non-opioid

SNC 80 (NIH 10815) is a potent, highly selective and non-peptide δ-opioid receptor agonist, Ki = 1.78 nM, IC50 = 2.73 nM. SNC80 also selectively activates μ-δ heteromer in HEK293 cells with an EC50 of 52.8 nM. SNC80 shows antinociceptive, antihyperalgesic and antidepressant‐like effects. SNC80 has the potential for multiple headache disorders treatment.

AT-121 is a dual μ-opioid and neuropeptide receptor partial agonist (Kis 16.49 and 3.67 nM, respectively). It stimulates [35S]GTPγS binding to cell membranes expressing either μ-opioid receptors or neuropeptide receptors (EC50s of 19.6 and 34.7 nM, respectively.) AT-121 (0.003-0.03 mg/kg) reduced capsaicin-induced thermal anisocoria in a dose-dependent manner, but did not increase scratching activity in rhesus monkeys. In rhesus monkey drug self-administration tests, AT-121 at doses of 0.3 to 10 μg/kg per injection lacked reinforcing effects (a potential marker of abuse) and did not reduce the reinforcing effects of food pellets.AT-121 (0.01 or 0.03 mg/kg) did not induce hyperalgesia, a marker of tolerance, in rhesus monkeys.AT-121 is a safe non-addictive pain reliever with anti-injury and analgesic effects.

Vocacapsaicin hydrochloride (CA-008 hydrochloride) is a non-opioid TRPV1 agonist, a raw material for capsaicin, and is used for pain relief.

Ziconotide Acetate (107452-89-1 free base) (Prialt) is an analgesic agent and has been used to treat neuropathic and non-neuropathic pain. Ziconotide Acetate (107452-89-1 free base) acts by binding to N-type calcium channels situated on the terminal part of primary afferent neurons of the nociceptive pathway therefore reducing synaptic transmission with potent antinociceptive effects.

Opiranserin (VVZ-149) hydrochloride is a dual antagonist of glycine transporter type 2 (GlyT2) and serotonin receptor 2A (5HT2A), with IC50s of 0.86 and 1.3 μM, respectively. It shows antagonistic activity on rP2X3 (IC50=0.87 μM). It is development as an injectable agent for the treatment of postoperative pain.

TAN67 is the first effective selective non-peptide delta1 opioid receptor.

Unifiram is a nootropic agent.1It increases acetylcholine (ACh) release in the rat cerebral cortexin vivoand induces a long-lasting increase in the amplitude of field excitatory postsynaptic potentials (fEPSPs) in the rat hippocampal CA1 region (EC50= 27 nM). It does not bind to serotonin (5-HT), dopamine, muscarinic, nicotinic, adrenergic, glutamate, histamine, opioid, or GABA receptors at 1 μM. Unifiram (0.1 mg/kg) improves memory in non-memory-impaired rats in a social learning test.2It also prevents memory deficits induced by the anticholinergic agent scopolamine, nicotinic receptor antagonist mecamylamine, GABABreceptor agonist baclofen, or α2-adrenergic receptor agonist clonidine in the passive avoidance test in mice when administered at a dose of 0.01 mg/kg and prevents memory deficits induced by the AMPA/kainate glutamate receptor antagonist NBQX at 0.1 mg/kg.1 1.Romanelli, M.N., Galeotti, N., Ghelardini, C., et al.Pharmacological characterization of DM232 (unifiram) and DM235 (sunifiram), new potent cognition enhancersCNS Drug Rev.12(1)39-52(2006) 2.Ghelardini, C., Galeotti, N., Gualtieri, F., et al.The novel nootropic compound DM232 (unifiram) ameliorates memory impairment in mice and ratsDrug Develop. Res.56(1)23-32(2002)

Flupirtine maleate (Katadolon maleate), a centrally acting non-opioid analgesia, is the salt form of Flupirtine. It is an NMDA receptor antagonist , and also a specific neuronal potassium channel opener.

Bicifadine, also known as DOV-220075, CL 220,075, is a SNDR inhibitor potentially for the treatment of lower back pain. Bicifadine has a non-opioid, non-NSAID mechanism for the treatment of pain, which should have less abuse potential than opioid drugs and less propensity to cause gastric ulcers than NSAID drugs. While the drug is purported to be a serotonin (SERT) and noradrenaline transporter (NET) inhibitor, it also has effects at the dopamine transporter (DAT), effectively making it a broad-spectrum monoamine transporter inhibitor or triple reuptake inhibitor.

Flupirtine HCl is the salt form of Flupirtine, also known as W-2964, an aminopyridine that functions as a centrally acting non-opioid analgesic. It first became available in Europe in 1984, and is sold mainly under the names Katadolon, Trancolong, Awegal, Efiret, Trancopal Dolo, and Metanor. Like nefopam, it is unique among analgesics in that it is a non-opioid, non-NSAID, non-steroidal centrally acting analgesic. Flupirtine is a selective neuronal potassium channel opener that also has NMDA receptor antagonist and GABAA receptor modulatory properties.

Enkephalin-leu, ala(2)-ser(6)- is an active compound at the delta (non-complexed) opioid receptor.

Exp 631 is a centrally-acting non-opioid analgesic; exhibits serotonin and norepinephrine reuptake inhibiting activities.

Vocacapsaicin (CA-008), a prodrug of Capsaicin and a first-in-class non-opioid TRPV1 agonist, offers significant and enduring pain relief.

Opiranserin is a development as an injectable agent for the treatment of postoperative pain. Opiranserin is a non-opioid and non-NSAID analgesic candidate and is a dual antagonist of glycine transporter type 2 (GlyT2) and serotonin receptor 2A (5HT2A) (IC50s: 0.86 and 1.3 μM, respectively). Opiranserin displays antagonistic activity on rP2X3 (IC50=0.87 μM).

AT-121 hydrochloride is a dual agonist of nociception and mu opioid receptor with Ki values of 3.67 and 16.49 nM, respectively.AT-121 hydrochloride is a safe, non-addictive, pain relieving compound with anti-injury and analgesic activity. AT-121 hydrochloride is a safe, non-addictive, pain relieving compound with anti-injury and analgesic activity.

(Rac)-SNC80, a racemate of SNC80 (NIH 10815), is a potent, highly selective non-peptide δ-opioid receptor agonist, characterized by a K_i of 1.78 nM and an IC_50 of 2.73 nM. Demonstrating antinociceptive, antihyperalgesic, and antidepressant-like effects, SNC80 holds potential for the treatment of multiple headache disorders [1] [2] [3] [4] [5] [6].

Nefopam hydrochloride (Nefopam HCl) is the hydrochloride salt form of nefopam, a centrally-acting, non-opioid benzoxazocine with analgesic activity.

LIH383 is a peptide agonist specifically designed to activate the chemokine (C-X-C motif) receptor 7 (CXCR7), which functions both as a chemokine and an opioid peptide scavenger receptor. Demonstrating a high selectivity, LIH383 activates CXCR7 with an effective concentration (EC50) of 0.61 nM, showing significantly lower affinity towards μ-, δ-, and κ-opioid receptors, as well as the nociceptin opioid peptide (NOP) receptor, even at concentrations of 3 µM in β-arrestin recruitment assays. Furthermore, at a concentration of 3 µM, LIH383 effectively inhibits the uptake of opioid peptides by CXCR7, a process normally induced by dynorphin A, a non-selective opioid receptor agonist, in U87-ACKR3 cells.

DDD-028 is a potential non-opioid and non-cannabinoid analgesic. It was used for treating neuropathic and inflammatory pain.

Gaboxadol hydrobromide is a GABA agonist. It is an inhibitor of GABA uptake systems. Gaboxadol can also be a non-opioid analgesic and a novel type of hypnotic.

A-286501 is an orally active adenosine kinase inhibitor (IC50=0.47 nM). A-286501 effectively attenuates nociception by a non-opioid, non-non-steroidal anti-inflammatory drug ADO, receptor mediated mechanism.

Tebanicline hydrochloride (Ebanicline hydrochloride) , is an effective synthetic nicotinic (non-opioid) analgesic drug.

Lappaconitine HCl is a centrally acting non-opioid analgesic and class-I antiarrhythmic. It acts by binding to the site-2 receptor and irreversibly blocking hH1 sodium channels.

Matrine (Vegard), an alkaloid isolated from the Sophora genus, acts as a kappa opioid receptor agonist.

Elismetrep is a non-opioid analgesic.

FR64822(N-(4-pyridylcarbamoyl)amino 1,2,3,6,-tetrahydropyridine), a novel non-opioid antinociceptive compound, displays antinociceptive activities in a variety of assays with mice and rats. It has a strong antinociceptive activity in the acetic acid writh

non-peptide δ1 opioid receptor agonist

Nepinalone is an alchilaminate derivative of β-tetralone. Nepinalone is an orally active cough suppressant that possesses a non-opioid antitussive activity [1].

Nepinalone hydrochloride, a non-opioid antitussive, is an alchilaminate derivative of β-tetralone. This orally active compound effectively suppresses coughing.

Levallorphan tartrate is an opioid antagonist with properties similar to those of NALOXONE. Levallorphan reverses severe opioid-induced respiratory depression but may exacerbate respiratory depression such as that induced by alcohol or other non-opioid ce

Tebanicline is a potent synthetic nicotinic (non-opioid) analgesic drug. It was developed as a less toxic analogue of the potent poison dart frog-derived compound epibatidine. Like epibatidine, tebanicline showed potent analgesic activity against neuropat

L-Sophoridine (Matridin-15-one) , a natural product obtained from medicinal plants, which has a variety of pharmacological effects, including anti-Y effects, and selectively induces apoptotic cell death in a variety of human Y cells in vitro and in vivo; however, its mechanism of action needs to be further elaborated.