neuropeptide receptor

Neuropeptide Y5 receptor ligand-1 (Compound 54), a carbazole derivative, acts as a powerful antagonist to the neuropeptide Y5 (NPY-5) receptor [1].

AT-121 is a dual μ-opioid and neuropeptide receptor partial agonist (Kis 16.49 and 3.67 nM, respectively). It stimulates [35S]GTPγS binding to cell membranes expressing either μ-opioid receptors or neuropeptide receptors (EC50s of 19.6 and 34.7 nM, respectively.) AT-121 (0.003-0.03 mg kg) reduced capsaicin-induced thermal anisocoria in a dose-dependent manner, but did not increase scratching activity in rhesus monkeys. In rhesus monkey drug self-administration tests, AT-121 at doses of 0.3 to 10 μg kg per injection lacked reinforcing effects (a potential marker of abuse) and did not reduce the reinforcing effects of food pellets.AT-121 (0.01 or 0.03 mg kg) did not induce hyperalgesia, a marker of tolerance, in rhesus monkeys.AT-121 is a safe non-addictive pain reliever with anti-injury and analgesic effects.

Selvigaltin (GB1211) is a Gal-3 inhibitor with potential anticancer activity. Selvigaltin is used in the study of cirrhosis and cancer.

Pancreatic Polypeptide, rat acetate is an agonist of NPY receptor, with high affinity at NPYR4.

Urotensin I acetate, a CRF-like neuropeptide, acts as an agonist of CRF receptor with pEC50s of 11.46, 9.36 and 9.85 for human CRF1, human CRF2 and rat CRF2α receptors in CHO cells, and Kis of 0.4, 1.8, and 5.7 nM for hCRF1, rCRF2α and mCRF2β receptors, respectively[1][2].

Neurokinin antagonist 1 is a potent is a neuropeptide antagonist that can be used to study neurological disorders.

BPR1M97 is a mu opioid receptor (MOP) and neuropeptide-orphin FQ (NOP) receptor agonist with blood-brain barrier permeability and potency, with Kis values of 1.8 nM for MOP and 4.2 nM for NOP.BPR1M97 exhibits anti-injurious effects and antinociceptive effects.

Y1 receptor antagonist 1 (H 409-22 isomer) is the active isomer of H-409 22, a neuropeptide Y (NPY) Y1 receptor antagonist that dose-dependently antagonizes the vascular response to exogenous and endogenous NPY in pigs. lagodeoxycholic acid (H 409-22 isomer) is the active isomer of H-409 22, an antagonist of neuropeptide Y (NPY) Y1 receptor.

DF-1012 FA is a structural analog of DF-1012, a neuropeptide inhibitor used in the study of asthma and cough.

(S)-VU0637120 is a selective neuropeptide Y(4)R-mutant antagonist used in the study of metabolic disorders.

Zolmitriptan (311C90) selectively binds to and activates serotonin (5-HT) 1B receptors expressed in intracranial arteries and 5-HT 1D receptors located on peripheral trigeminal sensory nerve terminals in the meninges and central terminals in brainstem sensory nuclei. Zolmitriptan is a member of the triptan class of agents with anti-migraine properties. Receptor binding results in constriction of cranial vessels, reduction of vessel pulsation and inhibition of nociceptive transmission, thereby providing relief of migraine headaches. Zolmitriptan may also relieve migraine headaches by inhibition of pro-inflammatory neuropeptide release.

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).

SF 11 is a potent, brain-penetrant neuropeptide Y Y2 receptor antagonist with an IC50 of 199 nM, exhibiting antidepressant-like activity.

WAY-639889 is a small molecule compound with selective and potent inhibitory effects on neuropeptide Y-5 receptors.

Neuropeptide AF (human) acetate (Neuropeptide AF (human) acetate (192387-38-5 Free base)) is an anti-opioid neuropeptide, a Neuropeptide AF (human) derivative, which regulates adipocyte metabolism.

Pancreatic Polypeptide (human) acetate is a C-terminally amidated 36 amino acid peptide, which acts as a neuropeptide Y (NPY) Y4/Y5 receptor agonist.

Neuropeptide Y (29-64), amide, human acetate is involved in Alzheimer's disease (AD) and protects rat cortical neurons against β-Amyloid toxicity.

Neuropeptide SF(mouse,rat) acetate (Neuropeptide SF(mouse,rat) acetate (230960-31-3 free base)) is a potent neuropeptide FF receptor agonist, Ki for NPFF1 and NPFF2 are 48.4 nM and 12.1 nM, respectively. Neuropeptide SF(mouse,rat) acetate (Neuropeptide SF(mouse,rat) acetate (230960-31-3 free base)) increases the amplitude of the sustained current of heterologously expressed acid sensing ion channel 3 (ASIC3).

RFRP-3(human) acetate, a human GnIH peptide homolog, is a potent inhibitor of gonadotropin secretion by inhibiting Ca2+ mobilization. RFRP-3(human) acetate is a NPFF1 receptor agonist, it inhibits forskolin-induced production of cAMP with an IC50 of 0.7 n

M1145 acetate, a chimeric peptide, is a selective galanin receptor type 2 (GAL2) agonist, with a Ki of 6.55 nM. M1145 acetate shows more than 90-fold higher affinity for GAL2 over GAL1 (Ki=587 nM) and a 76-fold higher affinity over GalR3 (Ki=497 nM). M1145 acetate has an additive effect on the signal transduction of galanin[1].

M40 acetate is a potent, non-selective galanin receptor antagonist (Ki values are 1.82 and 5.1 nM at GAL1 and GAL2 respectively) that inhibits galanin (1-29) binding in rat brain in vitro (IC50 = 3 - 15 nM). Attenuates the antidepressant effects of fluoxetine and blocks galanin-induced food intake in vivo. Also exhibits weak partial agonist activity at peripheral GAL2 receptors at doses > 100 nM.

M617 acetate is a selective agonist of galanin receptor 1 (GAL1). M617 acetate acts through central GAL1, promotes GLUT4 expression, and enhances GLUT4 content in the cardiac muscle of type 2 diabetic rats. The Ki values are 0.23 and 5.71 nM for GAL1 and GAL2, respectively.

M871 acetate is a selective galanin GAL2 receptor antagonist (Ki values are 13.1 and 420 nM at GAL2 and GAL1 receptors, respectively).It blocks pronociceptive effects of GAL2 agonists including AR-M1896.

MK-0557 is a selective and orally available antagonist of the neuropeptide Y5 receptor (Ki: 1.6 nM).