Opioid Agonists

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P134 (−)-Pentazocine ≥98% (HPLC)  
U111 (−)-trans-(1S,2S)-U-50488 hydrochloride hydrate solid, ≥98% (HPLC) Potent κ opioid receptor agonist; more potent enantiomer of (±)-trans-U-50488.
M0267 (±)-Methadone hydrochloride powder, ≥98% (TLC) μ opioid receptor agonist that desensitizes both the μ opioid receptor and the δ opioid receptor on chronic exposure; narcotic analgesic, characterized by a gradual onset of action and prolonged, milder withdrawal; may also block L-type calcium channels independently of its effects on opioid receptors.
D8040 (±)-trans-U-50488 methanesulfonate salt Selective κ-opioid receptor agonist.
P127 (+)-Pentazocine solid σ receptor agonist; active enantiomer of pentazocine.
A114 (+)-N-Allylnormetazocine hydrochloride ≥98% (HPLC) Selective σ1 receptor agonist.
SML1017   Acetyl fentanyl ≥98% (HPLC) Acetyl fentanyl is an impurity formed in the production process of fentany, and is a very potent μ opiod receptor agonist.
SML1261 Asimadoline hydrochloride ≥98% (HPLC) Asimadoline is a potent and selective κ-opioid agonist that does not penetrate the blood-brain barrier. Asimadoline produces both analgesic and antidiarrheal effects.
SML0917   BMS-986122 ≥98% (HPLC) BMS-986122 is a positive allosteric modulator (PAM of the m-opioid receptor). BMS986122 displays little or no agonist activity alone, but dose dependently increases endomorphin-I induced b-arrestin recruitment, and inhibition of forskolin-induced adenyl cyclase activity. The compound also potentiates DAMGO-stimulated GTPgS receptor binding.
B8930 BW373U86 dihydrobromide powder Potent, non-peptide δ-opioid receptor agonist.
SML0299 Biphalin trifluoroacetate salt ≥97% (HPLC) Biphalin is a dimeric enkephalin that is a potent and non-selective opioid receptors (OR) agonist. It displays a high analgesic potency that is over 1000-fold greater than morphine. Studies show that biphalin exhibits neuroprotective effects in rat models of stroke.
B9275 Buprenorphine hydrochloride Full agonist at ORL1 receptors, antagonist or partial agonist at μ, κ, and δ opioid receptors.
B1935 Butorphan S(+)-mandelate ≥98% (HPLC), solid κ/μ opioid receptor agonist.
B9156 Butorphanol (+)-tartrate salt ≥99% κ/μ opioid receptor agonist.
SML0980   CYM51010 ≥98% (HPLC) CYM51010 is a biased ligand of μ-opioid receptor – δ-opioid receptor heterodimers. CYM51010 exhibits anti-nociceptive activity similar to morphine, but with a decreased levels of tolerance development and withdrawal symptoms.
C4662   Carbetapentane citrate salt High affinity σ1 agonist; ORL1 antagonist; antitussive.
C5901 Codeine monohydrate analytical standard Weak narcotic analgesic, perhaps due to conversion to morphine, with minimal hypnotic properties; potent antitussive
SML0829   Dermorphin trifluoroacetate salt ≥98% (HPLC) Dermorphin is a natural opioid originally isolated from the skin of South American frogs Dermophin has high selectivity as a μ-Opioid receptor (MOR) agonist and is 30–40 times more potent than morphine.
E8512 Ethylmorphine Narcotic analgesic; antitussive
F3886 Fentanyl citrate salt Phenylpiperidine analgesic that is 80 times more potent than morphine as an analgesic and 6000 times more potent than morphine as a μ opioid receptor agonist.
G133 GR 89696 fumarate salt solid Selective κ2 opioid receptor agonist.
H4516 Hydrocodone (+)-bitartrate salt μ opioid receptor agonist; narcotic analgesic and antitussive.
H5136 Hydromorphone hydrochloride Narcotic opiate analgesic; μ opioid receptor agonist.
I122 ICI 204,448 hydrochloride solid κ opioid receptor agonist that does not cross the blood-brain barrier.
SML1461 Kyotorphin acetate salt ≥98% (HPLC) Kyotorphin is a neuroactive dipeptide (Tyr-Arg) shown to have analgesic, neuroprotective, and neuromodulatory properties. It is synthesized in nerve terminals and found in the brain and in cerebro-spinal fluid (CSF). Kyotorphin indirectly stimulates opioid receptors by releasing methionine enkephalin (met-enkephalin). CSF levels are lower in patients with persistent pain and in patients with Alzheimer’s disease.
L8539 L-687,384 hydrochloride ≥98% (HPLC), powder σ1 receptor agonist.
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.
L3669 LPK-26 ≥98% (HPLC), powder LPK-26 is an analog of ICI-199441 and (-)U50,488H (classic kappa agonists). It has extremely high kappa affinity (0.64 nM) and low mu and delta receptor affnities (1170 and 10,000nM). LPK-26 produces an antinocicpetive effect with much higher potency in vivo than morphine or U50488. LPK-26 does not produce physical dependence in mice, but it does suppress naloxone-induced behavioral effects in mice treated with morphine.
L5143 Levorphanol (+)-tartrate salt dihydrate white powder, ≥98% (HPLC) Synthetic morphine analog that is a narcotic analgesic and μ opioid receptor agonist.
PZ0159 MCOPPB trihydrochloride hydrate >98% (HPLC) MCOPPB trihydrochloride is a potent non-peptide nociceptin/orphanin FQ peptide (NOP)-receptor full agonist [or opioid-receptor-like-1 (ORL1) receptor agonist]. MCOPPB is the most potent novel non-peptide NOP full agonist in vitro and an orally potent anxiolytic in the mice. It inhibited signaling through the NOP receptor in the mouse brain, suggesting that it penetrated into the brain after it was orally administered. It did not affect locomotor activity or memory, nor did it contribute to ethanol-induced hypnosis.
SML1140 ML138 ≥98% (HPLC) ML138 (CID 44601470) is a highly selective agonist at kappa opioid receptors (KOR) that potently activate G protein coupling but weakly interact with β arrestin2.
M3142 Meperidine hydrochloride Phenylpiperidine analgesic; sedative; μ opioid receptor agonist with greater κ opioid receptor agonist activity than morphine.
M3528 Morphine 6-β-D-glucuronide hydrate ≥90% (HPLC) Major metabolite of morphine that is a potent μ−opioid receptor agonist.
M8777 Morphine sulfate salt pentahydrate Narcotic analgesic; prototypic μ opioid receptor agonist; also agonist at κ opioid receptors.
SML0791 N,N-Dimethyltryptamine ≥97% (HPLC) N,N-Dimethyltryptamine (DMT) is a hallucinogen now known to be an endogenous sigma-1 receptor agonist. In keeping with the known sigma-1 receptor modulation of voltage gated Na+ channels, DMT was found to reversibly inhibit Na currents by 62% in vitro. N,N-Dimethyltryptamine also induced hypermotility in WT mice (but not in sigma-1 KO mice), all evidence of its sigma-1 agonist activity.
N165 Naloxone benzoylhydrazone solid Agonist for κ3 opioid receptors; antagonist for ORL1 and μ opioid receptors.
O5889 Opipramol dihydrochloride ≥98% (HPLC), solid σ12 opioid receptor agonist; an antagonist at D2, 5HT2 and H1 receptors; atypical antidepressant, antipsychotic and anxiolytic
P9246 PB28 dihydrochloride ≥98% (HPLC), solid Selective σ2 opioid receptor ligand; putative σ2 agonist
P2607 PRE-084 solid Potent and highly selective σ1 opioid receptor agonist.
P3029 Phencyclidine hydrochloride σ opioid receptor agonist and psychostimulant; inhibits NMDA glutamate receptor activation by binding to an allosteric site within the ion channel.
R1908 Remifentanil hydrochloride ≥97% (HPLC), powder Remifentanil hydrochloride is a mu opioid receptor agonist, anesthetic, and analgesic compound. Remifentanil was developed as an ultra-short-acting mu opioid receptor agonist with improved pharmacodynamic properties.
S2812 SNC80 ≥98% (HPLC), solid SNC80 is a δ opioid receptor agonist.
SNC80 is a highly selective agonist of δ opioid receptor but also binds to μ-δ opioid receptor heteromers to produce antinociception in mice.2 It also acts as anti-depressant3, elicits dopamine-related behaviors and enhances behavioral responses to psychostimulants.4
SML0398 Salsolinol hydrobromide ≥96% (HPLC) Salsolinol is the condensation product of acetaldehyde and dopamine. Salsolinol is a potential neurotoxin suspected to contribute to alcohol abuse. It appears that salsolinol excites the ventral tegmental area (VTA) dopamine neurons indirectly by activating μ-opioid receptors (MORs), which inhibit GABA neurons in the VTA.
S8071 Salvinorin A ≥98% (HPLC), powder Salvinorin A is a potent, non-nitrogenous κ opioid selective receptor agonist. Salvinorin A is isolated from Salvia divinorum. Salvinorin A displays high affinity at both native (Ki=4.3 nm) and cloned (Ki=16 nm) κ -opioid receptors. Preliminary studies suggest that Salvanorin A is chemically unique among the psychtropic drugs and does not bind to any known receptor.
SML0976   Siramesine fumarate salt ≥98% (HPLC) Siramesine is a blood-brain barrier penetrant, selective and potent sigma-2 receptor agonist, which exhibits potent and very long-lasting anxiolytic effects in rodents. Also, siramesine is a lysosome-destabilizing agent that causes lysosomal cell death in varies immortalized and cancer cell lines.
SML0535   Sufentanil citrate ≥98% (HPLC) Sufentanil is a mu-opioid selective agonist, 10 times more potent than fentanyl, over 1000 times more potent than morphine. Sufentanil citrate is used as an analgesic and anesthesia adjunct. There are some differences in activity and selectivity among the mu-opiate agonist analgesics. Receptor-internalizing agonists like beta-endorphin, methadone, fentanyl, and sufentanil have been found to induce NADH/NADPH-mediated reactive oxygen species (ROS) synthesis via Phospholipase D-dependent signaling pathways whereas agonists like morphine that do not induce receptor endocytosis failed to activate ROS synthesis. In another report meperidine, remifentanil and tramadol were found to interact with alpha(2)-adrenoceptors, whereas sufentanil did not.
U105 U-62066 solid Highly selective κ opioid receptor agonist; antitussive.
U103 U-69593 solid U-69593 is a selective κ opioid receptor agonist. U-69593 is known to inhibit cocaine sensitization in meso-limbic dopamine neurons by normalizing basal overflow of dopamine.