SML0242
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AZ-MTAB ≥98% (HPLC)
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AZ-MTAB is a potent, short acting κ-opioid receptor (KOR) selective antagonist.
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B8562
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BD 1047 dihydrobromide ≥95% (HPLC)
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BD-1047 is a selective, putative σ receptor antagonist with antidystonic activity. BD-1047 has >50-fold selectivity at σ1 over σ2 and also >100-fold selectivity over opiate, phencyclidine, muscarinic, dopamine, α1- & α2-adrenoceptor, 5-HT1, and 5-HT2. Though s receptor antagonism is consistent with antipsychotic, especially anti-schizophrenic, activity, BD-1047 shows only modest activity in animal screens for antipsychotics. In human immunodeficiency (HIV)-1 seropositive patients, BD 1047 along with other antioxidants may aid in reduction of cathepsin B- based neuropathology.
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N1771
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nor-Binaltorphimine dihydrochloride
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Highly selective k-opioid receptor antagonist. nor-Binaltorphimine has antidepressant properties.
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human ... OPRK1(4986)
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B8312
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BNTX maleate salt hydrate ≥98% (HPLC)
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BNTX is a selective nonpeptide δ1 opioid receptor antagonist. It antagonizes the effect of D-Pen2,5-enkephalin (a δ1 agonist 4-6 fold, but did not affect the activity of δ2 or μ agonists.<<<107>>> BNTX is used to discriminate among opioid receptor subtypes in effects such as alcohol and drug dependence. It binds 100× more tightly to δ1 than to δ2 receptors. In the tail-flick assay, antinocieceptive ED50 = 646.4 pmol/mouse.
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O001
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β-Chlornaltrexamine dihydrochloride solid
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Irreversible μ, δ and κ opioid receptor antagonist.
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O003
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β-Funaltrexamine hydrochloride solid
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Selective irreversible μ opioid receptor antagonist that is also a κ opioid receptor agonist.
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G3416
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5′-Guanidinonaltrindole di(trifluoroacetate) salt hydrate solid, ≥98% (HPLC)
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Selective κ opioid receptor antagonist; GNTI is five-fold more potent and 500-fold more selective than norbinaltorphimine (nor-BNI) for the κ opioid receptor in smooth muscle preparations.
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human ... OPRK1(4986)
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L121
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Levallorphan tartrate salt ≥98% (HPLC), powder
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Partial agonist (antagonist) at μ and δ opioid receptors.
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human ... OPRD1(4985), OPRM1(4988)
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SML0225
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LY255582 ≥98% (HPLC)
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LY255582 inhibits the diet-associated increases in mesolimbic dopamine levels and reduces the consumption of highly-palatable food intake. LY255582 is a centrally active opioid receptor antagonist (defined as an inverse agonist in 2011 JPET paper) that inhibited weight gain in obese Zucker rats over 30 days. It is more that 5-fold selective for mu opioid receptor compared to kappa opioid receptors and 13-fold selective over delta opioid receptors.
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SML0277
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Methylnaltrexone bromide ≥97% (HPLC)
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Methylnaltrexone bromide is a narcotic antagonist. It is a peripheral mu-opiod receptor antagonist that cannot cross the blood-brain barrier. It reverses many opioid side-effects without interfering with pain relief.
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human ... OPRM1(4988)
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N4396
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Nalbuphine hydrochloride hydrate ≥98% (HPLC)
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Partial agonist for μ and κ opioid receptors.
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human ... OPRD1(4985), OPRK1(4986), OPRM1(4988)
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N176
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Naloxonazine dihydrochloride hydrate powder, ≥95% (HPLC)
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Potent opioid antagonist that is selective for μ1 opioid receptors.
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human ... OPRM1(4988)
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N7758
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Naloxone hydrochloride dihydrate ≥98% (TLC and titration), powder
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Competitive antagonist for μ, κ, δ, and σ opioid receptors; blocks the action of σ-agonists at opioid sites. Naloxone′s antagonistic effect last for about 45 min and thus, requires repeated dosage. It results in critical side effects such as pulmonary edema.
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human ... OPRD1(4985), OPRK1(4986), OPRM1(4988), OPRS1(10280)
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N129
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Naloxone methiodide ≥98% (HPLC), solid
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Naloxone methiodide has low affinity for opioid receptors than naloxone. Administration of naloxone inhibits opioid receptor and opioid-induced respiratory depression. Quaternary salt of naloxone that, like the parent compound, is a nonselective antagonist at opioid receptors. It does not cross the blood-brain barrier.
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N3136
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Naltrexone hydrochloride
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Competitive antagonist for μ, κ, δ, and σ-opioid receptors; has greater oral efficacy and longer duration of action than naloxone.
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human ... OPRD1(4985), OPRK1(4986), OPRM1(4988), OPRS1(10280)
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N156
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Naltriben methanesulfonate hydrate ≥98% (HPLC), solid
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Naltriben methanesulfonate is a highly selective δ2 opioid receptor antagonist. The relative ability of the delta antagonists benzylidenenaltrexone and naltriben to inhibit DPDPE-stimulated [35S]GTPgammaS binding suggests that the opioid receptor is of the delta-2 subtype. Ligand binding assays demonstrates biphasic binding of the antagonist to the single receptor type. [35S]GTPgammaS binding is also stimulated by [D-Ser2,Leu5,Thr6]enkepha
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N115
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Naltrindole hydrochloride solid
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Highly selective, non-peptide δ-opioid receptor antagonist that crosses the blood-brain barrier.
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human ... OPRD1(4985)
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