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5-HT Receptor Antagonist

" in MedChemExpress (MCE) Product Catalog:

758

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2

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1

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21

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93

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-B0002B
    Ondansetron
    5+ Cited Publications

    GR 38032; SN 307

    5-HT Receptor Neurological Disease
    Ondansetron (GR 38032; SN 307) is a highly selective 5-HT3 receptor antagonist with an IC50 value of 103 pM. Ondansetron exerts its antiemetic effect by antagonizing 5-HT receptors located in localized neurons in the peripheral and central nervous systems. Ondansetron can inhibit nausea and vomiting induced by chemotherapy and radiotherapy .
    Ondansetron
  • HY-14544
    Quetiapine
    3 Publications Verification

    ICI204636

    5-HT Receptor Dopamine Receptor Neurological Disease
    Quetiapine (ICI204636) is a 5-HT receptors agonist with a pEC50 of 4.77 for human 5-HT1A receptor. Quetiapine is a dopamine receptor antagonist with a pIC50 of 6.33 for human D2 receptor. Quetiapine has moderate to high affinity for the human D2, HT1A, 5-HT2A, 5-HT2C receptor with pKis of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects .
    Quetiapine
  • HY-B0982
    Pindolol
    2 Publications Verification

    LB-46

    5-HT Receptor Adrenergic Receptor Neurological Disease
    Pindolol (LB-46) is the antagonist for 5-HT 1A (Ki=33 nM) and 5-HT 1B. Pindolol is the antagonist for β1/β2-adrenergic receptor. Pindolol exhibits anti-anxiety and antidepressant effects .
    Pindolol
  • HY-15370A
    SB-269970 hydrochloride
    5+ Cited Publications

    SB-269970A

    5-HT Receptor Neurological Disease
    SB-269970 hydrochloride is a potent, selective and brain-penetrant 5-HT7 receptor antagonist with a pKi of 8.3. SB-269970 hydrochloride exhibits >50-fold selectivity against other 5-HT receptors .
    SB-269970 hydrochloride
  • HY-B1033
    Metergoline
    2 Publications Verification

    5-HT Receptor Dopamine Receptor Sodium Channel Neurological Disease
    Metergoline is a serotonin (5-HT) receptor and dopamine receptors antagonist, with pKis of 8.64, 8.75 and 8.75 for 5-HT2A, 5-HT2B and 5-HT2C, respectively. Metergoline is a high-affinity ligand for the h5-HT7 receptor, with a Ki of 16 nM. Metergoline is also a reversible neural Na + channels inhibitor. Metergoline is commonly used for the research of seasonal affective disorder, prolactin hormone regulation .
    Metergoline
  • HY-14542
    Ziprasidone
    3 Publications Verification

    CP-88059

    5-HT Receptor Dopamine Receptor Neurological Disease
    Ziprasidone (CP-88059), an orally active antipsychotic agent, is a combined 5-HT and dopamine receptor antagonist . Ziprasidone mesylate trihydrate has affinities for Rat D2 (Ki=4.8 nM), 5-HT2A (Ki=0.42 nM) and 5-HT1A (Ki=3.4 nM) .
    Ziprasidone
  • HY-B0002
    Ondansetron hydrochloride
    5+ Cited Publications

    GR 38032 hydrochloride; SN 307 hydrochloride

    5-HT Receptor Neurological Disease
    Ondansetron (GR 38032; SN 307) hydrochloride is a highly selective 5-HT3 receptor antagonist with an IC50 value of 103 pM. Ondansetron hydrochloride exerts its antiemetic effect by antagonizing 5-HT receptors located in localized neurons in the peripheral and central nervous systems. Ondansetron hydrochloride can inhibit nausea and vomiting induced by chemotherapy and radiotherapy .
    Ondansetron hydrochloride
  • HY-17407
    Ziprasidone hydrochloride monohydrate
    3 Publications Verification

    CP 88059 hydrochloride monohydrate

    5-HT Receptor Dopamine Receptor Neurological Disease
    Ziprasidone (CP-88059) hydrochloride monohydrate is an orally active combined 5-HT and dopamine receptor antagonist . Ziprasidone hydrochloride monohydrate has affinities for Rat D2 (Ki=4.8 nM), 5-HT2A (Ki=0.42 nM) and 5-HT1A (Ki=3.4 nM) .
    Ziprasidone hydrochloride monohydrate
  • HY-B0031
    Quetiapine hemifumarate
    3 Publications Verification

    5-HT Receptor Dopamine Receptor Neurological Disease
    Quetiapine hemifumarate is a 5-HT receptors agonist with a pEC50 of 4.77 for human 5-HT1A receptor. Quetiapine hemifumarate is a dopamine receptor antagonist with a pIC50 of 6.33 for human D2 receptor. Quetiapine hemifumarate has moderate to high affinity for the human D2, HT1A, 5-HT2A, 5-HT2C receptor with pKis of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects .
    Quetiapine hemifumarate
  • HY-B0002A

    GR 38032 hydrochloride dihydrate; SN 307 hydrochloride dihydrate

    5-HT Receptor Neurological Disease
    Ondansetron (GR 38032; SN 307) hydrochloride dehydrate is a highly selective 5-HT3 receptor antagonist with an IC50 value of 103 pM. Ondansetron hydrochloride dehydrate exerts its antiemetic effect by antagonizing 5-HT receptors located in localized neurons in the peripheral and central nervous systems. Ondansetron hydrochloride dehydrate can inhibit nausea and vomiting induced by chemotherapy and radiotherapy .
    Ondansetron hydrochloride dihydrate
  • HY-B1154
    Penbutolol sulfate
    1 Publications Verification

    (-)-Terbuclomine

    Adrenergic Receptor 5-HT Receptor Neurological Disease
    Penbutolol sulfate ((-)-Terbuclomine) is a potent β-adrenoceptor and 5-HT receptor antagonist with Ki of 11.6 nM and 11.9 nM for 5-HT in rat cornu ammonis 1 (CA1) and human CA3 .
    Penbutolol sulfate
  • HY-14542A
    Ziprasidone hydrochloride
    3 Publications Verification

    CP-88059 hydrochloride

    5-HT Receptor Dopamine Receptor Neurological Disease
    Ziprasidone (CP-88059) hydrochloride is an orally active combined 5-HT and dopamine receptor antagonist . Ziprasidone hydrochloride has affinities for Rat D2 (Ki=4.8 nM), 5-HT2A (Ki=0.42 nM) and 5-HT1A (Ki=3.4 nM) .
    Ziprasidone hydrochloride
  • HY-17390A
    Loxapine succinate
    1 Publications Verification

    5-HT Receptor Dopamine Receptor Infection Neurological Disease
    Loxapine succinate is an orally active dopamine inhibitor, 5-HT receptor antagonist and also a dibenzoxazepine anti-psychotic agent. Loxapine can also suppresses bacterial efflux pump activity and inhibit intracellular multiple-antibiotic-resistant Salmonella enterica serovar Typhimurium in macrophages .
    Loxapine succinate
  • HY-17390
    Loxapine
    1 Publications Verification

    5-HT Receptor Dopamine Receptor Bacterial Neurological Disease
    Loxapine is an orally active dopamine inhibitor, 5-HT receptor antagonist and also a dibenzoxazepine anti-psychotic agent .
    Loxapine
  • HY-100562

    5-HT Receptor COMT Neurological Disease
    Flopropione is a 5-HT receptor antagonist and also a catechol-o-methyltransferase (COMT) inhibitor . Flopropione also as an antispasmodic agent .
    Flopropione
  • HY-15370
    SB-269970
    5+ Cited Publications

    5-HT Receptor Neurological Disease
    SB-269970 is a potent, selective and brain-penetrant 5-HT7 receptor antagonist with a pKi of 8.3. SB-269970 exhibits >50-fold selectivity against other 5-HT receptors .
    SB-269970
  • HY-109112

    RP5063

    Dopamine Receptor 5-HT Receptor Neurological Disease Inflammation/Immunology
    Brilaroxazine (RP5603) is a potent and orally active multimodal dopamine (DA)/serotonin (5-HT) modulator. Brilaroxazine is a partial agonist of dopamine (DA) D2, D3, and D4 receptors, 5-HT1A (Ki=1.5 nM) and 5-HT2A (Ki=2.5 nM), and has antagonist activity at 5-HT2B (Ki=0.19 nM), and 5-HT7 (Ki=2.7 nM) receptors . Brilaroxazine is an atypical antipsychotic agent, and has the potential to improve cognitive impairments in neuropsychiatric and neurological diseases in vivo .
    Brilaroxazine
  • HY-19818A

    5-HT Receptor Neurological Disease
    NAN-190 hydrobromide is a serotonin receptor 5-HT antagonist. NAN-190 is a selective antagonist of 5-HT1A .
    NAN-190 hydrobromide
  • HY-15574
    Piboserod
    4 Publications Verification

    SB-207266

    5-HT Receptor Cardiovascular Disease
    Piboserod is an orally available selective antagonist of the 5-HT4 receptor, with a Ki value of approximately 0.1 nM for human 5-HT4 receptors. Piboserod can competitively bind to the 5-HT4 receptor and block the activation of the 5-HT4 receptor. Piboserod can inhibit the enhancing effect of 5-HT on the nerve-mediated contraction response of the human bladder detrusor muscle. Piboserod is mainly used in the research of urinary system diseases (such as overactive bladder) and cardiovascular diseases (such as chronic heart failure) .
    Piboserod
  • HY-G0014A
    Quetiapine sulfoxide dihydrochloride
    1 Publications Verification

    Quetiapine S-oxide dihydrochloride

    Drug Metabolite Neurological Disease
    Quetiapine sulfoxide dihydrochloride (Quetiapine S-oxide dihydrochloride) is a main metabolite of Quetiapinem. Quetiapine is a second-generation antipsychotic . Quetiapine is a 5-HT receptors agonist and a dopamine receptor antagonist .
    Quetiapine sulfoxide dihydrochloride
  • HY-103156
    NAS-181 dimesylate
    3 Publications Verification

    5-HT Receptor Neurological Disease
    NAS181 is a potent and selective antagonist of rat 5-HT1B receptor, with a Ki of 47 nM. NAS181 shows 13-fold selectivity for r5-HT1B over bovine 5-HT1B receptor (Ki=630 nM). NAS181 increases the 5-HT turnover and the synaptic concentration of 5-HT by inhibiting terminal r5-HT1B autoreceptors .
    NAS-181 dimesylate
  • HY-131255

    Ziprasidone Impurity C; Ziprasidone open ring impurity

    5-HT Receptor Dopamine Receptor Neurological Disease
    Ziprasidone amino acid (Ziprasidone Impurity C) is an impurity of Ziprasidone. Ziprasidone is a combined 5-HT (serotonin) and dopamine receptor antagonist. Ziprasidone exhibits potent effects of antipsychotic activity .
    Ziprasidone amino acid
  • HY-116790
    (-)-Penbutolol
    1 Publications Verification

    (S)-Penbutolol; (-)-Isopenbutolol

    Adrenergic Receptor 5-HT Receptor Neurological Disease
    (-)-Penbutolol ((S)-Penbutolol) is a potent β-adrenoceptor and 5-HT receptor antagonist with Ki values of 11.6 nM and 11.9 nM for 5-HT in rat cornu ammonis 1 (CA1) and human CA3 .
    (-)-Penbutolol
  • HY-100851A

    5-HT Receptor Cardiovascular Disease
    LY-272015 hydrochloride is an orally active, specific 5-HT2B receptor antagonist. LY-272015 hydrochloride completely inhibits the phosphorylation of ERK2 induced by 5-HT or BW723C86. LY-272015 hydrochloride is antihypertensive in Deoxycorticosterone Acetate (DOCA)-salt-hypertensive rats .
    LY-272015 hydrochloride
  • HY-14544R

    ICI204636 (Standard)

    Reference Standards 5-HT Receptor Dopamine Receptor Neurological Disease
    Quetiapine (Standard) is the analytical standard of Quetiapine. This product is intended for research and analytical applications. Quetiapine (ICI204636) is a 5-HT receptors agonist with a pEC50 of 4.77 for human 5-HT1A receptor. Quetiapine is a dopamine receptor antagonist with a pIC50 of 6.33 for human D2 receptor. Quetiapine has moderate to high affinity for the human D2, HT1A, 5-HT2A, 5-HT2C receptor with pKis of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects .
    Quetiapine (Standard)
  • HY-101222

    5-HT Receptor Cardiovascular Disease Neurological Disease
    SB-203186 hydrochloride is a potent, selective and competitive 5-HT4 antagonist. SB-203186 hydrochloride antagonizes the 5-HT4 receptor-mediated relaxations of the carbachol-contracted rat isolated oesophagus against 5-HT with pKB values of 10.9 (rat oesophagus), 9.5 (guinea-pig ileum), and 9.0 (human colon) respectively .
    SB-203186 hydrochloride
  • HY-B0031R

    Reference Standards 5-HT Receptor Dopamine Receptor Neurological Disease
    Quetiapine (hemifumarate) (Standard) is the analytical standard of Quetiapine (hemifumarate). This product is intended for research and analytical applications. Quetiapine hemifumarate is a 5-HT receptors agonist with a pEC50 of 4.77 for human 5-HT1A receptor. Quetiapine hemifumarate is a dopamine receptor antagonist with a pIC50 of 6.33 for human D2 receptor. Quetiapine hemifumarate has moderate to high affinity for the human D2, HT1A, 5-HT2A, 5-HT2C receptor with pKis of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects .
    Quetiapine hemifumarate (Standard)
  • HY-B0031S1

    5-HT Receptor Dopamine Receptor Neurological Disease
    Quetiapine-d4 (hemifumarate) is the deuterium labeled Quetiapine hemifumarate. Quetiapine hemifumarate is a 5-HT receptors agonist and a dopamine receptor antagonist. Antidepressant and anxiolytic effects .
    Quetiapine-d4 hemifumarate
  • HY-B0982R

    LB-46 (Standard)

    Reference Standards 5-HT Receptor Adrenergic Receptor Neurological Disease
    Pindolol (Standard) is the analytical standard of Pindolol. This product is intended for research and analytical applications. Pindolol (LB-46) is the antagonist for 5-HT 1A (Ki=33 nM) and 5-HT 1B. Pindolol is the antagonist for β1/β2-adrenergic receptor. Pindolol exhibits anti-anxiety and antidepressant effects .
    Pindolol (Standard)
  • HY-W016194

    1-Carboxycyclohexaneacetic acid; Gabapentin Impurity E; Gabapentin Related Compound E

    5-HT Receptor Neurological Disease
    1-(Carboxymethyl)cyclohexanecarboxylic acid (1-Carboxycyclohexaneacetic acid; Gabapentin Impurity E) is a potential impurity in commercial preparations of the antiepileptic agent Gabapentin (HY-A0057). It is also used as a precursor for the synthesis of a serotonin (5-HT) receptor subtype 5-HT2A antagonist.
    1-(Carboxymethyl)cyclohexanecarboxylic acid
  • HY-101480

    5-HT Receptor Neurological Disease
    Xylamidine is a peripheral 5-HT receptor antagonist used to investigate possible peripheral appetite suppressant effects of 5-hydroxytryptophan (5-HTP) and fenfluramine. In a 1-hour food intake test, xylamidine attenuated the decrease in food intake induced by 5-HT and 5-HTP, but had no effect on fenfluramine, suggesting that the appetite suppressant effect of 5-HTP is mediated in part through peripheral 5-HT receptors. Microstructural analysis revealed that 5-HTP and fenfluramine induced a decrease in food intake rate and a reduction in feeding batch size. Xylamidine reversed the effects of 5-HTP on food intake rate and induced a slight increase in feeding batch size itself, thus, the peripheral effect of 5-HTP appears to be to slow food intake rate. No effect of xylamidine on fenfluramine-induced changes in feeding was observed. The results suggest that the appetite suppressant effects of 5-HTP and fenfluramine are differentiated based on the peripheral effects of 5-HTP. The peripheral effects of 5-HTP are distinct from the previously reported 5-HT-induced decreases in feeding batch size and duration. Possible mechanisms underlying the differences in peripheral effects of 5-HT and 5-HTP are discussed.
    Xylamidine
  • HY-B0002BS

    GR 38032-d5; SN 307-d5

    5-HT Receptor Isotope-Labeled Compounds Neurological Disease
    Ondansetron-d5 is the deuterium labeled Ondansetron (HY-B0002B). Ondansetron (GR 38032; SN 307) is a highly selective 5-HT3 receptor antagonist with an IC50 value of 103 pM. Ondansetron exerts its antiemetic effect by antagonizing 5-HT receptors located in localized neurons in the peripheral and central nervous systems. Ondansetron can inhibit nausea and vomiting induced by chemotherapy and radiotherapy .
    Ondansetron-d5
  • HY-169127

    5-HT Receptor Neurological Disease
    Seganserin is an orally active 5-HT receptor antagonist with a plasma half-life of 26.1 ± 12.9 (S.D.) h. Seganserin can be utilized in neurological research .
    Seganserin
  • HY-118557

    S-MPEC

    5-HT Receptor Inflammation/Immunology
    Iferanserin (S-MPEC) is a selective 5-HT receptor (serotonin receptor) antagonist with an affinity for 5-HT2A receptor. Iferanserin has the potential for internal hemorrhoid disease treatment .
    Iferanserin
  • HY-B0031S

    5-HT Receptor Dopamine Receptor Neurological Disease
    Quetiapine-d4 (fumarate) is the deuterium labeled Quetiapine fumarate. Quetiapine fumarate is a 5-HT receptors agonist and a dopamine receptor antagonist. Antidepressant and anxiolytic effects .
    Quetiapine-d4 fumarate
  • HY-100648

    5-HT Receptor Dopamine Receptor Neurological Disease
    Keto Ziprasidone is an impurity of Ziprasidone . Ziprasidone, an antipsychotic agent, is a combined 5-HT (serotonin) and dopamine receptor antagonist .
    Keto Ziprasidone
  • HY-156807

    Serotonin Transporter 5-HT Receptor Neurological Disease
    LY 367265 is a 5-hydroxytryptamine transporter (SERT) inhibitor (IC₅₀ = 3.1 nM) and a 5-HT₂A receptor antagonist (Kᵢ = 0.81 nM). LY 367265 has the inhibitory activity on the norepinephrine transporter (NET) of extremely weak (IC₅₀ > 1000 nM); it has low affinity for subtypes such as 5-HT₁B (Kᵢ = 490 nM) and 5-HT₁D (Kᵢ = 81 nM), showing high selectivity. LY 367265 concentration-dependently enhances of [³H]5-HT efflux (EC₅₀ = 250 nM). LY 367265 antagonizes the contraction response of Sumatriptan (HY-B0121B), indicating its functional antagonistic activity on 5-HT₁D-like receptors. LY 367265 can be used for the study of diseases such as anxiety disorders and post-traumatic stress disorder .
    LY 367265
  • HY-B1213A

    5-HT Receptor Bacterial Neurological Disease
    Trimipramine is a 5-HT receptor antagonist, with pKi binding values of 6.39, 8.10, 4.66 for 5-HT1C, 5-HT2 and 5-HT1A, respectively. Trimipramine is also a potent and selective inhibitor targeting human noradrenaline (hNAT), serotonin (hSERT) and organic cation transporters (hOCT1, hOCT2) with IC50 values of 4.99 μM, 2.11 μM, 3.72 μM, 8.00 μM, respectively. Trimipramine has vascular activity and anxiolytic efficacy .
    Trimipramine
  • HY-17390B

    Dopamine Receptor 5-HT Receptor Neurological Disease
    Loxapine hydrochloride is an orally active dopamine inhibitor, 5-HT receptor antagonist and also a dibenzoxazepine anti-psychotic agent .
    Loxapine hydrochloride
  • HY-103089

    5-HT Receptor Neurological Disease
    LY393558 is a potent and orally active inhibitor of the 5-HT transporter and an antagonist of 5-HT1B and 5-HT1D receptors. LY393558 increase the extracellular levels of 5-HT in mice model frontal cortex. LY393558 can be used for researching depression .
    LY393558
  • HY-19417A

    Serotonin Transporter 5-HT Receptor Neurological Disease
    Wf-516 is an inhibitor of 5-HT reuptake, and an antagonist of 5-HT1A and 5-HT2A receptors, with Ki of 5 nM and 40 nM for 5-HT1A receptor and 5-HT2A receptor in humans, respectively, and has potent antidepressant activity.
    Wf-516
  • HY-G0014

    Quetiapine S-oxide

    Drug Metabolite Neurological Disease
    Quetiapine sulfoxide (Quetiapine S-oxide) is a main metabolite of Quetiapinem. Quetiapine is a second-generation antipsychotic . Quetiapine is a 5-HT receptors agonist and a dopamine receptor antagonist .
    Quetiapine sulfoxide
  • HY-101344

    5-HT Receptor Neurological Disease
    Cyanopindolol fumarate is a 5-HT receptor antagonist .
    Cyanopindolol fumarate
  • HY-14542C

    CP-88059 mesylate

    5-HT Receptor Dopamine Receptor Neurological Disease
    Ziprasidone (CP-88059) mesylate is an orally active combined 5-HT and dopamine receptor antagonist . Ziprasidone mesylate has affinities for Rat D2 (Ki=4.8 nM), 5-HT2A (Ki=0.42 nM) and 5-HT1A (Ki=3.4 nM) .
    Ziprasidone mesylate
  • HY-14542B

    CP-88059 mesylate trihydrate

    5-HT Receptor Dopamine Receptor Neurological Disease
    Ziprasidone (CP-88059) mesylate trihydrate is an orally active combined 5-HT and dopamine receptor antagonist . Ziprasidone mesylate trihydrate has affinities for Rat D2 (Ki=4.8 nM), 5-HT2A (Ki=0.42 nM) and 5-HT1A (Ki=3.4 nM) .
    Ziprasidone mesylate trihydrate
  • HY-B0031S2

    Isotope-Labeled Compounds 5-HT Receptor Dopamine Receptor Neurological Disease
    Quetiapine-d8 (fumarate) is the deuterium labeled Quetiapine. Quetiapine is a 5-HT receptors agonist with a pEC50 of 4.77 for human 5-HT1A receptor. Quetiapine is a dopamine receptor antagonist with a pIC50 of 6.33 for human D2 receptor. Quetiapine has moderate to high affinity for the human D2, HT1A, 5-HT2A, 5-HT2C receptor with pKis of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects .
    Quetiapine-d8 fumarate
  • HY-P3839

    Opioid Receptor Neurological Disease
    Nocistatin, a neuropeptide, is an endogenous ligand for the orphan opioid receptor-like receptor. Nocistatin is also a functional antagonist of neuropeptide nociceptin or orphanin FQ (Noc/OFQ). Nocistatin inhibits 5-HT release via a Gi/o proteinmediated pathway. Nocistatin blocks Nociceptin (Nociceptin)-induced allodynia and hyperalgesia .
    Nocistatin
  • HY-W982195

    Adrenergic Receptor 5-HT Receptor Neurological Disease
    Napamezole hydrochloride is an orally active α-2 adrenergic receptor antagonist and serotonin (5-HT Receptor) reuptake inhibitor, with Ki values of 28 nM and 93 nM for rat α-2 and α-1 adrenergic receptors, respectively. Napamezole hydrochloride can be used for the research of depression .
    Napamezole hydrochloride
  • HY-106605

    LY 120363

    Dopamine Receptor 5-HT Receptor Neurological Disease
    Flumezapine (LY 120363) is a potent and balanced antagonist of the dopamine D2 receptor and the 5-hydroxytryptamine receptor (5-HT receptor). Flumezapine does not alter the increase in serum cortisol caused by κ-opioid receptor agonists. Flumezapine inhibits the conditioned avoidance response in rats and has a low risk of extrapyramidal side effects. Flumezapine can be used in antipsychotic research .
    Flumezapine
  • HY-153091

    Adrenergic Receptor 5-HT Receptor Sigma Receptor Neurological Disease
    BMY 14802 is a sigma-1 receptor (σ1R) antagonist, as well as an agonist at serotonin (5-HT) 1A and adrenergic alpha-1 receptors. BMY 14802 inhibits abnormal involuntary movement (AIM) in rat Parkinson's disease (PD) model, with down-regulating the expression of AIM .
    BMY 14802

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