2. Signaling Pathways
  3. GPCR/G Protein
    Neuronal Signaling
  4. 5-HT Receptor
  5. 5-HT1 Receptor Isoform
  6. 5-HT1 Receptor Antagonist

5-HT1 Receptor Antagonist

5-HT1 Receptor Antagonists (98):

Cat. No. Product Name Effect Purity
  • HY-10349
    WAY-100635
    		Antagonist 99.51%
    WAY-100635 is a potent and selective 5-HT1A Receptor antagonist with a pIC50 of 8.87, an apparent pA2 of 9.71. WAY-100635 is a potent and selective 5-hydroxytryptamine 1A (5-HT1A) receptor antagonist with an IC50 value of 0.91 nM and Ki value of 0.39 nM. WAY-100635 has pIC50 values for 5-HT1A and α1-adrenergic receptors of 8.9 and 6.6, respectively. WAY-100635 is also a potent dopamine D4 receptor agonist.
  • HY-106617
    Etoperidone
    		Antagonist
    Etoperidone, an antidepressant agent, is an orally active serotonin and nor-adrenaline re-uptake antagonist. Etoperidone 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.
  • HY-14940
    Volinanserin
    		Antagonist 99.76%
    Volinanserin is a potent and selective antagonist of 5-HT2 receptor, with a Ki of 0.36 nM, and shows 300-fold selectivity for 5-HT2 receptor over 5-HT1c, alpha-1 and DA D2 receptors. Volinanserin has antipsychotic activity.
  • HY-B0982
    Pindolol
    		Antagonist 99.91%
    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.
  • HY-14542
    Ziprasidone
    		Antagonist 99.81%
    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).
  • HY-B1371
    Spiperone
    		Antagonist 99.00%
    Spiperone (Spiroperidol) is a potent dopamine D2, serotonin 5-HT1A, and serotonin 5-HT2A antagonist. Spiperone is also a labelled ligand for neuroleptic receptors. Spiperone enhances intracellular calcium level and inhibits the Wnt signaling pathway. Spiperone has the potential for the research of neurology diseases.
  • HY-103152
    GR 113808
    		Antagonist 99.96%
    GR 113808 is a potent and highly selective 5-HT4 receptor antagonist (pKb= 8.8). GR 113808 shows 300-fold selectivity over 5-HT1A, 5-HT1B, 5-HT2A, 5-HT2C and 5-HT3 receptors.
  • HY-B1517
    Alprenolol
    		Antagonist 99.94%
    Alprenolol ((RS)-Alprenolol; dl-Alprenolol) is an orally active non-selective β-adrenoceptor antagonist and an antagonist of 5-HT1A and 5-HT1B receptors. Alprenolol is used as an anti-hypertensive, anti-anginal and anti-arrhythmic agent.
  • HY-101105A
    SB-224289 hydrochloride
    		Antagonist ≥99.0%
    SB-224289 hydrochloride is a selective 5-HT1B receptor antagonist, with anxiolytic effect.
  • HY-107836
    Methiothepin mesylate
    		Antagonist 99.60%
    Methiothepin (Metitepine) mesylate is a potent and non-selective 5-HT2 receptor antagonist, with pKds of 7.10 (5-HT1A), 7.28 (5HT1B), 7.56 (5HT1C), 6.99 (5HT1D), 7.0 (5-HT5A), 7.8 (5-HT5B), 8.74 (5-HT6), and 8.99 (5-HT7), and pKis of 8.50 (5HT2A), 8.68 (5HT2B), and 8.35 (5HT2C).
  • HY-N0096
    Rotundine
    		Antagonist 99.96%
    Rotundine is an antagonist of dopamine D1, D2 and D3 receptors with IC50s of 166 nM, 1.4 μM and 3.3 μM, respectively. Rotundine is also an antagonist of 5-HT1A with an IC50 of 370 nM.
  • HY-B1213
    Trimipramine maleate
    		Antagonist 99.82%
    Trimipramine maleate 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 maleate 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 maleate has vascular activity and anxiolytic efficacy.
  • HY-11100
    Asenapine maleate
    		Antagonist 99.95%
    Asenapine maleate is a 5-HT (1A, 1B, 2A, 2B, 2C, 5A, 6, 7) and D2 antagonist with Ki values of 0.03-4.0 nM, 1.3nM, respectively, and an antipsychotic.
  • HY-B1517A
    Alprenolol hydrochloride
    		Antagonist 99.76%
    Alprenolol ((RS)-Alprenolol; dl-Alprenolol) hydrochloride is an orally active non-selective β-adrenoceptor antagonist and an antagonist of 5-HT1A and 5-HT1B receptors. Alprenolol hydrochloride is used as an anti-hypertensive, anti-anginal and anti-arrhythmic agent.
  • HY-10847B
    SB-277011 hydrochloride
    		Antagonist 98.54%
    SB-277011 hydrochloride (SB-277011A hydrochloride) is a potent, selective, orally bioavailable and brain penetrate dopamine D3 receptor (D3R) antagonist with Ki values of 10.7 nM and 11.2 nM at rodent and human D3R, respectively. SB-277011 hydrochloride displays 80- to 100-fold selectivity over other dopamine receptors with pKis of 8.0, 6.0, <5.2, and 5.9 for D3, D2, 5-HT1B, and 5-HT1D receptors, respectively.
  • HY-17407
    Ziprasidone hydrochloride monohydrate
    		Antagonist 98.11%
    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).
  • HY-13527
    LY310762
    		Antagonist 98.68%
    LY310762 is a selective 5-HT1D receptor antagonist (Ki=249 nM) with a weak affinity for 5-HT1B receptor. LY310762 effectively abolishes the renal vasodilatory effects of 5-HTSumatriptan (HY-B0121B)-induced decrease in excitatory postsynaptic potential (EPSC) amplitude.
  • HY-B0500
    Alverine citrate
    		Antagonist 99.71%
    Alverine citrate is a 5-HT1A receptor antagonist, with an IC50 of 101 nM.
  • HY-19818A
    NAN-190 hydrobromide
    		Antagonist 99.11%
    NAN-190 hydrobromide is a serotonin receptor 5-HT antagonist. NAN-190 is a selective antagonist of 5-HT1A.
  • HY-100794
    GR127935 hydrochloride
    		Antagonist 99.38%
    GR127935 hydrochloride is a potent and orally active 5-HT1D and 5-HT1B receptor antagonist with pKis of 8.5 for both isoforms. GR127935 hydrochloride has 100-fold selectivity for 5-HT1B/1D receptors over 5-HT1A, 5-HT2A, and 5-HT2C receptors. GR127935 hydrochloride can be used in neurological disease research.