Opioid Receptor Agonist

[Arg14,Lys15]Nociceptin TFA is a highly potent and selective NOP receptor (ORL1; OP4) agonist, with an EC₅₀ of 1 nM. [Arg14,Lys15]Nociceptin TFA displays high selectivity over opioid receptors, with IC₅₀s of 0.32, 280, >10000 and 1500 nM for NOP, μ, δ and κ receptors, respectively.

(D-Arg2, Sar 4)-Dermorphin (1-4) is a tetrapeptide derivative of the peptide Dermorphin (HY-P0244) found in amphibian skin. (D-Arg2, Sar 4)-Dermorphin (1-4) has significant analgesic effects by binding to the μ-opioid receptor (MOR) in the body. (D-Arg2, Sar 4)-Dermorphin (1-4) can be used in the development of analgesic drugs.

CJ-15161 is a κ-opioid receptor agonist. CJ-15161 can be used to study physiological functions such as pain relief and emotional regulation.

DPI-3290 (Org 41793) is a potent and specific opioid receptors agonist with K_i values of 0.18 nM, 0.46 nM, and 0.62 nM for δ-, μ-, and κ-opioid receptors, respectively. DPI-3290 is one of a series of novel centrally acting agents with potent antinociceptive activity.

TAN-67 (SB-205607) is a non-peptidic delta-opioid receptor agonist that exhibits significant antinociceptive activity in both diabetic and non-diabetic mice. TAN-67 demonstrates a marked and dose-dependent reduction in acetic acid-induced abdominal constrictions, with a notably stronger effect in diabetic mice compared to their non-diabetic counterparts. TAN-67's antinociceptive properties are primarily mediated through the activation of delta 1-opioid receptors, as indicated by the pronounced antagonism observed upon administration of a selective delta 1-opioid receptor antagonist.

Mesyl Salvinorin B is a potent and selective kappa opioid receptor (KOP-r) agonist. Mesyl Salvinorin B prevents the ADE (Alcohol deprivation effect) in mice. Mesyl Salvinorin B dose-dependently reduces alcohol intake and preference in CED (chronic escalation drinking) mice.

β-Lipotropin (61-69) is a potent opioid agonist.

SHR0687 is a selective tetrapeptide kappa opioid receptor (KOR) agonist with an EC₅₀ of 0.53 pM. SHR0687 displays high potency and selectivity over MOR and DOR, with negligible blood-brain barrier penetration. SHR0687 activates KOR specifically, leading to potential modulation of neurological pathways without significant central nervous system effects. SHR0687 can be used for the research of pain.

CA1001 is a small-molecule ZNF74 inhibitor and a peripherally restricted κ/δ dual opioid receptor agonist. CA1001 exhibits potent antitumor activity both in vitro and in vivo. CA1001, in combination with immune checkpoint inhibitors, significantly enhances tumor regression. CA1001 activates peripherally restricted κ/δ dual opioid receptors and exerts analgesic effects under conditions of inflammatory pain, neuropathic pain, and mechanical hyperalgesia. CA1001 can be used in research related to melanoma, mechanical hyperalgesia, neuropathic pain, and inflammatory arthritis pain.

Dynorphin A (1-10) an endogenous opioid neuropeptide, binds to extracellular loop 2 of the κ-opioid receptor. Dynorphin A (1-10) also blocks NMDA-activated current with an IC₅₀ of 42.0 μM.

Herkinorin is a potent and selective agonist of µ opioid receptor with a K_i of 45 nM Herkinorin is widely used for pain research.

K-Opioid receptor agonist-1 (Compound 5a) is an agonist for κ-Opioid receptor with K_i of 0.25 nM and EC₅₀ of 2 nM. K-Opioid receptor agonist-1 is blood brain barrier (BBB) penetrate (brain/plasma ratios of 0.50 to 0.65). K-Opioid receptor agonist-1 exhibits anti-inflammatory activity in dermatitis models induced by Arachidonic acid (HY-109590) or oxazolidinone.

Ac-RYYRWK-NH2 is a potent and selective partial agonist for the nociceptin receptor (NOP), [³H]Ac-RYYRWK-NH2 binds to rat cortical membranes ORL1 with a K_d of 0.071 nM, but has no affinity for μ-, κ- or δ-opioid receptors.

SYK-1106 is a potent delta-opioid receptor (DOR) agonist with an EC₅₀ of 89 pM and a K_i of 848 pM. SYK-1106 is selective for μ and κ opioid receptors, with K_i values of 9.54 nM and 2.45 nM, respectively. SYK-1106 induces dose-dependent antidepressant-like effects. SYK-1106 can be used for the research of depression.

μ opioid receptor agonist 3 (compound 20) is a potent μ opioid receptor (µOR) agonist with an EC₅₀ of 0.87 nM. μ opioid receptor agonist 3 has the potential for pain and neuropsychiatric indications research.

KK-103 is a precursor of leucine-enkephalin (Leu-ENK) overcomes high proteolytic instability of Leu-ENK via markedly increased plasma stability in mice that has antinociceptive effect.

UFP-512 is a selective and potent σ-opioid receptor (DOP receptor) peptidic agonist with antidepressant- and anxiolytic-like effects. UFP-512 exhibits as a potent agonist on adenylyl cyclase inhibition and Erk1/2 activation. UFP-512 induces phosphorylation of DOP receptors on Ser³⁶³ with a low desensitization of the cAMP pathway. UFP-512 is promising for research of mood disorders.

Frakefamide is a potent analgesic that acts as a peripheral active μ-selective receptor agonist. Frakefamide is unable to penetrate the blood-brain-barrier and enter the central nervous system.

ID110460002 possesses both full agonist activity at the μ-opioid receptor (OPRM) and agonist activity at the δ-opioid receptor (OPRD). ID110460002 acts as a potent agonist for the G protein pathways of both receptors, but exhibits only very weak partial agonist activity towards the β-arrestin-2 pathway. The agonistic potency of ID110460002 at OPRM has extremely high intrinsic activity and is unaffected by reduced receptor expression levels, while its potency at OPRD depends on receptor expression levels. ID110460002 displays tissue- or organ-dependent properties, and serves as a critical compound for investigating pain mechanisms and analgesia.

LY-281217 is a potent mu-opioid agonist with analgesic effects.