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.
In human immunodeficiency (HIV)-1 seropositive patients, BD 1047 along with other antioxidants may aid in reduction of cathepsin B- based neuropathology.
 
N1771 nor-Binaltorphimine dihydrochloride Highly selective k-opioid receptor antagonist. nor-Binaltorphimine has antidepressant properties.
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)
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.
 
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.
human ... OPRM1(4988)
N4396 Nalbuphine hydrochloride hydrate ≥98% (HPLC) Partial agonist for μ and κ opioid receptors.
human ... OPRD1(4985), OPRK1(4986), OPRM1(4988)
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. Naloxone′s antagonistic effect last for about 45 min and thus, requires repeated dosage. It results in critical side effects such as pulmonary edema.
human ... OPRD1(4985), OPRK1(4986), OPRM1(4988), OPRS1(10280)
N129 Naloxone methiodide ≥98% (HPLC), solid 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.
 
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)