δ Opioid Receptor/DOR Antagonist

Naltrexone is an orally active, long-acting opioid receptor (opioid receptor) antagonist. Naltrexone blocks the euphoric effects of exogenous opioids and reduces alcohol craving by blocking opioid receptors (μ, κ, and δ) as well as opioid growth factor receptors. Low doses of Naltrexone are used to relieve chronic pain, treat inflammatory diseases and inhibit tumor growth, while high doses or continuous administration exert pro-inflammatory or pro-proliferative effects. Naltrexone relieves intractable pruritus caused by psoriasis, atopic dermatitis and other conditions, and its combination with Bupropion (HY-B0403) inhibits food craving, thereby reducing body weight.

CTAP TFA is a potent, highly selective, and BBB penetrant μ opioid receptor antagonist, with an IC₅₀ of 3.5 nM. CTAP TFA displays over 1200-fold selectivity over δ opioid (IC₅₀=4500 nM) and somatostatin receptors. CTAP TFA can be used for the study of L-DOPA-induced dyskinesia (LID) and opiate overdose or addiction.

CTAP is a potent, highly selective, and BBB penetrant μ opioid receptor antagonist, with an IC₅₀ of 3.5 nM. CTAP displays over 1200-fold selectivity over δ opioid (IC₅₀=4500 nM) and somatostatin receptors. CTAP can be used for the study of L-DOPA-induced dyskinesia (LID) and opiate overdose or addiction.

TAN-452 is an orally active, selective peripherally acting δ-opioid receptor (DOR) antagonist with a K_i of 0.47 nM and a K_b of 0.21 nM. TAN-452 is an antagonist for μ-opioid receptor (MOR; K_i=36.56 nM and K_b=9.43 nM) and κ-opioid receptor (KOR; K_i=5.31 nM and K_b=7.18 nM). TAN-452, a derivative of Naltrindole, demonstrates low brain penetrability and attenuates morphine-induced side effects without affecting pain control.

J-113397 is the first potent and selective nonpeptidyl ORL1 receptor antagonist (K_i: cloned human ORL1=1.8 nM) without any agonistic effects on other opioid receptors.

LY255582 is a pan-opioid antagonist and has high affinity for mu, delta, and kappa receptors (K_i: 0.4 nM, 5.2, 2.0 nM respectively). LY255582 can decrease food intake and body weight. LY255582 can be used for the research of obesity.

AT-076 is an opioid pan antagonist at nociception, kappa, mu, and delta opioid receptors, with K_i values of 1.75 nM (NOP), 1.67 nM (MOP), 1.14 nM (KOP) and 19.6 nM (DOP), respectively.

LY2048978 is a non-selective opioid receptor antagonist with K_i of 0.287, 0.471 and 1.05 nM for human mu, kappa and delta opioid receptors in vitro, respectively. LY2048978 can be used in the research of major depressive disorder and alcohol use disorder.

SRI-22136 is a Delta Opioid Receptor (DOR) antagonist that can cross blood-brain barrier with a IC₅₀ of 0.42 nM. SRI-22136 does not have agonistic activity but antagonistic activity against DOR, MOR (IC₅₀ = 370 nM), KOR (IC₅₀ = 54 nM) and can avoid addiction/aversion effects. SRI-22136 can effectively inhibit the BACE1 activity induced by DADLE (a DOR agonist) (HY-105343) (IC₅₀ = 120 nM). SRI-22136 prevents completely Alzheimer’s-like pathology in mouse model. SRI-22136 can used for the study of Alzheimer’s disease.

Methocinnamox (M-CAM) a selective and long-acting μ-opioid receptor (MOR) antagonist with a K_i of 0.6 nM. Methocinnamox binds to the orthosteric site of the MOR in a pseudo-irreversible, non-covalent manner, resulting in prolonged receptor blockade that persists until new receptors are synthesized. Methocinnamox acts as a reversible antagonist at both the kappa-opioid receptor (KOR) (K_i = 4.9 nM) and delta-opioid receptor (DOR) (K_i = 2.2 nM), and it exhibits no intrinsic agonist activity at these receptors. Methocinnamox can be used to reverse and prevent opioid overdose and addiction.

Mu opioid receptor antagonist 9 is potent, selective and CNS-pentrant mu-opioid receptor (MOR) antagonist with a K_i of 77.3 nM. Mu opioid receptor antagonist 9 exhibits selectivity over kappa-opioid receptor (KOR), and delta-opioid receptor (DOR). Mu opioid receptor antagonist 9 effectively blocks the antinociceptive effects of psychoactive substances. Mu opioid receptor antagonist 9 can reverse psychoactive substances-induced respiratory depression in mice. Mu opioid receptor antagonist 9 can be used for the research of Opioid Use Disorder (OUD).

N-Benzylnaltrindole hydrochloride is a potent δ2-selective opioid receptor antagonist. Benzylnaltrindole hydrochloride has a long duration of action in vivo than Naltriben (NTB). N-Benzylnaltrindole hydrochloride iserve as a useful tool in the pharmacologic characterization of δ-opioid receptor function.

BNTX (7-Benzylidenenaltrexone) is a highly selective δ1 opioid receptor antagonist. BNTX selectively antagonizes the antinociceptive activity mediated by spinal δ₁ opioid receptors, and does not alter the antinociceptive effects mediated by δ₂, μ or κ opioid receptors at selective doses.

RK-851 is a highly selective and orally active δ-opioid receptor antagonist, with a negative logarithm of the antagonist concentration (pA₂) of 8.84. TRK-851 exhibits the selectivity for the δ receptor of more than 100 times higher than that for the μ or κ receptors. TRK-851 exhibits a potent antitussive effect in a rat model of capsaicin-induced cough. TRK-851 can be used for research on antitussive effects.

Axelopran (TD-1211) is an opioid receptor antagonist with pKi values of 9.8, 8.8 and 9.9 for human recombinant μ and δ receptors and guinea pig κ receptor, respectively.

δ opioid receptor antagonist 1 (compound 6-Cy3) is a fluorescent antagonist probe with high selectivity for δ opioid receptor (DOR) (K_i=1.7 nM). δ opioid receptor antagonist 1 can be used to study the mechanism of pain perception.

Ondelopran (LY 2196044) is a non-selective opioid receptor antagonist. Ondelopran inhibits the release of dopamine in the nucleus accumbens induced by alcohol, reduces the rewarding effect of alcohol consumption, and lowers the craving. Ondelopran can be used for alcohol use disorder (AUD).

RX 809055AX is a potent long lasting opioid antagonist with selectivity towards at mu and delta receptors.