1. Signalwege
  2. GPCR/G Protein
    Neuronal Signaling
  3. 5-HT Receptor

5-HT Receptor

Serotonin Receptor; 5-hydroxytryptamine Receptor

5-HT receptors (Serotonin receptors) are a group of G protein-coupled receptors (GPCRs) and ligand-gated ion channels (LGICs) found in the central and peripheral nervous systems. Type: 5-HT1, 5-HT2, 5-HT3, 5-HT4, 5-HT5, 5-HT6, 5-HT7. They mediate both excitatory and inhibitory neurotransmission. The serotonin receptors are activated by the neurotransmitter serotonin, which acts as their natural ligand. The serotonin receptors modulate the release of many neurotransmitters, as well as many hormones. The serotonin receptors influence various biological and neurological processes such as aggression, anxiety, appetite, cognition, learning, memory, mood, nausea, sleep, andthermoregulation. The serotonin receptors are the target of a variety of pharmaceutical drugs, including many antidepressants, antipsychotics, anorectics,antiemetics, gastroprokinetic agents, antimigraine agents, hallucinogens, and entactogens.

Art. -Nr. Produktname Wirkung Reinheit Chemical Structure
  • HY-135241
    25I-NBF hydrochloride
    Agonist
    25I-NBF hydrochloride is a highly potent partial agonist for the 5-HT2A receptors receptor with a Ki value of 0.26 nM and an EC50 value of 1.6 nM.
    25I-NBF hydrochloride
  • HY-123272
    E6801
    Agonist
    E6801 is a 5-HT6 receptor agonist that improves recognition memory by jointly modulating cholinergic and glutamatergic neurotransmission. E6801 can be used in studies of dementia, depression, obesity, epilepsy, etc.
    E6801
  • HY-165624B
    (R)-LY-41
    Agonist
    (R)-LY-41, R-enantiomer of LY-41 (HY-165624), is 2-Sminotetralin (HY-W022362) derivative and 8-OH-DPAT (HY-112061) analogue. (R)-LY-41 is a potent and selective 5-HT1A receptor agonist. (R)-LY-41 can reduce the accumulation of 5-hydroxytryptophan (the precursor for 5-HT synthesis) in the rat brain induced by decarboxylase inhibitors (NSD 1015). (R)-LY-41 can lower the body temperature of rats and inhibit the escape response from the cage. (R)-LY-41 can induce the 5-HT behavioral syndrome but is weaker than (S)-LY-41 (HY-165624A). (R)-LY-41 can be used for the research of neurological disease, such as depression and anxiety.
    (R)-LY-41
  • HY-156533
    5-HT2 agonist-1
    Agonist
    5-HT2 agonist-1 (Compound 24) is a 5-HT2A & 5-HT2B & 5-HT2C agonist, with IC50s of 10 nM, 8.3, and 1.6 nM respectively. 5-HT2 agonist-1 free base can be used for research of depression, alcoholism, tobacco and cocaine addiction, inflammation, cluster headache, PTSD, seizure disorders and other CNS disorders.
    5-HT2 agonist-1
  • HY-103107B
    LY334370 fumarate
    Agonist
    LY334370 fumarate is the fumarate of LY334370 (HY-103107). LY334370 is a selective 5-HT1F receptor agonist with a Ki of 1.6 nM.
    LY334370 fumarate
  • HY-117507
    U92016A hydrochloride
    Agonist 99%
    U92016A hydrochloride is a potent, metabolically stable, orally acitive 5-HT1A receptor agonist with an exceptionally high degree of intrinsic activity. U92016A hydrochloride binds with high affinity to human 5-HT1A receptors expressed in Chinese hamster ovary cells (Ki=0.2 nM).
    U92016A hydrochloride
  • HY-15401
    WAY 163909
    Agonist
    WAY 163909 is an orally active, blood-brain barrier permeable 5-HT2C receptor-selective agonist. WAY 163909 exhibits an EC50 of 8 nM and a Ki of 10.5 nM for h5-HT2C. Instead of triggering apoptosis, WAY 163909 induces anorectic, antipsychotic-like, antidepressant-like, anti-aggressive and anti-compulsive effects. WAY 163909 alleviates ketamine-induced hypothermia, but impairs sexual function at high doses. With rapid antidepressant-like properties, WAY 163909 can be used in research related to obesity, schizophrenia, depression, obsessive-compulsive disorder, and anesthesia-induced hypothermia.
    WAY 163909
  • HY-14153S
    Tegaserod-d11
    Agonist
    Tegaserod-d11 is deuterated labeled Tegaserod (HY-14153). Tegaserod is an orally active serotonin receptor 4 (HTR4; 5-HT4R) agonist and a 5-HT2B receptor antagonist. Tegaserod has pKis of 7.5, 8.4 and 7.0 for human recombinant 5-HT2A, 5-HT2B and 5-HT2C receptors, respectively. Tegaserod causes tumor cell apoptosis, blunts PI3K/Akt/mTOR signaling and decreases S6 phosphorylation. Tegaserod has anti-tumor activity and has the potential for irritable bowel syndrome (IBS) research.
    Tegaserod-d<sub>11</sub>
  • HY-100171
    PRX933 hydrochloride
    Agonist
    PRX933 hydrochloride is a 5-HT2c receptor agonist extracted from patent WO 2014140631 A1.
    PRX933 hydrochloride
  • HY-155116
    5-HT6 agonist 1
    Agonist
    5-HT6 agonist 1 (Compound 19) is a 5-HT6 agonist (Ki: 5 nM). 5-HT6 agonist 1 has antidepressant-like properties, and improves cognitive deficits. 5-HT6 agonist 1 also inhibits platelet aggregation. 5-HT6 agonist 1 has high metabolic stability.
    5-HT6 agonist 1
  • HY-169446
    ALEPH hydrochloride
    Agonist
    ALEPH (hydrochloride) is the h5-HT2A and h5-HT2B partial agonist with the EC50 values of 10.3 nM and 19.2 nM, respectively. ALEPH (hydrochloride) causes head twitch response in mice (ED50: 0.80 mg/kg).
    ALEPH hydrochloride
  • HY-121001
    Amanozine
    Agonist
    Amanozine (Compound 15) is a 5-HT3 serotonin receptor agonist. Amanozine is promising for research of nervous system disorders.
    Amanozine
  • HY-106465
    Proterguride
    Agonist
    Proterguride is a potent dopamine receptor agonist. Proterguride also shows antagonistic properties at the histamine H(1) receptor and alpha(1)-adrenoceptor and partially agonize serotonergic 5-HT2A/B receptor. Proterguride can be used for the research of neurological disease, such as Parkinson's disease .
    Proterguride
  • HY-167663A
    (S)-Ebalzotan
    Agonist
    (S)-Ebalzotan is the S-form of Ebalzotan (HY-167663). Ebalzotan is a 5-HT1A receptor agonist with activity in the study of depression. Ebalzotan can serve as a precursor to important active pharmaceutical ingredients. The synthesis of Ebalzotan involves a multi-enzyme catalyzed reduction reaction to obtain saturated primary or secondary alcohols in high yields and high enantioselectivity.
    (S)-Ebalzotan
  • HY-107847
    2-(2-Methoxyphenoxy)ethylamine hydrochloride
    Agonist 99.65%
    2-(2-Methoxyphenoxy)ethylamine hydrochloride (Compound 2b) is a mixed agonist/antagonist. 2-(2-Methoxyphenoxy)ethylamine hydrochloride is a5-HT1A receptor partial agonist and a α1-adrenergic receptor antagonist. 2-(2-Methoxyphenoxy)ethylamine hydrochloride can be used for neurological diseases research, such as anxiety, depression and psychosis.
    2-(2-Methoxyphenoxy)ethylamine hydrochloride
  • HY-169791
    ECPLA
    Agonist
    ECPLA, a lysergamide lysergic acid diethylamidean (LSD) analog, is a potent 5-HT2A agonist (EC50 of 14.6 nM) for Gq-mediated calcium flux. ECPLA has high affinity for most serotonin receptors, α2-adrenoceptors, and D2-like dopamine receptors.
    ECPLA
  • HY-124412
    Paynantheine
    Agonist
    Paynantheine is an alkaloid with antinociceptive activity, which is found in Mitragyna speciosa. Paynantheine is also a 5-HT1AR and 5-HT2BR agonist that induces lower lip retraction and antinociception in rats.
    Paynantheine
  • HY-122303
    4-hydroxy DiPT hydrochloride
    Agonist 99.9%
    4-hydroxy DiPT hydrochloride is an 5-HT2A agonist that induces the head-twitch response (HTR) in mice, indicating psychoactivity. 4-hydroxy DiPT hydrochloride significantly reduced freezing responses to conditioned cues in a dose-dependent manner with a greater potency in female mice than male mice.
    4-hydroxy DiPT hydrochloride
  • HY-101208A
    L-694247 TFA
    Agonist
    L694247 (TFA) is a selective 5-HT1D agonist with pIC50 values of 10.03, 8.64, 6.42, and 5.66 for 5-HT1D, 5-HT1A, 5-HT1C, and 5-HT1E receptors, respectively.
    L-694247 TFA
  • HY-156534
    5-HT2A&5-HT2C agonist-1
    Agonist
    5-HT2A&5-HT2C agonist-1 (Example 2) is a 5-HT2A & 5-HT2C agonist, with IC50s of 196 nM and 0.9 nM respectively. 5-HT2A&5-HT2C agonist-1 can be used for research of depression, alcoholism, tobacco and cocaine addiction, inflammation, cluster headache, PTSD, seizure disorders and other CNS disorders.
    5-HT2A&5-HT2C agonist-1
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