postsynaptic

L-Phenylalanine (3-Phenyl-L-alanine) is an essential amino acid and the precursor of the amino acid tyrosine, acts as an antagonist at α2δ calcium channels.

Nefazodone hydrochloride (Serzone) is a serotoninergic modulating antidepressant that is used in therapy of depression, aggressive behavior and panic disorder.

(+)-Coclaurine is a natural product.

Lumateperone (ITI 722) is a 5HT2A receptor antagonist and a dopamine receptor phosphoprotein modulator (DPPM).

Ro 67-7476 is a positive allosteric modulator of mGluR1, which can enhance the calcium release induced by glutamate in HEK293 cells expressing rat mGluR1a. The EC50 is 60.1 nM. It is a P-ERK1/2 agonist, and can activate ERK1/2 phosphorylation without the addition of exogenous glutamate (EC50 = 163.3 nM).

lumateperone Tosylate (ITI-007) is a 5-HT2A receptor antagonist (Ki: 0.54 nM), a SERT blocker (Ki: 61 nM), a partial agonist of presynaptic D2 receptors and an antagonist of postsynaptic D2 receptors (Ki: 32 nM).

Dopamine hydrochloride (ASL279) is a natural catecholamine neurotransmitter that mainly acts on dopamine receptors (D1-5 receptors) (EC50=2.7 nM). Dopamine hydrochloride induces VEGFR2 endocytosis through D2 dopamine receptor and has pro-angiogenic activity.

Lesopitron is an anxiolytic with pre- and postsynaptic 5-HT1A agonist activity and is more effective than 5-HT1A agonists in rat social interaction and marmoset anxiety models. lesopitron counteracts benzodiazepine withdrawal-induced anxiety in rodents with low acute toxicity and does not potentiate the effects of alcohol or barbiturates.

Doxazosin mesylate (UK 33274 mesylate)(UK 33274) is a quinazoline-derivative. It is a selectively antagonizes postsynaptic α1-adrenergic receptors.

Phenoxybenzamine hydrochloride (NCI-c01661) is the hydrochloride salt form of phenoxybenzamine, a synthetic, dibenzamine alpha-adrenergic antagonist with antihypertensive and vasodilatory properties. Phenoxybenzamine non-selectively and irreversibly blocks the postsynaptic alpha-adrenergic receptor in smooth muscle, thereby preventing vasoconstriction, relieving vasospasms, and decreasing peripheral resistance. Reflex tachycardia may occur and may be enhanced by blockade of alpha-2 receptors which enhances norepinephrine release. Phenoxybenzamine is reasonably anticipated to be a human carcinogen.

Yohimbine hydrochloride is a plant-derived alkaloid with alpha-2 adrenergic receptor blocking activity. By blocking presynaptic or postsynaptic alpha-2 adrenergic receptors, it promotes the release of norepinephrine and dopamine. It has been used in studies related to mydriasis and erectile dysfunction and is commonly used to induce hypertension models.

Dantrolene is a postsynaptic muscle relaxant by inhibiting Ca2+ ions release from sarcoplasmic reticulum stores by antagonizing ryanodine receptors.

Pyridostigmine(Regonol) is an acetylcholinesterase inhibitor that can treat myasthenia gravis by increasing acetylcholine at the postsynaptic motor endplate.

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)

Fluphenazine Decanoate Dihydrochloride is an antipsychotic agent, it could block postsynaptic dopamine D2 receptors in the limbic, cortical system and basal ganglia.

Flufenazine is an antipsychotic drug. It is used to treat chronic mental illnesses such as schizophrenia. Flufenazine works by blocking postsynaptic dopamine D2 receptors in the limbic system, cortical system, and basal ganglia. This prevents the effects

Tat-NR2B9c (NA-1) is a postsynaptic density-95 (PSD-95) inhibitor with neuroprotective and antiepileptic effects.Tat-NR2B9c inhibits PSD-95d2, PSD-95d1, and PSD-95, which prevents the activation of NMDA-induced NADPH oxidase in neurons, thereby blocking the production of superoxide, which reduces ischemic injury in the acute phase after stroke.

Tat-NR2B9c TFA is a 20-aa peptide, and acts as an inhibitor of postsynaptic density-95 (PSD-95)(EC50 of 6.7 nM for PSD-95d2), and possesses neuroprotective efficacy.

Tat-NR2B9c acetate (NA-1 acetate) is a postsynaptic density-95 (PSD-95) inhibitor, with EC50 values of 6.7 nM and 670 nM for PSD-95d2 (PSD-95 PDZ domain 2) and PSD-95d1, respectively. Tat-NR2B9c acetate disrupts the PSD-95/NMDAR interaction, inhibiting NR2A and NR2B binding to PSD-95 with IC50 values of 0.5 μM and 8 μM, respectively. Tat-NR2B9c acetate also inhibits neuronal nitric oxide synthase (nNOS)/PSD-95 interaction, and possesses neuroprotective efficacy.

Tiodazosin is a competitive antagonist of the postsynaptic alpha-adrenergic receptor.

Doxazosin D8 (UK 33274 D8) is a deuterium labeled Doxazosin (UK 33274).Doxazosin, a quinazoline derivative, selectively antagonizes postsynaptic AP1 adrenergic receptor.

RDS-127 induces biphasic dose-related changes in spontaneous locomotor activity in rats, similar to the reported effects of APO. Compared to APO, RDS-127 demonstrates a more potent stimulation of movement, with an efficacy that is tripled and lasts four times longer. In terms of selectivity, RDS-127 clearly outperforms APO, showing a preference for activating DA autoreceptors in the nigrostriatal pathway rather than postsynaptic DA receptors.

Gamma-DGG TFA is an antagonist of excitatory amino acids that can inhibit depolarization induced by NMDA, Kainate, and Quisqualate. In addition, it counteracts excitatory postsynaptic potentials (e.p.s.p.) in rat hippocampal slices.

Fluphenazine hydrochloride is an effective, orally active phenothiazine class dopamine receptor (dopamine receptor) antagonist. It blocks voltage-gated sodium ion channels (sodium channels) in neurons. The compound primarily exerts its effects by antagonizing postsynaptic dopamine-2 receptors in mesolimbic, nigrostriatal, and tuberoinfundibular pathways. It counteracts stereotypy induced by methylphenidate in mice and suppresses climbing behavior. Fluphenazine hydrochloride is used in studying psychoses and diabetic-related painful peripheral neuropathy, with potential to inhibit SARS-CoV-2.