5-HT Receptors

Cat. No.

A18261

CAS No.

17692-51-2

Metergoline

Metergoline is a psychoactive drug of the ergoline chemical class which acts as a ligand for various serotonin and dopamine receptors.

Cat. No.

A29343

CAS No.

1038988-11-2

5HT6-ligand-1

5HT6-ligand-1 is a potent ligand for the 5-HT6 receptor, exhibiting a competitive inhibition constant (Ki) of 1.43 nM. This compound is utilized in neuropharmacological research to investigate the role of the 5-HT6 receptor in various neurological conditions and psychiatric disorders. Its high affinity contributes to studies focused on neurotransmitter modulation and potential therapeutic applications.

Cat. No.

A29372

CAS No.

2836-69-3

6-Fluoro-N,N-diethyltryptamine

Synonyms: 6-F-DET

6-Fluoro-N,N-diethyltryptamine (6-F-DET) is a selective ligand for the 5-HT2A receptor. This compound exhibits high affinity and binding characteristics, making it valuable for investigating serotonergic signaling pathways. Its biological activity is essential for studies related to neuropharmacology, psychopharmacology, and the exploration of potential therapeutic agents targeting serotonin-related disorders.

Cat. No.

A29388

CAS No.

4350-07-6

D-5-Hydroxytryptophan

Synonyms: D-5-HTP; 5-Hydroxy-D-tryptophan

D-5-Hydroxytryptophan (D-5-HTP) is a D-isomer of 5-Hydroxytryptophan that primarily serves as a ligand for serotonin (5-HT) receptors. As a significant research tool, D-5-HTP binds to the 5-HT site with micromolar affinity, providing a valuable negative control in behavioral studies. Unlike its L-counterpart, D-5-HTP does not elicit any observable effects on mouse behavior, making it crucial for comparative studies in neuropharmacological research.

Cat. No.

A29393

CAS No.

1080-95-1

2-Methyl-N,N-dimethyltryptamine

Synonyms: 2,N,N-TMT; 2-Me-DMT

2-Methyl-N,N-dimethyltryptamine acts as a ligand for the serotonin (5-HT) receptors, exhibiting a pA2 value of 6.04. Its affinity for these receptors positions it as a valuable tool in the study of neuropharmacology and neurological diseases. Researchers can utilize this compound to investigate serotonin signaling pathways and their implications in various neurological conditions.

Cat. No.

A29400

CAS No.

155638-80-5

4-Bromo-2,5-DMMA

4-Bromo-2,5-DMMA is a selective ligand for the 5-HT2 receptor. It demonstrates a significant affinity for 5-HT2 binding sites, with an effective dose (ED50) of 0.82 mg/kg observed in rat discrimination tests. This compound is utilized in pharmacological research focusing on serotonergic signaling and its implications in neuropsychopharmacology.

Cat. No.

A29430

CAS No.

2974362-88-2

SEP-4199

SEP-4199 is a potent 5-HT7 receptor ligand with a Ki value of 66 nM for the human 5-HT7 receptor and 16 nM for the human D2 receptor. It has demonstrated antidepressant activity and is particularly relevant for studies focused on bipolar depression. This compound serves as a valuable research tool for exploring serotonergic and dopaminergic pathways in mood disorders.

Cat. No.

A29467

CAS No.

113777-40-5

MDL 72832 (hydrochloride)

MDL 72832 (hydrochloride) is a selective ligand for the 5-HT1a receptor, a crucial target in neuropharmacology. This compound exhibits high affinity for the receptor, making it a valuable tool for studying serotonergic signaling pathways. It is primarily utilized in research applications related to anxiety, depression, and other neuropsychiatric disorders.

Cat. No.

A29544

CAS No.

528859-61-2

E-6837

E-6837 is an orally active selective ligand for the 5-HT6 receptor, exhibiting partial agonism at the rat 5-HT6 receptor and full agonism at the constitutively active human variant, as evidenced by modulation of the cAMP signaling pathway. This compound has been shown to induce hypophagia, decrease fat mass and body weight, and enhance glycemic control. E-6837 is a valuable tool for research applications related to obesity and metabolic disorders.

Cat. No.

A29656

CAS No.

1919029-61-0

PZ-1129

PZ-1129 is a selective ligand for the 5-HT7 receptor, exhibiting a Ki of 7 nM, with moderate affinity for 5-HT1A and D2 receptors (Ki values of 159 nM and 24 nM, respectively). This compound effectively inhibits constitutive cAMP production via the Gs signaling pathway, with an EC50 of 13.7 nM. PZ-1129 is suitable for research into emotional disorders, including depression and bipolar disorder, providing a valuable tool for understanding the underlying mechanisms of these conditions.

Cat. No.

A29761

CAS No.

195627-15-7

R 116712

R 116712 is a selective ligand for the 5-HT4 receptor, demonstrating high affinity and specificity. This compound plays a key role in research applications related to neuropharmacology and gastrointestinal motility. Additionally, R 116712 can be utilized in the development of isotopic markers to further enhance studies in receptor pharmacology and signaling pathways.

Cat. No.

A29809

CAS No.

2758571-64-9

5-HT7 receptor ligand 1

5-HT7 receptor ligand 1 is a selective ligand targeting the 5-HT7 receptor, exhibiting a Ki value of 8 nM. This compound demonstrates significant biological activity and has potential applications in neuropharmacology research, particularly in exploring serotonin signaling pathways. Additionally, 5-HT7 receptor ligand 1 shows low hepatotoxicity and a moderate potential for interaction with agents metabolized by CYP3A4 or CYP2D6, making it suitable for various experimental conditions.

Cat. No.

A29811

CAS No.

1386928-34-2

LP-20 hydrochloride

LP-20 hydrochloride functions as a ligand for the 5-HT7 receptor, a subtype of the serotonin receptor family. This compound selectively modulates serotonin signaling pathways and has implications in the study of neuropsychiatric disorders and circadian rhythms. LP-20 hydrochloride can be utilized in research exploring the therapeutic potential of 5-HT7 receptor antagonism or agonism, contributing to a deeper understanding of serotonin-related mechanisms.

Cat. No.

A29816

CAS No.

851375-22-9

5-HT7/5-HT2A receptor antagonist 1

5-HT7/5-HT2A receptor antagonist 1 is a high-affinity ligand targeting both the 5-HT7 and 5-HT2A receptors, demonstrating oral bioavailability and significant brain permeability with a pKi of 8.1. This compound functions as an antagonist in in vitro assays for the 5-HT2A receptor and as an inverse agonist for the 5-HT7 receptor. In vivo studies have shown that it effectively blocks 5-Carboxamidotryptamine (5-CT)-induced hypothermia in rats and DOI-induced head-twitches in mice, while it also occupies 5-HT2A receptor binding sites in the frontal cortex. 5-HT7/5-HT2A receptor antagonist 1 is suitable for investigating neuropharmacological disorders.

Cat. No.

A29911

CAS No.

145208-86-2

5-HT1A modulator 4

5-HT1A modulator 4 is a potent ligand for the 5-HT receptors, specifically targeting the 5-HT1A subtype with a Ki value of 2.18 μM. Additionally, it demonstrates activity at the 5-HT2A receptor with a Ki value of 19.7 μM. This compound is valuable for research applications related to neuropharmacology, particularly in studying the role of serotonin receptors in mood regulation and various neurological disorders.

Cat. No.

A34140

CAS No.

1029802-21-8

Platelet aggregation-IN-3

Platelet aggregation-IN-3 is a ligand for H2 histamine receptors, α2-adrenergic receptors (α2-AR), and 5-HT2(B,C) serotonin receptors. This compound effectively inhibits platelet aggregation induced by ADP and collagen and modulates tumor cell-induced platelet aggregation (TCIPA). Platelet aggregation-IN-3 shows potential for applications in antiplatelet therapy for cardiovascular diseases and in the prevention of cancer-related thrombosis and tumor metastasis.

Cat. No.

A45887

CAS No.

76330-71-7

Altanserin

Altanserin is a selective binder for the 5-HT2 receptors, primarily utilized in neuropharmacological research. It demonstrates high affinity for these receptors, making it valuable for studying serotonergic signaling in the brain. This compound supports investigations into neuropsychiatric disorders and provides insights into receptor dynamics through imaging techniques.

Cat. No.

A45984

CAS No.

1216468-02-8

SB-258585 hydrochloride

SB-258585 hydrochloride is a high-affinity ligand for the 5-HT6 receptor. It exhibits selective binding to a single population of 5-HT6 receptors expressed in human cell lines, making it a valuable tool for studying receptor dynamics. This compound can be utilized to label both recombinant and natural 5-HT6 receptors in various research applications, facilitating investigations into neuropharmacology and related fields.

Cat. No.

A46038

CAS No.

475110-48-6

Iloperidone carboxylic acid

Synonyms: P95-12113

Iloperidone carboxylic acid is a ligand targeting the 5-HT2A receptor. This metabolite of Iloperidone demonstrates a strong affinity for the 5-HT2A receptor, with a pKi value of 8.15, while also showing moderate binding affinity to adrenergic receptors α1, α2B, and α2C. It serves as a valuable reagent for research exploring neuropharmacology and the modulation of serotonergic signaling in various biological contexts.

Cat. No.

A46090

CAS No.

5464-78-8

1-(2-Methoxyphenyl)piperazine hydrochloride

1-(2-Methoxyphenyl)piperazine hydrochloride is a ligand targeting 5-HT (serotonin) receptors, crucial for the development of various antipsychotic agents. Its high affinity for serotonin receptors makes it a valuable compound in synthesizing pharmacological agents, such as Piperazine phosphate, Piperazine citrate, and Fluphenazine dihydrochloride. Additionally, this reagent can be utilized in the synthesis of Rifampicin, contributing to studies in neuroscience and psychiatric research.

Cat. No.

A46099

CAS No.

127-77-5

Sulfabenz

Sulfabenz is an amine-substituted N1-phenylsulfonyl indole derivative that targets the human 5-HT6 serotonin receptor with a binding affinity of Ki 200 nM. This compound serves as a valuable tool for investigating the ligand binding mechanisms of the 5-HT6 receptor and exploring its implications in various neurological disorders related to this receptor. Research applications include studies focusing on serotonin-mediated pathways and neurological disease models.