5-HT Receptor

Adenosine receptor A1 antagonist 5 acts as an adenosine antagonist, is an oxypurine, acts as an insecticide and pest control agent, and has an inhibitory effect on elevated blood pressure.

RXFP1 receptor agonist-5 (Example 98) is an agonist that targets the RXFP1 receptor and demonstrates its bioactivity by inhibiting cAMP production in HEK293 cells with stable human RXFP1 expression, exhibiting an EC50 of 1.3 nM [1].

Thrombin Receptor Activator for Peptide 5 (TRAP-5), also known as Coagulation Factor II Receptor (1-5) or Proteinase Activated Receptor 1 (1-5), is employed in coronary heart disease (CHD) research.

2-Methyl-5-HT (2-Methyl-5-hydroxytryptamine) is a potent and selective 5-HT3 receptor agonist with anti-depressive-like effects.

5-HT2A receptor agonist-2 is a potent compound that acts as an agonist on the serotonin 5-HT2 receptor. It specifically stimulates the 5-HT 2A, 5-HT 2B, and 5-HT 2C receptors, with EC 50 values of 1.7 nM, 0.58 nM, and 0.50 nM, respectively [1].

2-Methyl-5-HT maleate (2-Methyl-5-hydroxytryptamine maleate) is a potent and selective 5-HT3 receptor agonist, which is shown to display anti-depressive-like effects[1].

2-Methyl-5-HT hydrochloride (2-Methyl-5-hydroxytryptamine) is a potent and selective 5-HT3 receptor agonist with anti-depressive-like effects.

GABAA Receptor Agent 5 (compound 018) serves as a potent γ-GABAAR antagonist, possessing a Ki of 0.020 μM. This compound exhibits γ-GABAAR antagonist properties, yet it demonstrates low cellular membrane permeability [1].

5-HT6/5-HT2A receptor ligand-1 (compound 33) is a dual antagonist for the 5-HT6 and 5-HT2A receptors. It exhibits a K i value of 2 nM and 11 nM for the respective receptors. This compound holds promise for research in neurological and psychiatric disorders [1].

5-HT2A receptor agonist-3 represents the highest selectivity for the human 5-HT2A receptor currently identified, exhibiting a K i of 2.5 nM. It also demonstrates a remarkable 124-fold selectivity over its structurally analogous 5-HT2C receptor [1].

Compound 42, a 5-HT6/5-HT2A receptor ligand-2, serves as a dual antagonist for the 5-HT6 and 5-HT2A receptors with Ki values of 25 nM and 32 nM, respectively. This brain-penetrant compound exhibits pro-cognitive properties [1].

5-HT7 receptor ligand 1 (Compound 5c) is a potent ligand for the 5-HT7 receptor, with a K i value of 8 nM. The compound demonstrates non-hepatotoxic properties and displays moderate potential for drug-drug interactions with substrates of CYP3A4 or CYP2D6 enzymes [1].

Estrogen receptor antagonist 5 is a potent antagonist of the Estrogen receptor. Estrogen receptor (Estrogen receptor) is a ligand-activated transcriptional regulatory protein that interacts with endogenous estrogens and mediates the induction of a variety of biological effects. estrogen receptor antagonist 5 has potential for metastatic disease studies.

Sigma-1 receptor antagonist 5 (compound 12), a 4-pyridylpiperidine derivative, exhibits analgesic properties through its antagonistic action on sigma receptors (Ki=4.5 nM (σ1R), 10 nM (σ2R)) and the histamine H3 receptor (hH3R, Ki=7.7 nM, IC50=215 nM). It effectively attenuates Capsaicin-induced nociception and demonstrates significant antinociceptive effects in both nociceptive and neuropathic pain models [1].

Androgen receptor-IN-5 is a potent inhibitor of the androgen receptor with anticancer properties. It additionally suppresses the synthesis of IL-17A, IL-17F, and INF-γ.

AMPA Receptor Modulator-5 (Example 217) serves as an AMPA receptor modulator, utilized in neurological disease research [1].

APJ receptor agonist 5 (compound 3) is a potent and orally active apelin receptor (APJ) agonist (EC 50:0.4 nM). APJ receptor agonist 5 has excellent pharmacokinetic profiles in rodent models of heart failure (HF) and an acceptable safety profile in preclinical toxicology studies. APJ receptor agonist 5 can improve cardiac function and can be used in the study of HF disease.

Androgen receptor antagonist 5 is a potent antagonist of the androgen receptor (AR) (IC50: 6.17 μM). Androgen receptor antagonist 5 inhibited the proliferation of prostate cancer cells LNCaP and showed antitumor effect in LNCaP xenograft mice model, which can be used to study prostate cancer.

Glucagon receptor antagonists-5 is an orally bioavailable indazole-based glucagon receptor antagonist (Ki: 32 nM). It has potential for the treatment of type 2 diabetes mellitus (T2DM).

NMDA receptor antagonist 5 (Compound 10e), a potent and non-toxic NMDA receptor antagonist, exhibits brain permeability. It is of significance in studying neurological disorders [1].

NMDA receptor modulator 5 (Compound 195), a potent NMDA receptor modulator, exhibits potential for neurological disorder research [1].

Mu opioid receptor antagonist 5 (compound NAP) is a selective mu opioid receptor (MOR) antagonist that crosses the blood-brain barrier (EC50: 1.14 nM, Ki: 0.37 nM). Mu opioid receptor antagonist 5 can be used to study opioid use disorder (OUD).

Ritanserin (R 55667) is a highly effective, relatively selective, long-acting antagonist of 5-HT2 receptor (IC50: 0.9 nM), less active on Histamine H1, Dopamine D2, Adrenergic α1, Adrenergic α2 receptors.

Pimavanserin tartrate (Nuplazid) is an effective and specific serotonin 5-HT2A inverse agonist (pIC50: 8.73), used in the therapy of psychosis associated with Parkinson's disease.

Ziprasidone hydrochloride monohydrate (CP 88059) is a united 5-HT (serotonin) and dopamine receptor antagonist which shows potent effects of the antipsychotic activity.

Aripiprazole (OPC-14597) is an antipsychotic agent that is structurally related to piperazines and quinolones. It is a partial agonist of SEROTONIN RECEPTOR, 5-HT1A and DOPAMINE D2 RECEPTORS, where it also functions as a post-synaptic antagonist, and an antagonist of SEROTONIN RECEPTOR, 5-HT2A.

LY 272015 hydrochloride is an orally active and selective 5-HT2B receptor antagonist that displays antihypertensive effects in DOCA-salt hypertensive rats.LY 272015 hydrochloride inhibits 5-HT- or BW723C86-induced ERK2 phosphorylation and attenuates MVIC and Tissue downstream cellular effects of 5HT signaling and can be used to study hepatocellular carcinoma.

Trazodone hydrochloride (Trazodone HCl) is a serotonin uptake inhibitor that is used as an antidepressive agent. It has been shown to be effective in patients with major depressive disorders and other subsets of depressive disorders. It is generally more useful in depressive disorders associated with insomnia and anxiety.

Vilazodone (SB659746A) is a selective serotonin (5-HT) reuptake inhibitor (SSRI) and a 5-HT-1A receptor partial agonist, with antidepressant and anti-anxiety activities. Vilazodone inhibits the reuptake of serotonin from the synaptic cleft while stimulating the release of 5-HT into the synaptic cleft. This increases the concentration of 5-HT in the synaptic cleft and potentiates serotonergic neurotransmission in the central nervous system.

Cannabigerol is a high affinity α±2-adrenergic receptor agonist, moderate affinity 5-HT1A receptor antagonist, and low affinity CB1 receptor antagonist ; also binds to the CB2 receptor; it can relieve interocular pressure, which may be of benefit in the treatment of glaucoma.

dopamine D1 receptor antagonist

Perphenazine (Trilafon) is a phenothiazine derivative and a dopamine antagonist with antiemetic and antipsychotic properties.

Pimethixene (Calmixen) is a highly potent 5-HT1A, 5-HT2A, 5-HT2B, 5-HT2C, histamine H1, dopamine D2 and D4.4 as well as muscarinic M1 and M2 receptors antagonist(pKis of 7.63, 10.22, 10.44, 8.42, 10.14, 8.19, 7.54, 8.61 and 9.38, respectively).

SLV-310 is a potent dopamine D2 receptor antagonist and 5-HT reuptake receptor inhibitor used in the study of neurological disorders such as bipolar disorder and schizophrenia.

(+)-OSU 6162 (Piperidine, 3-[3-(methylsulfonyl)phenyl]-1-propyl-, (3R)-) is an agonist of 5-HT Receptor with anti-Alzheimer and antidepressant activities.

5-Methyltryptamine hydrochloride is a high-affinity 5-HT1C receptor ligand and a partial agonist of 5-HT. 5-Methyltryptamine hydrochloride protects mice subjected to burn, tourniquet and endotoxin shock.

Litoxetine is a selective 5-HT uptake inhibitor and is a 5-HT3 receptor antagonist. Litoxetine acts as an antidepressant and has shown antiemetic properties in ferrets. Litoxetine (1 and 10 mg/kg i.v.) dose-dependently reduced the number of regurgitations and vomiting and delayed the onset of vomiting. Litoxetine has an affinity for brain 5HT3 receptors (Ki = 85 nM).

Brexpiprazole HCl (OPC 34712 dihydrochloride) is a new antipsychotic drug.

Nexopamil (LU-49938) is a calcium channel antagonist and a 5-hydroxytryptamine 2A receptor antagonist. Nexopamil inhibits 5-HT-induced contraction and proliferation of mesenchymal cells.

Naratriptan is a selective agonist of 5-HT1 receptor and is is used for the treatment of migraine headaches.

Adatanserin hydrochloride (WY50324 hydrochloride) is a novel 5-HT(1A)/5-HT(2) receptor ligand with potential neuroprotective effects and inhibition of ischemic efflux of endogenous amino acids, which can be used in the study of depression and anxiety disorders.

Ecopipam (UNII-0X748O646K) is a potent, selective and orally active antagonist of dopamine D1 D5 receptor, with Kis of 1.2 nM and 2.0 nM, respectively. Ecopipam shows more than 40-flod selectivity over D2, D4, 5-HT, and α2a receptor (Ki=0.98, 5.52, 0.08, and 0.73 μM, respectively). Ecopipam can be used for the research of schizophrenia and obesity.

Eplivanserin (SR-46349) is an effective and selective antagonist of 5-HT2A receptor with a Kd of 1.14 nM and an IC50 value of 5.8 nM in rat cortical membrane.

C-Type Natriuretic Peptide (CNP) (1-22), human acetate is an agonist of natriuretic peptide receptor B (NPR-B), an endothelial-derived relaxant and growth inhibitory factor. C-Type Natriuretic Peptide (CNP) (1-22), human acetate inhibits cAMP synthesis stimulated by histamine and 5-HT or directly by Forskolin.

Lecozotan HCl (SRA-333) is a potent and selective 5-HT antagonist that significantly enhances KCl-stimulated glutamate and acetylcholine release from the hippocampal dentate gyrus and has cognitive enhancing properties. Chronic administration of Lecozotan HCl did not induce 5-HT(1A) receptor tolerance or desensitization in a behavioral model demonstrating 5-HT(1A) receptor function.

Alaproclate is a non-competitive NMDA receptor antagonist and a new selective 5-HT uptake inhibitor for the study of depression and dementia.

Osemozotan Free Base is a 5-HT(1A) receptor agonist.

SB-269970 hydrochloride (SB-269970A) , a hydrochloride salt form of SB-269970, is a 5-HT7 receptor antagonist (pKi of 8.3) and exhibits >50-fold selectivity against other receptors.

Donitriptan is a 5-HT receptor agonist with pKis of 9.4 and 9.3 for 5-HT1B and 5-HT1D, respectively.

cis-Urocanic acid ((E)-Urocanic acid) is a 5-HT2A receptor agonist (Kd: 4.6 nM). It is an immune modulator that induces immunosuppression by binding to the 5-HT2A receptor.