Dopamine Receptor Modulator

Glovadalenum (Glovadalen) is an orally active, selective, blood-brain barrier permeable positive allosteric modulator of dopamine D1 receptor. Glovadalenum selectively enhances the efficacy of dopamine in activating dopamine D1 receptor. Glovadalenum can be used for the research of Parkinson's disease.

AL-LAD is a 5-HT2A receptor ligand with rat K_i values of 8.1 nM and 3.4 nM. AL-LAD mediates behavioral responses characteristic of serotonergic psychedelics. AL-LAD induces the head-twitch response in male C57BL/6J mice in an inverted-U-shaped dose-dependent manner. AL-LAD exhibits LSD-like behavioral effects in male C57BL/6J mice.

Raxlaprazine etomoxil is a small molecule compound with dopamine D2 and D3 receptor modulating activity, which has potential application value in research related to mental illnesses. Raxlaprazine etomoxil exhibits high affinity for human recombinant D2L receptors, with an inhibition constant (K_i) of 1.95 nM. Raxlaprazine etomoxil effectively inhibits forskolin-stimulated cAMP accumulation, with an half maximal effective concentration (EC₅₀) of 3.72 nM in functional activity experiments.

MIF-1 (Melanostatin), an endogenous brain peptide, is a potent dopamine receptor allosteric modulator. MIF-1 inhibits melanin formation. MIF-1 blocks the effects of opioid receptor activation to modulate the analgesic effects. MIF-1 accesses from the blood to the CNS by directly crossing the blood-brain barrier (BBB).

5-HT_1AR agonist 2 (Compound 4f) is a 5-HT_1A receptor agonist (K_i: 10.0 nM). 5-HT_1AR agonist 2 also binds to the SERT, D₂ receptor and 5-HT₆ receptor (K_i: SERT, 2.8 nM; D₂, 23 nM; 5-HT₆, 192 nM). 5-HT_1AR agonist 2 is stabilized in microsomes and induces hypothermia in mice.

UNC10062 is a dopamine D1 receptor (D1R) positive allosteric modulator. UNC10062 specifically binds to the extracellular allosteric pocket (upper pocket) at the interface of transmembrane helices (TM) 1 and 7 of D1R. UNC10062 can increase dopamine potency and D1R-mediated cAMP production. UNC10062 can be used for the research of neurological disease, such as Parkinson's disease.

Nooglutil (Nooglutyl; ONK-10) is a positive modulator of AMPA-type glutamate receptors (AMPARs). Nooglutil also regulates dopamine D2 receptor function to exert anxiolytic effects. Nooglutil is promising for research of neurodegenerative disorders (e.g., Alzheimer’s disease).

BP 897 hydrochloride is a potent and partial dopamine D3 receptor agonist and a weak D2 receptor antagonist. BP 897 hydrochloride displays a high affinity at the dopamine D3 receptor (K_i=0.92 nM) and a 70 times lower affinity at the D2 receptor (K_i=61 nM).

Lumateperone-¹³C,d₃ (ITI-007-¹³C,d₃) tosylate is ¹³C and deuterium labeled Lumateperone (tosylate). Lumateperone (ITI-007) tosylate is a 5-HT2A receptor antagonist (Ki = 0.54 nM), a partial agonist of presynaptic D2 receptors and an antagonist of postsynaptic D2 receptors (Ki = 32 nM), and a dopamine D1 receptor modulator. Lumateperone tosylate has anticancer activity and can also be used in studies of psychiatric disorders such as schizophrenia.

OPC-4392 is a orally active presynaptic dopamine autoreceptor agonist and postsynaptic D2 receptor antagonist. OPC 4392 reverses the Reserpine (HY-N0480)-induced dopamine accumulation, inhibits Apomorphine (HY-12723)-induced stereotypic and climbing behaviors in mouse models. OPC-4392 can be used as antipsychotic agent.

UNC9815 is a D1 dopamine receptor (D1R) orthosteric allosteric modulator (PAM). UNC9815 can dose-dependently enhance the functional efficacy of dopamine in β-inhibitory protein recruitment experiments and cAMP accumulation experiments. When used in combination with other PAMs, UNC9815 exhibits a significant synergistic enhancement effect. UNC9815 can be used to study neurological and psychiatric diseases such as Parkinson's disease and schizophrenia.

Dopamine D2 receptor agonist-3 (compound 3) is a selective D2 receptor partial agonist and Dopamine D3 receptor antagonist (with pEC₅₀ of 8.3 and <5.5 respectively).

Deulumateperone is a deuterium labeled Lumateperone (HY-17637). Lumateperone is the orally active 5-HT2A receptor antagonist (K_i = 0.54 nM) and the modulator for dopamine receptor that exhibits antipsychotic and antineoplastic activities.

Dopamine D2 receptor modulator-1 is a positive allosteric modulator of hD2R. Dopamine D2 receptor modulator-1 enhances the potency of Dopamine (HY-B0451) on hD2R without intrinsic agonist activity. Dopamine D2 receptor modulator-1 protects dopaminergic differentiated cells from neurotoxic damage. Dopamine D2 receptor modulator-1 exhibits neuroprotective activity. Dopamine D2 receptor modulator-1 can be used in the research of Parkinson's disease.

Lumateperone-d₄ tosylate (ITI-007-d₄ tosylate) is the deuterium labeled Lumateperone tosylate (HY-19733). Lumateperone (ITI-007) tosylate is a 5-HT2A receptor antagonist (Ki = 0.54 nM), a partial agonist of presynaptic D2 receptors and an antagonist of postsynaptic D2 receptors (Ki = 32 nM), and a dopamine D1 receptor modulator. Lumateperone tosylate has anticancer activity and can also be used in studies of psychiatric disorders such as schizophrenia.

BRL-44408 is a selective, blood-brain barrier-permeable α₂A-adrenergic receptor antagonist with a K_i value of 8.56 nM against human targets. BRL-44408 exhibits activities such as antidepressant, analgesic effects and attenuation of sepsis-induced acute lung injury by regulating the release of neurotransmitters such as norepinephrine and dopamine, or inhibiting signaling pathways including ERK1/2, p38MAPK and p65. BRL-44408 can be used in studies related to acute respiratory distress syndrome, depression and visceral pain.

NEO 376 is a selective modulator of 5-HT1 receptor, GABA receptor and dopamine receptor, with anti-psychotic actively.

5-HT₇R antagonist 3 (Compound 6.4) is a selective 5-HT₇R antagonist (K_i: 8 nM), with K_i of 511 nM (D₂), 8930 nM (5-HT_1A) and 5786 nM (5-HT_2A), respectively. 5-HT₇R antagonist 3 possesses antidepressant and anxiolytic effects in mice.

MeSeI exhibits a weak inhibitory activity against monoamine oxidase MAO-A and MAO-B (IC₅₀=198.8 µM). MeSeI regulates dopamine receptor D2 and norepinephrine receptor α2, β1, and exhibits antidepressant-like effect in mice. MeSeI is orally active.

ETH-LAD (N-Ethyl-nor-LSD) is an activator for 5-HT2A receptor with K_i of 5.1 nM. ETH-LAD exhibits affinity for dopamine receptor D1 and dopamine receptor D2 with K_i of 22.1 nM and 4.4 nM. ETH-LAD acts as psychoactive substance in rat model.