2020; 10(1): 1-10.
