ac ryyrik nh2

High affinity ligand for the NOP site (Ki = 1.5 nM). Antagonizes nociceptin-stimulated GTP binding in rat brain and the chronotropic effect of nociceptin on rat cardiomyocytes. However, displays potent agonist properties in vivo, inhibiting locomotor acti

Ac-RYYRIK-NH2 acetate is an agonist at nociceptin/orphanin FQ(noc/OFQ) receptors, affecting spontaneous locomotor activity. Ac-RYYRIK-NH2 acetate is a partial agonist on ORL1 transfected in CHO cells, antagonizes the stimulation of [35S]-GTPgammaS binding to G proteins by noc/OFQ in membranes and sections of rat brain.

Ac-RYYRIK-NH2 TFA acts as both a potent partial agonist for ORL1 when transfected in CHO cells (K d = 1.5 nM) and an endogenous ligand of ORL1. Moreover, it serves as a specific antagonist that inhibits G protein activation and competitively blocks the stimulation of [35S]-GTPγS binding to G proteins by nociceptin/orphanin FQ (noc/OFQ) in rat brain membranes and sections [1].

Ac-RYYRWK-NH2 acetate is a potent partial agonist of the nociceptin receptor(NOP), which is the endogenous ORL1 receptor agonist.

Potent agonist of the nociceptin (ORL1) receptor, demonstrated both in vitro and in vivo. Selective, competitive antagonism at the nociceptin receptor has also been reported (pA2 = 7.02 and 6.75 in the guinea pig ileum and mouse vas deferens respectively)

Ac-hMCH(6-16)-NH2 shows non-selective agonist activity towards both MCH-1R and MCH-2R, which are human MCH receptors in the brain. The compound effectively binds to and activates these receptors, with IC 50 values of 0.16 nM and 2.7 nM for MCH-1R and MCH-2R, respectively.

Ac-SVVVRT-NH2, a PGC-1α modulator, enhances the activity of the human PGC-1α promoter (114%), elevates PGC-1α mRNA levels (125%), and promotes intracellular lipid accumulation (128%) in subcutaneous human adipocytes. This compound has potential applications in research related to diseases influenced by PGC-1α.

Ac-Ser-Gln-Asn-Tyr-Pro-Val-Val-NH2 is a peptide substrate specific to HIV-1 protease, used as the variable component in peptidolytic assays designed to measure the enzyme's inhibition [1][2].

Ac-RYYRWK-NH2 is a highly effective and specific partial agonist for the nociceptin receptor (NOP). It demonstrates a remarkable affinity for rat cortical membranes ORL1, with [3H]Ac-RYYRWK-NH2 exhibiting a Kd value of 0.071 nM. However, it shows negligible affinity towards μ-, κ-, or δ-opioid receptors.

Ac-DArg-c[Cys-Glu-His-DPhe-Arg-Trp-Cys]-NH2 is a synthetic cyclic octapeptide acting as a melanocortin-4 receptor (MC4R) agonist, significantly elevating heart rate and blood pressure [1].

Ac-[Nle4,D-Phe7]-α-MSH (4-10)-NH2, a melanotropin derivative and melanocyte-stimulating hormone, activates tyrosinase and demonstrates a thermoregulatory effect in rat models [1][2].

Potent, selective partial agonist peptide for the NOP receptor (Ki = 0.71 nM). Selective over μ, δ and κ opioid receptors (IC50 > 4000 nM). Increases food intake in vivo.