2. Signaling Pathways
  3. GPCR/G Protein
  4. Neuropeptide S Receptor

Neuropeptide S Receptor

Neuropeptide S Receptor; NPSR; GPR154; Vasopressin receptor-related receptor 1; VRR1

Neuropeptide S Receptor (NPSR) is a member of the G protein-coupled receptor (GPCR) superfamily and serves as the specific receptor for neuropeptide S (NPS). Upon binding to NPS, which occurs with high affinity, NPSR activates both Gq and Gs proteins, resulting in increased intracellular calcium levels and cyclic adenosine monophosphate (cAMP) accumulation. NPSR is predominantly expressed in brain regions associated with anxiety and stress responses, including the amygdaloid complex, paraventricular hypothalamic nucleus, and hippocampus. This receptor plays significant roles in various physiological processes, including inflammation, nociception, locomotor activity, wakefulness, anxiety regulation, and food intake, and is particularly implicated in the pathogenesis of asthma[1][2].

Neuropeptide S Receptor Related Products (3):

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-108625
    SHA 68
    		Antagonist 99.84%
    SHA 68 is a potent and selective non-peptide neuropeptide S receptor (NPSR) antagonist with IC50s of 22.0 and 23.8 nM for NPSR Asn107 and NPSR Ile107, respectively. SHA 68 has limited the blood-brain barrier (BBB) penetration and the activity in neuralgia.
    SHA 68
  • HY-108626
    ML154
    		Antagonist 99.59%
    ML154 (NCGC84) is a selective, brain-penetrant and non-peptide neuropeptide S receptor (NPSR) antagonist with a pA2 of 9.98. ML154 potently inhibits NPS-stimulated cellular calcium, cAMP, and ERK phosphorylation responses with IC50 values of 36.5 nM, 22.1 nM, and 9.3 nM, respectively.
    ML154
  • HY-P1437A
    Neuropeptide S(Mouse) TFA
    		Agonist
    Neuropeptide S(Mouse) TFA is a potent endogenous neuropeptide S receptor (NPSR) agonist (EC50=3 nM). Neuropeptide S(Mouse) TFA induces mobilization of intracellular Ca2+. Neuropeptide S(Mouse) TFA increases locomotor activity and wakefulness in mice. Neuropeptide S(Mouse) TFA also reduces anxiety-like behavior in mice.
    Neuropeptide S(Mouse) TFA