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Excitatory Amino Acids - Opiod Antagonists

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SML0242 AZ-MTAB ≥98% (HPLC) AZ-MTAB is a potent, short acting κ-opioid receptor (KOR) selective antagonist.
 
B8562 BD 1047 dihydrobromide ≥95% (HPLC) 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.
 
N1771 nor-Binaltorphimine dihydrochloride Potent and highly selective κ opioid receptor antagonist.
human ... OPRK1(4986)
B8312 BNTX maleate salt hydrate ≥98% (HPLC) 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.
 
O001 β-Chlornaltrexamine dihydrochloride solid Irreversible μ, δ and κ opioid receptor antagonist.
 
O003 β-Funaltrexamine hydrochloride solid Selective irreversible μ opioid receptor antagonist that is also a κ opioid receptor agonist.
 
G3416 5′-Guanidinonaltrindole di(trifluoroacetate) salt hydrate solid, ≥98% (HPLC) 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.
human ... OPRK1(4986)
L7418 LAAM hydrochloride ≥98% (HPLC), solid LAAM hydrochloride is μ opioid receptor agonist. LAAM hydrochloride is a DEA-controlled substance, which has a slow onset, but a long duration of action. LAAM is a useful tool for studying opiate tolerance and cross-reactivity with other μ opioid receptor agonists.
 
L121 Levallorphan tartrate salt ≥98% (HPLC), powder Partial agonist (antagonist) at μ and δ opioid receptors.
human ... OPRD1(4985), OPRM1(4988)
SML0225 LY255582 ≥98% (HPLC) 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.
 
M120 Metaphit methanesulfonate salt ≥98% (HPLC), solid Metaphit methanesulfonate salt is an irreversible, non-competitive antagonist at the phencyclidine site on the NMDA receptor; sigma receptor irreversible, competitive antagonist.
human ... OPRS1(10280)
M231 3-Methoxynaltrexone hydrochloride solid Putative antagonist at a novel opioid receptor that binds morphine-6-β-glucuronide; blocks endomorphin-2-induced antinociception.
 
SML0277 Methylnaltrexone bromide ≥97% (HPLC) 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.
 
N4396 Nalbuphine hydrochloride hydrate ≥98% (HPLC) Partial agonist for μ and κ opioid receptors.
human ... OPRK1(4986), OPRM1(4988)
N5770 Nalmefene Nonselective opioid receptor antagonist.
rat ... Oprd1(24613), Oprm1(25601)
N176 Naloxonazine dihydrochloride hydrate powder, ≥95% (HPLC) Potent opioid antagonist that is selective for μ1 opioid receptors.
human ... OPRM1(4988)
N7758 Naloxone hydrochloride dihydrate ≥98% (TLC and titration), powder Competitive antagonist for μ, κ, δ, and σ opioid receptors; blocks the action of σ-agonists at opioid sites.
human ... OPRD1(4985), OPRK1(4986), OPRM1(4988), OPRS1(10280)
N129 Naloxone methiodide ≥98% (HPLC), solid Quaternary salt of naloxone that, like the parent compound, is a nonselective antagonist at opioid receptors. It does not cross the blood-brain barrier.
 
N3136 Naltrexone hydrochloride Competitive antagonist for μ, κ, δ, and σ-opioid receptors; has greater oral efficacy and longer duration of action than naloxone.
human ... OPRD1(4985), OPRK1(4986), OPRM1(4988), OPRS1(10280)
N156 Naltriben methanesulfonate hydrate ≥98% (HPLC), solid 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  
N115 Naltrindole hydrochloride solid Highly selective, non-peptide δ-opioid receptor antagonist that crosses the blood-brain barrier.
human ... OPRD1(4985)
N157 Naltrindole isothiocyanate hydrochloride solid Selective irreversible δ2 opioid receptor antagonist.