Opioid Antagonists

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M231 3-Methoxynaltrexone hydrochloride solid Putative antagonist at a novel opioid receptor that binds morphine-6-β-glucuronide; blocks endomorphin-2-induced antinociception.
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.
346438 9-[3-(cis-3,5-Dimethyl-1-piperazinyl)propyl]carbazole dihydrochloride monohydrate 97% Cocaine antagonist
SML0242 AZ-MTAB ≥98% (HPLC) AZ-MTAB is a potent, short acting κ-opioid receptor (KOR) selective antagonist.
SML1347 Alvimopan ≥98% (HPLC) Alvimopan is a gastroprokinetic peripheral mu-opioid receptor antagonist. As a drug, Alvimopan is given to patients undergoing bowel surgery to protect the bowel from the effects of opioid medications that are used to treat pain, blocking the undesirable GI side-effects of the opioid agonists without affecting analgesia or causing withdrawal. Alvimopan does not cross the blood-brain barrier, competitively binding to gastrointestinal tract mu-opioid receptors.
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.
SML0276 BD 1063 dihydrochloride ≥98% (HPLC) BD 1063 is a potent sigma(1) receptor antagonist; approximately 50-fold selective for sigma-1 over sigma-2 and 100-fold or more selective over 9 other tested neurotransmitter receptors. BD 1063 has been shown to antagonize cocaine efffects.
BM0021 BMY-14802 ≥97% (HPLC) BMY-14802 is a potent and selective sigma-1 (σ1) receptor antagonist with an IC50 value of approximately 100 nM. BMY-14802 shows low affinity at serotonin (5-HT) 1A and adrenergic σ1 receptors and minimal activity at dopamine receptors. BMY-14802 has exhibited antipsychotic activity in rodent models and anti-dyskinetic effects against L-DOPA with preservation of antiparkinsonian efficacy.
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.
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.
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.
L121 Levallorphan tartrate salt ≥98% (HPLC), powder Partial agonist (antagonist) at μ and δ 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.
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.
SML0631   NE-100 ≥98% (HPLC) NE-100 is a potent and selective σ1 receptor antagonist with an IC50 value of 1.54 +/- 0.26 nM for σ1 receptors, > 55-fold selectivity over σ2 receptors and > 6000-fold selectivity over D1, D2, 5-HT1A, 5-HT2 and PCP receptors.
N4396 Nalbuphine hydrochloride hydrate ≥98% (HPLC) Partial agonist for μ and κ opioid receptors.
N5770 Nalmefene Nonselective opioid receptor antagonist.
N176 Naloxonazine dihydrochloride hydrate powder, ≥95% (HPLC) Potent opioid antagonist that is selective for μ1 opioid receptors.
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.
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.
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.
N157 Naltrindole isothiocyanate hydrochloride solid Selective irreversible δ2 opioid receptor antagonist.
PZ0206 PF-04455242 hydrochloride ≥98% (HPLC) PF-4455242 is a selective k opioid receptor (KOR) antagonist with 20-fold selectivity for kappa over mu receptors (k Ki = 3 nM, μ Ki =64 nM). PF-4455242 is orally active, has good brain penetration in rats and was able to block the effects of the kappa agonist U50488. Studies indicate that k blockade has afforded antidepressant activity in several animal models. PF-4455242 has been in phase I clinical trials for trial for bipolar depression.
SML0571   SB-612111 hydrochloride ≥98% (HPLC) SB-612111 is a potent antagonist of the nociceptin receptor ORL-1. SB-612111 binds to ORL-1 with high affinity (Ki = 0.33 nM) but has very low affinity for classic opioid receptors. The compound SB-612111 antagonizes the anti-morphine effects of nociceptin and blocks nociceptin-induced thermal hyperalgesia.
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.
SML1397 β-Naltrexamine dihydrochloride ≥98% (HPLC) β-Naltrexamine is a potent orally available, long lasting opioid antagonist.
N1771 nor-Binaltorphimine dihydrochloride Potent and highly selective κ opioid receptor antagonist.