Mas-related G-protein-coupled Receptor (MRGPR) Agonist

(R)-ZINC-3573 is a selective Mas-related G protein-coupled receptor X2 (MRGPRX2) agonist with an EC₅₀ value of 740 nM. (R)-ZINC-3573 can be used as a MRGPRX2 probe for the research of pain and itch.

PAMP-12(human, porcine) is a major component of immunoreactive (ir)-PAMP, is processed from the adrenomedullin precursor, is a potent hypotensive peptide and participates in cardiovascular control.

MRGPRX1 agonist 1 is a highly potent MRGPRX1 agonist (EC₅₀=50 nM) with greater than 50-fold selectivity for δ, μ, and κ opioid receptors. MRGPRX1 agonist 1 is inactive against MRGPRC11. MRGPRC11 inhibits high voltage-activated (HVA) Ca²⁺ currents, reduces neurotransmitter release, and mitigates nociceptive transmission in the spinal cord. MRGPRX1 agonist 1 is useful for the study of chronic pain, especially neuropathic pain.

CCG258747 is a selective GRK2 inhibitor (IC₅₀ = 18 nM) with high selectivity over GRK1, GRK5, PKA, and ROCK1 (518, 83, > 5500, and > 550-fold, respectively). CCG258747 also blocks the internalization of the µ-opioid receptor (MOR). CCG258747 attenuates IgE mediated anaphylaxis by inhibiting GRK2 and FcεRI signaling pathway but activates mast cells via MRGPRX2 and MRGPRB2. CCG258747 can be used to study diseases related to overexpression of GRK2 (such as heart failure, opioid tolerance).

PSB-22034 (compound 30d) is a selective agonist of MRGPRX4 with EC₅₀s of 11.2 nM and 30.0 nM in Ca²⁺ and β-arrestin experiments, respectively.

EP-3945 is a potent agonist of Mas-related G protein-coupled receptor (MRGPR), more effective than the MRGPRD small molecule agonist β-Alanine (HY-N0230). MRGPR plays a crucial role in inflammatory pruritus and pain sensation. Additionally, MRGPR binds to Gq (MRGPRX2, MRGPRX4, MRGPRX1 couple with Gq; MRGPRX2, MRGPRD couple with Gi), with EP-3945 measured EC₅₀ for Gq being 211.6 nM.

PAMP-12 (unmodified) TFA is an endogenous peptide and is a MrgX2 agonist. PAMP-12 (unmodified) TFA can reduce cAMP accumulation, increase Ca²⁺ levels, enhance beta-arrestin recruitment, decrease IP-1, and increases phosphoERK. PAMP-12 (unmodified) TFA can elicit hypotension through inhibiting catecholamine secretion from sympathetic nerve endings and adrenal chromaffin cells. PAMP-12 (unmodified) TFA can be used for the research of hypotension and ulcerative colitis.

MRGPRX1 agonist 4 (compound 1t) is a potent and orally active Mas-related G protein-coupled receptor X1 (MRGPRX1) positive allosteric modulator with an EC₅₀ value of 0.1 μM. MRGPRX1 agonist 4 has good metabolic stability and oral bioavailability. MRGPRX1 agonist 4 can reduce behavioral heat hypersensitivity in a neuropathic pain model humanized MRGPRX1 mice. MRGPRX1 agonist 4 can be used for researching neuropathic pain.

Neuropeptide AF (cattle), an amidated octadecapeptide, is RFamide neuropeptide. Neuropeptide AF (cattle) acts as a ligand of Mas-related gene receptor A4 (MrgprA4) (Mas-related G-protein-coupled Receptor (MRGPR)) (EC₅₀ of ~60 nM) and MrgprC11 (EC₅₀ of ~300 nM). Neuropeptide AF (cattle) also activate to the G protein-coupled receptors NPFF1 (Neuropeptide Y Receptor) (EC₅₀ of ~25-325 nM) and NPFF2 (EC₅₀ of ~1-5 nM). Neuropeptide AF (cattle) shows anti-opiate and related pain modulation effects.

JHU-58 is a peptidomimetic agonist targeting mouse MRGPRC11 and rat MRGPRC receptors. JHU-58 demonstrates analgesic effects in mouse models of neuropathic pain. JHU-58 is promising for research of neuropathic pain.

MRGPRX1 agonist 2 (compound 1a) is a potent Mas-related G protein-coupled receptor X1 (MRGPRX1) positive allosteric modulator with an EC₅₀ value of 0.48 μM. MRGPRX1 agonist 2 can be used for researching neuropathic pain.

(Rac)-EP-2825 is a Mas-related G-protein coupled receptor D (MRGPRD) modulator. (Rac)-EP-2825 can be used for the research of MRGPRD-dependent conditions.

PAMP-12(human, porcine) TFA is a major component of immunoreactive (ir)-PAMP, is processed from the adrenomedullin precursor, is a potent hypotensive peptide and participates in cardiovascular control.

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

4-Aminobenzimidamide Hydrochloride (Compound 4a) is a MRGPRX1 agonist. 4-Aminobenzimidamide Hydrochloride can be used in the study of MRGPRX1-mediated analgesic effects.

WO-459 is a potent Gpr52 agonist. WO-459 induces dose-dependent elevation of intracellular cAMP in cells expressing Gpr52. WO-459 can be used for the research of Huntington’s disease and psychotic disorders.

LY3325656 is a selective GPR142 receptor agonist. LY3325656 selectively activates GPR142 in humans and mice. LY3325656 enhances glucose-dependent insulin secretion, glucagon secretion, as well as the secretion of incretin hormones GLP-1 and GIP. LY3325656 can be used in research related to type 2 diabetes.