2. Signaling Pathways
  3. GPCR/G Protein
    Neuronal Signaling
  4. 5-HT Receptor

5-HT Receptor

Serotonin Receptor; 5-hydroxytryptamine Receptor

5-HT Receptor

Related Products

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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.

5-HT Receptor Isoform Specific Products:

5-HT Receptor Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-W743888
    AL-LAD
    		Activator
    AL-LAD (6-Allyl-6-nor-LSD) is an activator for 5-HT2A receptor with Ki of 3.4-8.1 nM. AL-LAD exhibits affinity for dopamine receptor D1 and dopamine receptor D2 with absolute affinitiesK0.5 of 189 nM and 12.3 nM. AL-LAD acts as psychoactive substance in mouse model.
    AL-LAD
  • HY-B0032S
    Lurasidone-d8 hydrochloride
    		Antagonist
    Lurasidone-d8 (hydrochloride) is the deuterium labeled Lurasidone, which is an inhibitor of Dopamine D2, 5-HT2A, 5-HT7, 5-HT1A and noradrenaline α2C.
    Lurasidone-d<sub>8</sub> hydrochloride
  • HY-19686A
    Ipsapirone hydrochloride
    		Modulator
    Ipsapirone hydrochloride (TVX Q 7821) is an anxiolytic compound and a 5-HT1A receptor partial agonist. Ipsapirone hydrochloride (TVX Q 7821) also exhibits 5-HT1A receptor antagonistic effect, and only at high doses it can also produce an inhibitory effect on 5-HT2 and the α1-adrenergic function.
    Ipsapirone hydrochloride
  • HY-101365
    RS-102221
    		Antagonist
    RS-102221 is a selective 5-HT2C receptor antagonist (Ki=10 nM). RS-102221 shows nearly 100-fold selectivity for the 5-HT2C receptor as compared to the 5-HT2A and 5-HT2B receptors. RS-102221 can promote the differentiation of new nerve cells. RS-102221 increases food-intake and weight-gain in rats.
    RS-102221
  • HY-172258
    5-HT2B antagonist-2
    		Inhibitor
    5-HT2B antagonist-2 (Compound 19c) is a 5HT2B receptor antagonist with an IC50 of 1.09 nM. 5-HT2B antagonist-2 can downregulate the expression of fibrosis-related genes α-SMA, Timp1, Col1a1, and Col3a1, and significantly reduce the deposition of fibrosis, thereby reducing the fibrotic area and inhibiting the fibrotic process in CCl4-induced liver fibrosis mouse models. 5-HT2B antagonist-2 can be used in the study of immune inflammatory-related diseases, particularly in the research of pulmonary fibrosis diseases.
    5-HT2B antagonist-2
  • HY-B0020R
    Tropisetron Hydrochloride (Standard)
    		Antagonist
    Tropisetron (Hydrochloride) (Standard) is the analytical standard of Tropisetron (Hydrochloride). Tropisetron Hydrochloride (SDZ-ICS-930) is an effective neuroprotective agent that acts as a 5-HT3 receptor antagonist, a calmodulin inhibitor, and an α7-nAChRreceptor agonist, with an IC50 of 70.1 nM for the 5-HT3 receptor. Tropisetron Hydrochloride has anti-inflammatory properties and immune-regulating functions, effectively alleviating symptoms associated with chemotherapy and post-surgery. Tropisetron Hydrochloride reduces Ab (HY-P4867)-induced hippocampal neuroinflammation.
    Tropisetron Hydrochloride (Standard)
  • HY-124135
    SB-656104
    		Antagonist
    SB-656104 is a potent antagonist of 5-HT7 receptor, with the pKi of 8.70, blocking 5-carboxamidotryptamine (5-CT) stimulated adenylyl cyclase activity.
    SB-656104
  • HY-106617A
    Etoperidone hydrochloride
    		Antagonist
    Etoperidone hydrochloride, an antidepressant agent, is an orally active serotonin and nor-adrenaline re-uptake antagonist. Etoperidone hydrochloride shows Kd values of 36 nM, 38 nM, 85 nM, and 570 nM for 5-HT2 receptor, α1-adrenergic receptor, 5-HT1A receptor, and α2-adrenergic receptor, respectively.
    Etoperidone hydrochloride
  • HY-B0901S1
    Bromperidol-d4-1
    		Inhibitor
    Bromperidol-d4-1 is deuterium labeled Bromperidol.
    Bromperidol-d<sub>4</sub>-1
  • HY-117119
    VER-3323
    		Agonist
    VER-3323 is an oral active 5-HT2C agonist and belongs to the class of indoline analogs. VER-3323 reduces food intake in rats by inducing swallowing dysfunction, with no significant impact on energy expenditure generated through thermogenesis or exercise. VER-3323 can be utilized in obesity research.
    VER-3323
  • HY-19578A
    Isamoltan hydrochloride
    		Antagonist
    Isamoltan ((±)-Isamoltane) hydrochloride is a selective antagonist of 5-HT1B receptor, with an IC50 of 39 nM for inhibits the binding of [125I]ICYP to 5-HT1B recognition sites in rat brain membranes. Isamoltan hydrochloride is also a β-adrenoceptor ligand, with an IC50 of 8.4 nM. Isamoltan hydrochloride shows anxiolytic activity.
    Isamoltan hydrochloride
  • HY-B1562C
    Bopindolol fumarate
    Bopindolol ((±)-Bopindolol) fumarate is an orally active antagonist of β-adrenoceptors (ARs) with partial agonist activity. Bopindolol fumarate is non-selective for β1- and β2-ARs and has low affinity for β3-AR subtype. Bopindolol fumarate has intrinsic sympathomimetic as well as membrane stabilizing actions, inhibits renin secretion, and interacts with 5-HT receptors. Bopindolol fumarate is a proagent of Pindolol (HY-B0982). Bopindolol fumarate can be used for essential and renovascular hypertension research.
    Bopindolol fumarate
  • HY-167675
    R-137696
    		Agonist
    R-137696 is an orally active serotonin-1A (5-HT1A) receptor agonist which relaxes the proximal stomach. R-137696 can be utilized in research related to functional dyspepsia.
    R-137696
  • HY-W011040
    LY320135
    		Modulator
    LY320135 is a potent and selective antagonist of CB1 receptor, with a Ki of 141 nM. LY320135 also binds to 5-HT2 and muscarinic receptors with Kis of 6.4 μM and 2.1 μM, respectively. LY320135 exhibits neuroprotective effect.
    LY320135
  • HY-14546A
    Aripiprazole monohydrate
    		Agonist
    Aripiprazole (OPC-14597) monohydrate, an atypical antipsychotic, is a potent and high-affinity dopamine D2 receptor partial agonist. Aripiprazole monohydrate is an inverse agonist at 5-HT2B and 5-HT2A receptors and displays partial agonist actions at 5-HT1A, 5-HT2C, D3, and D4 receptors. Aripiprazole monohydrate can be used for the research of schizophrenia and COVID19.
    Aripiprazole monohydrate
  • HY-B1473S2
    Serotonin-13C,D4
    Serotonin-13C,D4 (5-Hydroxytryptamine-13C,D4) is a 13C- and deuterated labeled Serotonin (HY-B1473A). Serotonin is a monoamine neurotransmitter in the CNS and an endogenous 5-HT receptor agonist. Serotonin is also a catechol O-methyltransferase (COMT) inhibitor with a Ki of 44 μM.
    Serotonin-<sup>13</sup>C,D<sub>4</sub>
  • HY-B1115S
    Buspirone-d8 hydrochloride
    		Agonist
    Buspirone-d8 (hydrochloride) is the deuterium labeled Buspirone hydrochloride. Buspirone hydrochloride is an anxiolytic psychotropic agent, is used to treat generalized anxiety disorder (GAD).
    Buspirone-d<sub>8</sub> hydrochloride
  • HY-118835
    Zimelidine
    		Inhibitor
    Zimelidine is a potent and selective inhibitor of serotonin 5-HT uptake and SERT. Zimelidine is an antidepressant.
    Zimelidine
  • HY-122537
    Arotinolol hydrochloride
    Arotinolol hydrochloride is a nonselective α/β-adrenergic receptor blocker and a vasodilating β-blocker. Arotinolol hydrochloride also shows potency for inhibiting the binding of the radioligand 125I-ICYP to 5HT1B-serotonergic receptor sites. Arotinolol hydrochloride is an antihypertensive agent for the treatment of a variety of cardiovascular pathologies as well as non-cardiovascular diseases.
    Arotinolol hydrochloride
  • HY-100426
    Osemozotan
    		Agonist
    Osemozotan (MKC242 free base) acts as an agonist for the 5-HT(1A) receptor.
    Osemozotan
Cat. No. Product Name / Synonyms Application Reactivity
5-HT Receptor Isoform Comparison

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