MOR modulator-1 

MOR modulator-1 (compound 6) is a potent and selective μ opioid receptor (MOR) modulator. MOR modulator-1 exhibits improved opioid receptor selectivity, enhanced in vivo antagonistic effect, and overall fewer withdrawal symptoms compared to NAT (6α-configuration). MOR modulator-1 links with carboxamido linker μ, δ, γ with K_i of 0.25, 41.1, 1.30 nM, respectively_[1]

MOR modulator-1 exhibits subnanomolar binding affinity at the MOR, single digit nanomolar binding affinity at the KOR (kappa opioid receptor), and much lower binding affinity to the DOR (delta opioid receptor), preserving reasonable selectivity at the MOR over the DOR^[1].
MOR modulator-1 displays the highest δ/μ selectivity, which is about 3-fold higher than that of NAT^[1].
MOR modulator-1 links with carboxamido linker μ, δ, γ with K_i of 0.25, 41.1, 1.30 nM, respectively^[1].
MOR modulator-1 binds with MOR [³⁵S]GTPγS with an EC₅₀ of 2.16 nM^[1].
MOR modulator-1 binds with KOR [³⁵S]GTPγS and DOR [³⁵S]GTPγS with an EC₅₀ of 3.83 and 23.6 nM, respectively^[1].
MOR modulator-1 shows nanomolar to subnanomolar potency and considerably low efficacy with %E_max values of 11.3^[1].
MOR modulator-1 significantly antagonizes DAMGO induced intracellular calcium increase in G_αqi5-transfected mMORCHO cells^[1].
MOR modulator-1 inhibits calcium with an IC₅₀ of 5.64 nM in G_αqi5-transfected mMORCHO cells^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

MOR modulator-1 (10 mg/kg, warm-water tail immersion, 20min) containing a 2’- thiazolyl moiety acts as the most potent member in this series of NAT analogs in antagonizing morphine mediated antinociception effect^[1].
MOR modulator-1 (10 mg/kg, warm-water tail immersion, 20 min) shows AD₅₀ value of 0.043 mg/kg, 10 times more potent compared to NAT^[1].
MOR modulator-1 (10 mg/kg, warm-water tail immersion, 20 min) stands out as the most active expoxymorphinan-based molecule among all MOR modulators^[1].
MOR modulator-1 (0.05-10 mg/kg, s.c., 20 min) exhibits fewer wet dog shakes and paw tremors at all testing doses than 1 mg/kg naloxone (NLX), even at the highest doses of 5 mg/kg and 10mg/kg, respectively^[1].
MOR modulator-1 (5 mg/kg, s.c., 20 min) mean count values in wet dog shake, jumps and paw tremors are 9.8, 36.8 and 30.2, respectively^[1].
MOR modulator-1 in brain at 5, 10, and 30 min after administration were 0.187, 0.235, and 0.264 μg/g, respectively, revealing that MOR modulator-1 quickly penetrated into the brain after s.c. administration and remained in the brain for a long time^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

453.55

C₂₄H₂₇N₃O₄S

2976336-81-7

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• [1]. Huang B, et al. Discovery of 6α-Thiazolylcarboxamidonaltrexamine Derivative (NTZ) as a Potent and Central Nervous System Penetrant Opioid Receptor Modulator with Drug-like Properties for Potential Treatment of Opioid Use Disorder. ACS Pharmacol Transl Sci. 2024 Dec 5;7(12):4165-4182.  [Content Brief]