dose-dependently

MCL0020 is a potent and selective melanocortin MC4 receptor antagonist (IC50 values are 11.63, 1115, and >10,000 nM at MC4, MC3, and MC1 receptors, respectively). It significantly reverses stress-induced anorexia without affecting food intake in free-feeding rats and exhibits anxiolytic-like activity in vivo.

Galantide acetate, a non-specific galanin receptor antagonist, is a peptide consisting of fragments of galanin and substance P. Galantide acetate recognizes two classes of galanin binding sites (KD<0.1 nM and ~6 nM) in the rat hypothalamus. Galantide acetate dose dependently (IC50=1.0 nM) antagonizes the galanin-mediated inhibition of the glucose-induced insulin secretion from mouse pancreatic islets. Galantide acetate appears to bind to a single population of SP receptors (KD~40 nM).

Gastrin-releasing peptide (GRP) is a neuropeptide that stimulates gastrin release. It binds to (Ki = 300 nM) and stimulates amylase secretion in rat pancreatic AR42J cells (EC50 = 0.3 nM). GRP increases proliferation of human liver carcinoma HepG2 and MHCC97H cells but does not affect the proliferation of normal HL-7702 liver cells at a concentration of 1 nM. In vivo, GRP (0.35 nmol/kg/h) increases both pancreatic exocrine secretion and pancreatic polypeptide (PP) release in rats. It dose-dependently stimulates gastrin, pancreatic amylase, lipase, bilirubin, and acid output and induces gallbladder contraction in humans when administered at doses ranging from 1 to 27 pmol/kg per hour.

CTOP TFA, a potent and highly selective μ-opioid receptor antagonist, antagonizes acute analgesic effects and hypermotility, while enhancing extracellular dopamine levels in the nucleus accumbens. It also dose-dependently increases locomotor activity [1] [2].

BeKm-1 TFA is a potent, selective blocker of the KV11.1 (hERG) channel, demonstrating specificity for KV11.1 over 14 other potassium channels. This compound dose-dependently prolongs the QTc interval in isolated rabbit hearts, affirming its role as a selective inhibitor.

m3-Huwentoxin IV (m3-HwTx-IV) is a potent inhibitor of sodium channels (NaV), with half-maximal inhibitory concentrations (IC50s) of 3.3 nM for hNaV1.7, 6.8 nM for hNaV1.6, 7.2 nM for hNaV1.3, 8.4 nM for hNaV1.1, 11.9 nM for hNaV1.2, and 369 nM for hNaV1.4 in the QPatch assay. It also alleviates spontaneous pain in a rodent model induced by the NaV1.7 activator OD1 in a dose-dependent manner [1].

α-Pompilidotoxin (α-PMTX), a neurotoxin sourced from Anoplius samanensis venom, reversibly and dose-dependently enhances excitatory postsynaptic currents (EPSCs), serving as a valuable tool in neuroscience research [1].

Val-Gly-Ser-Glu (NSC 350591), an ECF-A tetrapeptide, dose-dependently enhances the rosetting of human eosinophils with complement-coated sheep erythrocytes (EAC3b) without affecting neutrophils [1].

PACAP (1-38), a novel neuropeptide isolated from the bovine hypothalamus is more active than vasoactive intestinal peptide (VIP) in stimulating adenylate cyclase (EC50=7 nM). PACAP 1-38 (10-9 M) increased substance P (SP), gastrin releasing peptide (GRP),

[Sar9,Met(O2)11]-Substance P TFA is a selective tachykinin NK1 receptor agonist.[Sar9,Met(O2)11]-Substance P and septide (10-100 pmol per rat, i.c.v.) are equipotent in increasing mean arterial blood pressure (MAP) and heart rate (HR), yet they have dissi

[Sar9,Met(O2)11]-Substance P acetate is a tachykinin NK1 receptor selective agonist. [Sar9,Met(O2)11]-Substance P acetate is a selective tachykinin NK1 receptor agonist.[Sar9,Met(O2)11]-Substance P acetate and septide (10-100 pmol per rat, i.c.v.) are equipotent in increasing mean arterial blood pressure (MAP) and heart rate (HR), yet they have dissimilar time-course. Both agonists increase dose-dependently face washing and sniffing while [Sar9,Met(O2)11]-Substance P acetate is the sole to produce grooming.

Phe-Met-Arg-Phe, amide dose-dependently (ED50=23 nM) activates a K+ current in peptidergic caudodorsal neurons and appears to localize with neuropeptide Y in some brain regions.

Phe-Met-Arg-Phe, amide acetate, activates a K+ current in peptidergic caudodorsal neurons dose-dependently (ED50=23 nM) and appears to localize with neuropeptide Y in some brain regions.

Potent and selective KV11.1 (hERG) channel blocker. Selective for KV11.1 over a panel of 14 other potassium channels. Dose-dependently prolongs QTc interval in isolated rabbit heart.