nociception

Neuromedin U, rat acetate is a 23-amino acid brain-gut peptide. Neuromedin U (NMU), through its cognate receptor NMUR2 in the central nervous system, regulates several important physiological functions, including energy balance, stress response, and nociception.

[Leu5]-Enkephalin acetate(58822-25-6 free base) is an endogenous neuropeptide involved in nociception and an agonist of δ-opioid and μ-opioid receptors (Kis = 4.0 and 3.4 nM, respectively)

HS 014 acetate is a potent and selective melanocortin MC4 receptor antagonist (Ki values are 3.16, 108, 54.4 and 694 nM for cloned human MC4, MC1, MC3 and MC5 receptors respectively). Increases food intake in rats and nociception in mice following central

TLQP-21 TFA, a VGF-derived peptide endowed of endocrine and extraendocrine properties, is a potent G-protein-coupled receptor complement-3a receptor1 (C3aR1) agonist (EC50: mouse TLQP-21=10.3 μM; human TLQP-21=68.8μM). TLQP-21 TFA activates C3aR1 to induce an increase of intracellular Ca2+. TLQP-21 TFA is used for the research in regulation of nociception and other relevant physiologic functions[1][2]. TLQP-21 TFA is a peptide of 21 amino acids. At a dose of 3 μM TLQP-21 induces up to ~69% of the corresponding contraction promoted by acetylcholine[1][2]. [1]. Elena Bresciani , et al. TLQP-21, A VGF-Derived Peptide Endowed of Endocrine and Extraendocrine Properties: Focus on In Vitro Calcium Signaling. Int J Mol Sci. 2019 Dec 24;21(1):130. [2]. Cheryl Cero, et al. The TLQP-21 Peptide Activates the G-protein-coupled Receptor C3aR1 via a Folding-Upon-Binding Mechanism. ructure. 2014 Dec 2;22(12):1744-1753.

Scorpion toxin Tf2, a β-scorpion toxin first identified in the venom of the Brazilian scorpion Tityus fasciolatus, acts as an activator of the neuronal voltage-gated sodium (Nav) subtype Nav1.3, associated with epilepsy and nociception. It increases hNav1.3 activation voltage, prompting channel opening at resting membrane potentials [1].

[Tyr8,Nle11] Substance P, an analog of Substance P, is primarily a neuron-secreted peptide participating in diverse biological functions such as nociception and inflammation [1].

Neuromedin U (NMU) is a neuropeptide first demonstrated to drive smooth muscle contraction.1Translated as a 174 amino acid propeptide, NMU is cleaved to different lengths in different animals. It has diverse receptor-mediated rolesin vivo, as it regulates feeding, vasoconstriction, nociception, and bone remodeling and contributes to obesity, cancer and septic shock.2,2NMU-25 is the active form of NMU in humans. It binds with high affinity to receptors on human left ventricle and coronary artery (KDs = 0.26 and 0.11 nM, respectively), eliciting endothelium-independent vasoconstriction.3NMU-25 also suppresses glucose-stimulated insulin secretion in human islets, and this effect is lost in NMU R165W mutants, resulting in early-onset obesity.4 1.Mitchell, J.D., Maguire, J.J., and Davenport, A.P.Emerging pharmacology and physiology of neuromedin U and the structurally related peptide neuromedin SBritish Journal of Pharmacology15887-103(2009) 2.Greenwood, H.C., Bloom, S.R., and Murphy, K.G.Peptides and their potential role in the treatment of diabetes and obesityRev.Diabet.Stud.8(3)355-368(2011) 3.Mitchell, J.D., Maguire, J.J., Kuc, R.E., et al.Expression and vasoconstrictor function of anorexigenic peptides neuromedin U-25 and S in the human cardiovascular systemCardiovascular Research81353-361(2009) 4.Alfa, R.W., Park, S., Skelly, K.R., et al.Suppression of insulin production and secretion by a decretin hormoneCell Metabolism21(2)323-333(2015)

Neuromedin U (rat TFA), a 23-amino acid brain-gut peptide, operates via its specific receptor NMUR2 in the central nervous system to modulate critical physiological processes such as energy homeostasis, stress response, and nociception.

K 41498 is a selective peptide antagonist targeting both corticotropin-releasing factor receptor 2α (CRF2α) and CRF2β, demonstrating high affinity with Kis of 0.66 and 0.62 nM, respectively, in HEK293 cells expressing these human receptors. Its selectivity is evident as it exhibits a significantly reduced affinity for CRF1 receptor (Ki = 425 nM in HEK293 cells expressing the human CRF1 receptor). Additionally, K 41498, when administered intravenously at 1.84 µg/animal, effectively mitigates urocortin-induced hypotension in rats. Furthermore, its intrathecal delivery ranging from 0.075 to 0.5 µmol/animal significantly lowers the mechanical paw withdrawal threshold in a rat model, indicating its potential utility in managing nociception triggered by complete Freund's adjuvant.

Potent and selective melanocortin MC4 receptor antagonist (Ki values are 3.16, 108, 54.4 and 694 nM for cloned human MC4, MC1, MC3 and MC5 receptors respectively). Increases food intake in rats and nociception in mice following central administration in v

Neuromedin U,a 23-amino acid brain-gut peptide, regulates several important physiological functions through its cognate receptor NMUR2 in the central nervous system, including energy balance, stress response, and nociception.

[Leu5]-Enkephalin (Leu-enkephalin) is an endogenous neuropeptide involved in nociception and an agonist of δ-opioid and μ-opioid receptors (Kis = 4.0 and 3.4 nM, respectively)