Neuropeptide Y Receptor Modulator

NPY Y2 antagonist 2 is a modulator targeting the neuropeptide Y (NPY) receptor Y2, with pK_i values of 6.8 nM and 7.2 nM in human and rat brains, respectively, and demonstrating blood-brain barrier penetration. NPY Y2 antagonist 2 shows selectivity for the Y1 and Y5 receptors. NPY Y2 antagonist 2 blocks the negative feedback regulation mediated by the NPY Y2 receptor, thereby increasing endogenous NPY release and enhancing Y1 receptor activation, resulting in the modulation of central neurotransmitter release. NPY Y2 antagonist 2 exhibits moderate in vivo clearance, high free fraction in rat brain, and a favorable brain/plasma ratio and brain exposure. NPY Y2 antagonist 2 is applicable for research in conditions such as mood disorders, anxiety induced by alcohol withdrawal, and social anxiety associated with nicotine withdrawal.

M40 TFA is the TFA salt form of M40. M40 TFA is an antagonist or a weak agonist for galanin receptor depending on different subtypes of galanin receptors in the brain, hypothalamus, hippocampus, amygdala and pancreas.

tBPC is a selective positive allosteric modulator for human Y4 receptor (Y4R), which enhances the activation of Y4R in G protein signaling and arrestin3 recruitment.

CYM2503 is a putative GalR2-positive allosteric modulator. CYM2503 increases the latency to first electrographic seizure and decreases the total time in seizure. CYM2503 also attenuates electroshock-induced seizures in mice. Galanin receptors type 1 (GalR1) and/or type 2 (GalR2) represent unique pharmacological targets for the research of seizures and epilepsy.

M40 is an antagonist or a weak agonist for galanin receptor depending on different subtypes of galanin receptors in the brain, hypothalamus, hippocampus, amygdala and pancreas.

VU0506013 is a selective positive allosteric modulator of Y4R (K_B = 34.9 nM). VU0506013 can be used in the development of anti-obesity agents targeting Y4R.