opioid

Dermorphin is agonist of μ-opioid receptor (MOR) agonist.

DAMGO (DAGO) is an opioid receptor agonist with the ability to affect the locomotive activity in rodents. Possible analgesic agent due to μ-opiod receptor interaction.

Nociceptin (1-13), amide is a potent agonist Opioid receptor-like1 (ORL1) receptor with a pEC50 of 7.9 for mouse vas deferens and a Ki of 0.75 nM for binding to rat forebrain membranes.

BW-180C (DADLE) is a prototypical δ-opioid receptor agonist that also displays activity at the μ-opioid receptor. Displays antinociceptive activity in vivo.

b-Casomorphin (1-3) Acetate is a tri-peptide with an opioid effect.

β-Endorphin (1-27) (human) acetate, existing in the hypophysis cerebri and hypothalamus, exhibits antinociception activity. β-Endorphin (1-27) (human) acetate is an agonist of opioid receptor, showing preferred affinity for μ-opioid receptor and δ-opioid

Leu-enkephalin, an endogenous peptide consisting of five amino acids, functions as an agonist at opioid receptors. The N-terminally acetylated form of this compound is known as N-terminally acetylated Leu-enkephalin.

BAM 22P acetate is a potent opioid agonist.

N-Acetyl-α-Endorphin acetate is an acetylated α-Endorphin at N-terminal. α-Endorphin is an endogenous opioid peptide.

Dynorphin B (1-13) acetate acts as an agonist on opioid κ-receptor.

Neurotensin TFA (39379-15-2 free base) is an endogenous 13 amino acid neuropeptide with profound opioid-independent analgesic effects. It behaves as a neurotransmitter in the brain, as a hormone in the gut, and also as a neuromodulator. It is implicated in the pathophysiology of several CNS disorders (including schizophrenia, Parkinson's disease, drug abuse, pain, cancer, inflammation, eating disorders, and central control of blood pressure) due to its association with a wide variety of neurotransmitter systems such as dopaminergic, sertonergic, glutamatergic, GABAergic, and cholinergic systems. It has a role as a human metabolite, a mitogen, a neurotransmitter and a vulnerary.

Endomorphin 2 TFA, displays reasonable affinities for kappa3 binding sites, with Ki value between 20 and 30 nM. a high affinity, highly selective agonist of the μ-opioid receptor,

Deltorphin (Dermenkephalin) is Isolated from the skin of Phyllomedusa Sauvage. It also has an affinity to the opioid receptor.

Deltorphin acetate is a substance obtained from the skin secretions of a frog, Phyllomedusa bicolor and shows high selectivity and affinity for δ-opioid receptor.

Bam 12P is a Pro-Met-enkephalin precursor that is isolated from the bovine adrenal medulla.

Dynorphin (1-8) is an opioid octapeptide from the porcine hypothalamus. It comprises the N-terminal eight residues of dynorphin.

Leuphasyl TFA is an amid peptide, a δ-opioid receptor agonist, is a degradation resistant long-acting Leu-enkephalin analog used to study the signaling pathway of delta opioid receptors. Leuphasyl TFA is a potent, long-acting Leu-enkephalin analog that is resistant to enzymatic degradation

Acetyl tetrapeptide-15 Acetate (Skinasensyl Acetate), a synthetic peptide used in cosmetic products for sensitive skin, is an endomorphin-2 derivative that extends the range of neuronal excitability thresholds in the μ-opioid receptor via an endorphin-like pathway, and can be used to study inflammatory and neuropathic pain produced by skin hyperreactivity. Inflammatory and neuropathic pain produced by skin hyperresponsiveness.

(D-Ser2)-Leu-Enkephalin-Thr is a delta selective agent of opioid receptor and shows analgesic effects.

Nociceptin (1-7) acetate is a potent agonist of opioid receptor-like 1 (ORL1) receptor. Nociceptin (1-7) combines with nociceptin reduces hyperalgesia and has antinociceptive activity.

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.

Bilaid C is a tetrapeptide μ-opioid receptor agonist (Ki= 210 nM in HEK293 cell membranes expressing the human receptor) that has been found inPenicillium.1It inhibits forskolin-induced cAMP accumulation by 77% in HEK293 cells expressing the human μ-opioid receptor when used at a concentration of 10 μM. Bilaid C induces inward rectifying potassium channel (Kir) currents in rat locus coeruleus slices that endogenously express high levels of the μ-opioid receptor (EC50= 4.2 μM). 1.Dekan, Z., Sianati, S., Yousuf, A., et al.A tetrapeptide class of biased analgesics from an Australian fungus targets the μ-opioid receptorProc. Natl. Acad. Sci. USA116(44)22353-22358(2019)

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.

Difelikefalin (CR-845; FE-202845) is a peripherally restricted, selective kappa opioid receptor (KOR) agonist with anti-inflammatory properties, demonstrating potential for modulating pruritus in chronic kidney disease.