5-HT Receptors

Cat. No.

A29900

CAS No.

20776-45-8

5-Benzyloxytryptamine

Synonyms: 5-BT

5-Benzyloxytryptamine is a selective partial agonist of the 5-hydroxytryptamine 1D/1B (5-HT1D/1B) receptors, exhibiting an IC50 of 40 nM for bovine caudate 5-HT1D, with significantly lower affinity for 5-HT2 receptors (IC50 > 470 nM). This compound effectively inhibits adenylate cyclase, leading to a decrease in neurotransmitter release and downregulation of cAMP signaling. 5-Benzyloxytryptamine is valuable for the study of neurotransmitter imbalance-related disorders, particularly in research related to migraines.

Cat. No.

A29904

CAS No.

127266-56-2

Adatanserin

Synonyms: WY-50324; SEB-324

Adatanserin is a selective partial agonist of the 5-HT1A receptor, exhibiting a high affinity with a Ki value of 1 nM. Additionally, it acts as a moderate-affinity antagonist at the 5-HT2 receptor with a Ki of 73 nM. This compound demonstrates pronounced anxiolytic and antidepressant effects in preclinical animal models, making it a valuable tool for research in anxiety and mood disorders.

Cat. No.

A29926

CAS No.

171549-56-7

GR-4991W93

GR-4991W93 is an orally active partial agonist of the 5HT1B and 5HT1D receptors, showing pIC50 values of 6.95 and 7.80, respectively. This compound exhibits significant inhibition of electrically evoked plasma extravasation in guinea pig models, demonstrating its pharmacological potential in modulating neurogenic inflammation. GR-4991W93 is suitable for use in migraine research, offering insights into the mechanisms underlying this condition.

Cat. No.

A29931

CAS No.

1400811-63-3

PF-03382792

PF-03382792 is a potent partial agonist of the 5-HT4 receptor, exhibiting a Ki value of 2.7 nM and an EC50 of 0.9 nM for the 5-HT4d subtype. This compound demonstrates the ability to penetrate the blood-brain barrier and has been shown to elicit moderate increases in cortical acetylcholine levels in the rat prefrontal cortex. PF-03382792 is a valuable tool for research investigating cognitive processes and potential therapeutic strategies for neurological disorders.

Cat. No.

A29953

CAS No.

160777-43-5

(+)-OSU6162

(+)-OSU6162 is a partial agonist of the 5-HT2A receptor, acting as a stabilizer of dopaminergic and serotonergic signaling in the brain. This compound exhibits significant biological activity in modulating serotonin neurotransmission, making it a valuable tool for neurological research. Its ability to influence serotonin receptor activity positions it for use in studies related to mood disorders, cognitive function, and various neuropsychiatric conditions.

Cat. No.

A29957

CAS No.

1539266-13-1

25I-NBF hydrochloride

25I-NBF hydrochloride is a potent partial agonist of the 5-HT2A receptor, exhibiting a Ki value of 0.26 nM and an EC50 of 1.6 nM. This compound is primarily utilized in neuropharmacological research to investigate the role of 5-HT2A receptor modulation in various physiological and pathological processes. Its potency and selectivity make it a valuable tool for studying serotonergic signaling pathways and the development of related therapeutic agents.

Cat. No.

A29968

CAS No.

61638-08-2

ALEPH hydrochloride

ALEPH hydrochloride is a partial agonist of the 5-HT2A and 5-HT2B receptors, exhibiting EC50 values of 10.3 nM and 19.2 nM, respectively. This compound induces a head twitch response in mice, with an ED50 of 0.80 mg/kg. ALEPH hydrochloride is suitable for research applications investigating serotonin receptor functions and their roles in neuropharmacology.

Cat. No.

A45812

CAS No.

2855123-30-5

2-Bromo-LSD D-Tartrate

Synonyms: BOL-148 D-Tartrate; Bromolysergide D-Tartrate

2-Bromo-LSD D-Tartrate is a selective 5-HT2A receptor partial agonist and competitive antagonist. It exhibits significant biological activity, displaying an EC50 of 0.81 nM for Gq dissociation and a KB of 0.18 nM, making it a valuable tool for studying serotonergic signaling pathways. Additionally, it promotes dendritogenesis and spinogenesis while effectively reversing the behavioral impacts of chronic stress in animal models, enhancing active coping behaviors. This compound is suitable for research involving neurological and behavioral studies related to serotonin modulation.

Cat. No.

A45836

CAS No.

168986-60-5

RS 67333 hydrochloride

RS 67333 hydrochloride is a selective partial agonist of the 5-HT4 receptor, demonstrating a pKi of 8.7 in guinea pig striatum. This compound exhibits lower affinities for various other receptors, including 5-HT1A, 5-HT1D, 5-HT2A, 5-HT2C, dopamine D1, D2, and muscarinic M1-M3 receptors. RS 67333 hydrochloride is known for its neuroprotective properties, making it a valuable tool for research in Alzheimer's disease and related neurodegenerative disorders.

Cat. No.

A45975

CAS No.

851220-85-4

Aripiprazole monohydrate

Synonyms: OPC-14597 monohydrate

Aripiprazole monohydrate is a potent partial agonist of the dopamine D2 receptor and an inverse agonist at the 5-HT2B and 5-HT2A receptors. Additionally, it exhibits partial agonist functionality at 5-HT1A, 5-HT2C, D3, and D4 receptors. This compound is primarily utilized in research focused on schizophrenia and has also been explored for potential applications in treating COVID-19.

Cat. No.

A46018

CAS No.

1428862-32-1

Usmarapride free base

Synonyms: SUVN-D4010 free base

Usmarapride free base is a selective partial agonist of the 5-HT4 receptor, exhibiting a potent activity with an EC50 of 44 nM. This compound is orally active and can penetrate the blood-brain barrier, making it suitable for investigations into cognitive deficits related to Alzheimer's disease. Its mechanism of action supports research aimed at understanding and potentially mitigating Alzheimer's-associated cognitive impairments.

Cat. No.

A46037

CAS No.

2048491-06-9

FPT

FPT is a 2-aminotetralin that acts primarily as a partial agonist at the 5-HT1A receptor, and as a full agonist at both 5-HT1B and 5-HT1D receptors, exhibiting EC50 values of 39.3 nM, 1.2 nM, and 0.5 nM, respectively. Additionally, FPT displays weak agonistic activity at the 5-HT7 receptor. This compound demonstrates in vivo efficacy as an antiepileptic agent in Fmr1 knockout mice and produces anxiolytic-like and prosocial behaviors in various mouse models, making it a valuable tool for researching serotonergic modulation and its implications in neurological disorders.

Cat. No.

A46073

CAS No.

519148-48-2

CJ033466

CJ033466 is a selective partial agonist of the 5-HT4 receptor, exhibiting an EC50 of 9 nM. This compound demonstrates significant gastroprokinetic effects, making it a valuable tool for research applications related to gastrointestinal motility and related disorders. Its specificity towards the 5-HT4 receptor aids in elucidating receptor-mediated pathways and potential therapeutic interventions.

Cat. No.

A46104

CAS No.

99095-10-0

Tandospirone hydrochloride

Synonyms: SM-3997 hydrochloride

Tandospirone hydrochloride is a selective partial agonist of the 5-HT1A receptor, exhibiting a Ki value of 27 nM. This compound displays notable anxiolytic and antidepressant properties, making it valuable in the study of central nervous system disorders. Its unique action at the 5-HT1A receptor contributes to the understanding of underlying mechanisms related to anxiety and depression, facilitating research aimed at developing novel therapeutic approaches.