Alsevetin-OA (TLR-6124) is an optimized agent expressing potent alpha7 NAChR partial agonist activity with moderate efficacy and a high therapeutic index, devoid of tolerance inducing effects.
Indications for focus/ADHD, nootropic, anti-addiction, analgesic-sparing research.
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Alsevetin-OA (TLR-6124) is an optimized agent expressing potent alpha7 NAChR partial agonist activity with moderate efficacy and a high therapeutic index, lacking of tolerance inducing effects.. Based off the EVP-6124 model of alpha7 NAChR partial agonist therapeutic efficacy, Alsevetin-OA (TLR-6124) is a selective alpha7 NAChR moderate efficacy partial agonist. In animal assays Alsevetin-OA (TLR-6124) demonstrated comparable effects relative to that of EVP-6124 with approximately 20% the potency, as such requiring a dosing of 5x that of EVP-6124 (0.1mg/kg and 0.05mg/kg respectively per oral administration in mice) to elicit comparable effects.
Alsevetin-OA (TLR-6124) as well acts in a synergistic manner with prototypical PDE4 inhibitors, such as Roflumilast, and enhances the therapeutic index of these agents.
Alsevetin-OA (TLR-6124) displays potential benefit within anti-addiction and tolerance reduction protocols demonstrating a significant effect in reduction of naloxone and naltrexone induced opioid withdrawal symptoms and reversal of tolerance to opioid analgesics. Anti-addiction effects were seen to be more pronounced with dosing administrations 2-3x that the dose required for alpha7 related efficacy indicating another pathway of action being involved at higher doses.
Alsevetin-OA (TLR-6124) has indication as both a safe and non-tolerance inducing pro-cognitive agent, particularly with co-administration of PDE4i agents; as well as to promote a strong adjunctive addiction cessation potentiation in coordination with other agents such as ADDX-OX, guanfacine, LORA-OX, et. al. Potentials for adjunct coordination for smoking cessation appear highly promising.
Alsevetin-OA (TLR-6124) itself demonstrated no tendency to any signs of tolerance within assays.
Theoretical Potential Human Clinical Trial Protocol Estimations:
Alsevetin-OA (TLR-6124) dosing estimates as relates to any potential future human clinical trials, based off the animal data available, correlate to be anticipated at 5-10mg b.i.d. for ADHD and Alzheimer's Disease as well as for analgesic sparing and anti-addiction.
All data appears to indicate highest safety potential and high efficacy for strongest therapeutic index and optimized treatment.
Solubility: Supplied as a HCl salt soluble to 80mg/ml in water
USAGE: For Research Use Only! Not For Use in Humans.