mrgprx1

MRGPRX1 agonist 1 is a highly potent agonist of MRGPRX1 (Mas-related G-protein-coupled receptor X1) with an EC50 of 50 nM.

MRGPRX1 agonist 2 (compound 1a) is a potent positive allosteric modulator of Mas-related G protein-coupled receptor X1 (MRGPRX1) with an EC50 value of 0.48 μM, and has potential for use in neuropathic pain research [1].

MRGPRX1 agonist 3 (compound 1f) is a potent positive allosteric modulator of Mas-related G protein-coupled receptor X1 (MRGPRX1) with an EC50 of 0.22 μM, and it can be used for neuropathic pain research[1].

MRGPRX1 agonist 4 is a potent and orally active Mas-related G protein-coupled receptor X1 (MRGPRX1) positive conformation modulator (EC50: 0.1 μM). MRGPRX1 agonist 4 ameliorated the behavioral thermal allergic response in mice, a model of MRGPRX1 neuropathic pain.

4-Aminobenzimidamide Hydrochloride (Compound 4a) serves as an agonist for MRGPRX1. It is utilized in research focusing on analgesic effects mediated by MRGPRX1.

EP-3945 is an agonist of Mas-related G protein-coupled receptors (MRGPR), exhibiting greater potency than the small molecule agonist β-Alanine targeting MRGPRD. MRGPRs play a crucial role in inflammatory itch and pain perception. These receptors interact with Gq (MRGPRX2, MRGPRX4, and MRGPRX1 are coupled with Gq; MRGPRX2 and MRGPRD couple with Gi), with EP-3945 having an EC50 value of 211.6 nM for Gq.

BCFTP is a potent, orally active, and selective positive allosteric modulator of the human Mas-related G protein-coupled receptor X1 (MrgprX1). It selectively enhances MrgprX1 signaling in HEK293 cells. In a humanized MrgprX1 chronic constriction injury (CCI) mouse model, BCFTP alleviates specific neuropathic pain-related behaviors in an MrgprX1-dependent manner. Additionally, BCFTP synergistically enhances the analgesic effects with psychoactive substances in CCI MrgprX1 mice. This compound can be used for research in neuropathic pain.

Proadrenomedullin N-terminal 12 peptide (PAMP-12), an endogenous fragment originating from the adrenal medulla and spanning amino acids 9-20 of human PAMP-20, plays a role in causing hypotension. It functions as an agonist for the MAS-related G protein-coupled receptor family member X2 (MRGPRX2), inhibiting forskolin-stimulated cAMP accumulation in CHO cells expressing human MRGPRX2 (EC50 = 57.2 nM) and selectively prompting calcium mobilization in these cells (EC50 = 41 nM), but not in cells expressing MRGPRX1, MRGPRX3, or MRGPRX4 at 1 µM. As an antagonist of nicotinic acetylcholine receptors (nAChRs), PAMP-12 obstructs carbachol-triggered catecholamine release and the influx of calcium and sodium (IC50s = 1.3, 0.39, and 0.87 µM, respectively) in primary bovine adrenal chromaffin cells, with no effect on histamine-induced responses (IC50s = >1 µM for all). Additionally, it decreases mean arterial blood pressure in normotensive rats at doses ranging from 10 to 50 nmol/kg.

Endogenous peptide fragment that is a potent agonist for MRGPRX1 (EC50 values are 8 - 150 nM); first isolated from bovine adrenal medulla. Unlike BAM 22P , does not contain the met-enkephalin motif therefore displays no affinity for opioid receptors.