β-Endorphin (β-EP) is an endogenous opioid neuropeptide with diverse biological activities. It is produced via piomelanocortin cleavage in the pituitary gland, hypothalamus, and in lymphocytes, then migrates to its sites of action which include plasma, gut, skin, placenta, cerebrospinal fluid, and cardiac tissues. β-EP induces concentration-dependent decreases in electrically stimulated contraction of the mouse vas deferens that can be reversed by the μ-opioid antagonist CTP and δ-opioid antagonist ICI 174,864. In vivo, β-EP (5 μg, i.c.v.) slows gastrointestinal transit in mice. β-EP (0.5 or 5 μg, i.c.v.) stimulates food intake in rats for 4 to 6 hours, however, this effect is not prolonged with continuous infusion. It antagonizes the appetite-suppressive effects of α-melanocyte-stimulating hormone (α-MSH) for the first three days post administration. β-EP also reduces paralytic demyelination induced by the murine coronavirus MHV-JHM in immunocompetent, but not irradiated or immune-incompetent, mice and rats.
Acetyl β-endorphin (1-26) is a neuropeptide found in rat hippocampus, brain stem, and pituitary. It is also present in the human hypothalamus, where it comprises approximately 4.9% of total β-endorphin peptides. Acetyl β-endorphin (1-26) is produced through posttranslational processing of β-endorphin and is processed similarly in rat and human hypothalamus. Levels of acetyl β-endorphin (1-26) increase in the rat pars intermedia and brain stem following chronic administration of haloperidol .
β-Endorphin (1-27) is an endogenous peptide that binds to μ-, δ-, and κ-opioid receptors (Kis = 5.31, 6.17, and 39.82 nM, respectively, in COS-1 cells expressing rat receptors). It binds to rat and mouse brain membrane preparations (IC50s = 1.1 and 5.7 nM, respectively) and induces chemotaxis of human monocytes in vitro when used at a concentration of 1 nM. Intracerebroventricular administration of β-endorphin (1-27) increases the latency to tail withdrawal in response to thermal stimulation in mice with a median antinociceptive dose (AD50) of 1,500 pmol per animal. It inhibits antinociception induced by β-endorphin in mice in response to thermal stimuli when administered at a dose of 65 pmol per animal. In rats, β-endorphin (1-27) does not affect drug-associated place preference when administered at doses up to 20 μg, i.c.v., but inhibits β-endorphin-induced place preference when administered at a dose of 10 μg per animal.
N-Acetyl-α-Endorphin is a chemical compound consisting of α-Endorphin that has been acetylated at the N-terminal. α-Endorphin, in turn, is an endogenous opioid peptide.
α-Neoendorphin (1-8) is an 8-amino acid peptide derived from the N-terminal of α-Neoendorphin, an endogenous opioid peptide in the neoendorphin family, which are proteolytic cleavage products.
Endorphin Beta is A substance produced in the brain, especially in the pituitary gland, Endorphin Beta blocks the sensation of pain. Endorphin Beta is produced in response to pain, exercise, and other forms of stress. Endorphin Beta belongs to a group of
Veldoreotide, also known as Somatoprim, is a unique somatostatin receptor subtypes 2-, 4- and 5-selective analogue which effectively reduces GH secretion in human GH-secreting pituitary adenomas, even in Octreotide non-responsive tumours.
Potent and selective μ opioid receptor antagonist (IC50 = 3.5 nM). Displays > 1200-fold selectivity over δ opioid and somatostatin receptors. Brain penetrant and active in vivo.
Activator of protein kinase C; attached to cell permeabilization Antennapedia domain vector peptide. Consists of peptide derived from the C2 domain of PKC β linked by a disulfide bridge to the Antennapedia domain vector peptide. The Antennapedia peptide i
Dynorphin A TFA, 作为一种内源性阿片肽,主要在中枢神经系统(CNS)中发挥抑制性神经传导的作用。该化合物不仅是kappa阿片受体(KOR)的高效激动剂,还能激活其他阿片受体,包括mu(MOR)和delta(DOR)。Dynorphin A TFA具有诱导神经元死亡的能力,因此在神经系统疾病的研究中具有应用价值。