mk 801

Dizocilpine Maleate (MK-801 maleate) is a potent, selective, and non-competitive NMDA receptor antagonist with a Kd value of 37.2 nM. It is commonly used in the treatment of various neurodegenerative diseases in which NMDA receptors may be involved, and can also be used to induce schizophrenia models.

Dizocilpine (MK-801) is a selective non-competitive NMDA receptor antagonist with a Kd of 37.2 nM that exhibits anticonvulsant effects. It acts by binding to a site within the NMDA-associated ion channel, blocking the flow of Ca²⁺, and is commonly used to establish schizophrenia models.

(-)-Dizocilpine maleate ((-)-MK 801 (Maleate)) is a potent, selective, and non-competitive NMDA receptor antagonist, with a Kd of 37.2 nM in rat brain membranes.

5-HT2A 5-HT2C inverse agonist 1 serves as a dual and potent inverse agonist for the 5-HT2A and 5-HT2C receptors, with hERG inhibition properties that mitigate cardiovascular risks. Demonstrating significant antipsychotic efficacy in the MK-801-induced mouse model, this compound holds potential for psychosis research.

VU6024578 (BI02982816) is an orally bioavailable and selective positive allosteric modulator (PAM) of the metabotropic glutamate receptor mGluR1. It demonstrates activation with EC50 values of 54 nM for human mGluR1 and 46 nM for rat mGluR1. VU6024578 shows antipsychotic activity in rat models of amphetamine-induced hyperactivity and MK-801-induced novel object recognition (NOR). Additionally, it possesses blood-brain barrier permeability.

VU6033685 is an orally effective positive allosteric modulator (PAM) of mGlu1, capable of positively modulating human mGlu1 and mGlu5, with EC50 values of 39 nM and 3960 nM, respectively. Additionally, VU6033685 inhibits CYP1A2, CYP2C9, and CYP2D6 with IC50 values of 26, 22.3, and 23.8 μM. It reverses amphetamine-induced hyperactivity in rats and protects against MK-801-induced cognitive deficits. VU6033685 demonstrates favorable pharmacokinetic properties in rats, with an oral bioavailability of 42.8%.

ONO-TR-772 (VU6018042) is a selective TREK inhibitor with an IC50 of 15 nM. It improves recognition memory in the NOR mouse model induced by MK-801. ONO-TR-772 is useful in research on diseases associated with cognitive impairment.

ZH8965 is an orally active TAAR1-Gs/Gq agonist (EC50: 6.1/14.8 nM) that shows efficacy in alleviating antipsychotic-like phenotypes and cognitive deficits in an MK-801-induced psychosis model in mice. It is applicable for research related to schizophrenia.

Compound 8 (5-HT6R antagonist 1), a 5-HT6R antagonist (K i : 5 nM), not only demonstrates inhibition of platelet aggregation and excellent metabolic stability but also reverses MK-801-induced memory impairments in rats, suggesting its utility in Alzheimer's disease (AD) research [1].

Ampullosporin A is a peptaibol-type polypeptide isolated from the fungus Sepedonium ampullosporum (HKI-0053), exhibiting neuromodulatory activity. It inhibits hyperactivity induced by the NMDA receptor antagonist MK-801 and ameliorates social behavior abnormalities caused by subchronic ketamine treatment. Ampullosporin A modulates glutamate receptor activity without affecting dopamine D1 and D2 receptors.