5-HT Receptor

Asenapine citrate, an atypical antipsychotic, is an antagonist of serotonin receptors (pK_i: 8.4-10.5), adrenoceptors (pK_i: 8.9-9.5), dopamine receptors (pK_i: 8.9-9.4) and histamine receptors (pK_i: 8.2-9.0). Asenapine citrate can be used in the research of schizophrenia and bipolar disorder.

5-HT4 antagonist 3 hydrochloride is a highly selective 5-hydroxytryptamine receptor (5-HT₄) antagonist. 5-HT4 antagonist 3 (hydrochloride) blocks muscarine receptors and sodium channels. 5-HT4 antagonist 3 (hydrochloride) can be used to evaluate function of 5-HT₄ receptor .

Lintopride hydrochloride, a benzamide, is a potent 5HT-4 antagonist with moderate 5HT-3 antagonist properties. Lintopride hydrochloride increases gastric emptying, stimulates antral and duodenal motility and accelerates intestinal transit in animal. Lintopride hydrochloride significantly increases the lower oesophageal sphincter (LOS) basal tone.

EGIS-7625 free base is an orally active and selective competitive antagonist of 5-HT2B receptor, with a human K_i value of 1 nM. EGIS-7625 free base shows low affinity for 5-HT2A and 5-HT2C receptors. The pK_i values of EGIS-7625 free base for human 5-HT2B, 5-HT2A and 5-HT2C are 9.0, 6.2 and 7.7, respectively. EGIS-7625 free base alleviates mCPP-induced hypoactivity.

SB-773812 is a moderate-affinity antagonist at dopamine receptor 2 (pKi=7.4) and a high-affinity antagonist at the dopamine receptor 3 (pKi=8.5) and at the serotonin 5-hydroxytryptamine receptors 2A (pKi=9.0), 2C (pKi=8.1), and 6 (pKi=8.1). SB-773812 is promising for research of central nervous system disorders.

Cyclobenzaprine-d3-1 hydrochloride (MK130-d3-1 hydrochloride) is the deuterium labeled Cyclobenzaprine hydrochloride (HY-B0740). Cyclobenzaprine (MK130) hydrochloride is an orally active 5-HT₂ receptor antagonist. Cyclobenzaprine hydrochloride acts centrally, providing skeletal muscle relaxation, alleviating muscle spasms, and reducing pain. Additionally, Cyclobenzaprine hydrochloride has antiprotozoal activity. Additionally, Cyclobenzaprine hydrochloride also possesses antiparasitic activity. Cyclobenzaprine hydrochloride holds promise for research in the fields of acute, painful skeletal muscle disorders and infectious diseases

FPPQ is a dual-acting 5-HT₃ (K_i = 0.9 nM) and 5-HT₆ (K_i = 3 nM) receptor antagonist with antipsychotic and procognitive properties.

FR260010 free base is a selective 5-HT_2C receptor antagonist, with a K_i value of 1.1 nM.

DR4485 (hydrochloride) is an orally active and selective 5-HT₇ antagonist (pK_i=8.14).

S14063 is a potent 5-HT1A receptor antagonist. S14063 is devoid of β-adrenoceptor blocking properties.

Obuprazine is an orally active dopamine D3 receptor agonist and 5-HT2A receptor antagonist with IC₅₀ values of 0.37 and 4.19 nM, respectively. Obuprazine acts as a G protein-coupled receptor modulater. Obuprazine can be used for the research of schizophrenia.

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.

Hordenine sulfate (Ordenina sulfate; Peyocactine sulfate) is a multifunctional alkaloid with oral activity and blood-brain barrier penetration. Hordenine sulfate inhibits LPS-induced phosphorylation of p38, JNK, ERK1/2, p65, IκB, and AKT, prevents p65 nuclear translocation, and suppresses inflammatory cytokines and mediators. Hordenine sulfate promotes M2 macrophage polarization, restores blood-milk barrier integrity, alleviates oxidative stress by reducing ROS and MDA, and attenuates LPS-induced lung injury and pulmonary edema. Hordenine sulfate inhibits cAMP production, CREB phosphorylation, and MITF expression, thereby suppressing melanin synthesis in melanocytes and reconstructed epidermis. Hordenine sulfate activates the Wnt/β-catenin signaling pathway, promotes dermal papilla cell proliferation and hair shaft elongation, and accelerates hair regeneration. Hordenine sulfate activates DRD2, acts as a D3R partial agonist, α2A-AR full agonist, and 5-HT2A-R antagonist, and inhibits SERT and DAT. Hordenine sulfate inhibits α-synuclein accumulation and ameliorates motor deficits in Parkinson's disease models. Hordenine sulfate limits alcohol intake, reduces relapse drinking behavior, and modulates alcohol-induced conditioned place preference. Hordenine sulfate can be used for research on mastitis, skin pigmentation, acute lung injury, foodborne diseases, hair loss, Parkinson's disease, bacterial infections, and alcohol use disorder.

Benzcyclane fumarate (Bencyclane fumarate; Benzcyclan fumarate) is a vasodilator with serotonin receptor antagonism. Benzcyclane fumarate exerts atypical serotonin antagonistic effects in rabbit superior mesenteric arteries. Benzcyclane fumarate relaxes high K⁺-induced contractions in rabbit basilar arteries and superior mesenteric arteries, and selectively inhibits sympathetic nerve stimulation-induced contractions in rabbit pulmonary arteries. Benzcyclane fumarate exerts non-competitive norepinephrine antagonistic effects in rabbit superior mesenteric arteries, and slightly reduces the maximum contractile response induced by histamine. Benzcyclane fumarate relaxes smooth muscles, induces transient hypotension, inhibits thrombosis, and accelerates blood fibrinolytic activity. Benzcyclane fumarate increases cerebral glucose content/uptake, enhances hypoxia tolerance in mice, and increases cerebral blood supply in dogs. Benzcyclane fumarate is applicable to studies related to cerebral vascular circulation.

ITI-333 is a tetracyclic compound with oral bioavailability and analgesic activity, targeting multiple receptors. ITI-333 can be used for research on various forms of pain.

Elzasonan (CP-448187) is a 5-hydroxytryptamine1B receptor antagonist. Elzasonan is used in research on depression.

UH 301 hydrochloride is a 5-HT_1A receptor antagonist. UH 301 hydrochloride modulates consolidation of learning in normal and cognitively impaired rats. UH 301 hydrochloride can be used for Alzheimer’s disease and amnesia research.

TIK-301 (PD-6735) is a chlorinated melatonin derivative and a potent, high-affinity and orally active melatonin MT₁ and MT₂ receptors agonist with K_is of 0.081 nM and 0.042 nM, respectively. TIK-301 is also a 5-HT_2B/5-HT_2C receptors antagonist with antidepressant action. TIK-301 has the potential for sleep disorders and other circadian rhythm disorders treatment.

Loxapine hydrochloride is an orally active dopamine inhibitor, 5-HT receptor antagonist and also a dibenzoxazepine anti-psychotic agent.

Alverine hydrochloride citrate is a 5-HT_1A receptor antagonist, with an IC₅₀ of 101 nM.