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5-HT1B Receptors Inhibitors

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (25) Adrenergic Receptor (6) Autophagy (1) Isotope-Labeled Compounds (6) P2X Receptor (1) Reference Standards (2) Serotonin Transporter (8)
By Research Areas:	Cancer (6) Cardiovascular Disease (9) Inflammation/Immunology (5) Neurological Disease (20)

Inhibitors & Agonists

Isotope-Labeled Compounds

Targets Recommended: Serpin

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-103089

LY393558	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 .

HY-15414

Vortioxetine Maximum Cited Publications 9 Publications Verification Lu AA 21004	5-HT Receptor Serotonin Transporter	Neurological Disease Cancer
Vortioxetine (Lu AA 21004) is an antagonist of 5-HT_3A and 5-HT₇ receptors (K_i: 3.7 nM, 19 nM) and an inhibitor of serotonin transporter (SERT) (K_i: 1.6 nM), as well as a *5-HT_1A agonist and a partial agonist of 5-HT_1B* (K_i: 15 nM, 33 nM) .**

HY-15414A

Vortioxetine hydrobromide Maximum Cited Publications 9 Publications Verification Lu AA21004 hydrobromide	5-HT Receptor Serotonin Transporter	Neurological Disease Cancer
Vortioxetine (Lu AA 21004) hydrobromide is an antagonist of 5-HT_3A and 5-HT₇ receptors (K_i: 3.7 nM, 19 nM) and an inhibitor of 5-hydroxytryptamine transporter (SERT) (K_i: 1.6 nM), as well as a 5-HT_1A agonist and a partial 5-HT_1B agonist (K_i: 15 nM, 33 nM) .

HY-15414R

Vortioxetine (Standard) Lu AA 21004 (Standard)	Reference Standards 5-HT Receptor Serotonin Transporter	Neurological Disease Cancer
Vortioxetine (Standard) is an analytical standard for Vortioxetine. This product is intended for research and analytical applications. Vortioxetine (Lu AA 21004) is an antagonist of 5-HT_3A and 5-HT₇ receptors (K_i: 3.7 nM, 19 nM) and an inhibitor of serotonin transporter (SERT) (K_i: 1.6 nM), as well as a 5-HT_1A agonist and a partial 5-HT_1B agonist (K_i: 15 nM, 33 nM) .

HY-103156

NAS-181 dimesylate	5-HT Receptor	Neurological Disease
NAS181 is a potent and selective antagonist of rat 5-HT_1B receptor, with a K_i of 47 nM. NAS181 shows 13-fold selectivity for r5-HT_1B over bovine 5-HT_1B receptor (K_i=630 nM). NAS181 increases the 5-HT turnover and the synaptic concentration of 5-HT by inhibiting terminal r5-HT_1B autoreceptors .

HY-19578A

Isamoltan hydrochloride (±)-Isamoltane hydrochloride	Adrenergic Receptor 5-HT Receptor	Neurological Disease
Isamoltan ((±)-Isamoltane) hydrochloride is a selective antagonist of **5-HT_1B receptor, with an IC₅₀** of 39 nM for inhibits the binding of [ ¹²⁵I]ICYP to 5-HT_1B 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 .

HY-135507A

NAS-181 free base	5-HT Receptor	Neurological Disease
NAS181 free base is a potent and selective antagonist of rat 5-HT_1B receptor, with a K_i of 47 nM. NAS181 free base shows 13-fold selectivity for r5-HT_1B over bovine 5-HT_1B receptor (K_i=630 nM). NAS181 free base increases the 5-HT turnover and the synaptic concentration of 5-HT by inhibiting terminal r5-HT_1B autoreceptors .

HY-19578B

Isamoltane hemifumarate (±)-Isamoltane hemifumarate	5-HT Receptor Adrenergic Receptor	Neurological Disease
Isamoltane hemifumarate is a selective antagonist of **5-HT_1B receptor, with an IC₅₀** of 39 nM for inhibits the binding of [ ¹²⁵I]ICYP to 5-HT_1B recognition sites in rat brain membranes. Isamoltane hemifumarate is also a β-adrenoceptor ligand, with an IC₅₀ of 8.4 nM. Isamoltane hemifumarate shows anxiolytic activity .

HY-15414S

Vortioxetine-d8 Lu AA 21004 d₈	Isotope-Labeled Compounds 5-HT Receptor Serotonin Transporter	Neurological Disease
Vortioxetine-d₈ (Lu AA 21004-d₈) is a deuterated version of Vortioxetine. Vortioxetine (Lu AA 21004) is an antagonist of 5-HT_3A and 5-HT₇ receptors (K_i: 3.7 nM, 19 nM) and an inhibitor of 5-hydroxytryptamine transporter (SERT) (K_i: 1.6 nM), as well as a 5-HT_1A agonist and a partial 5-HT_1B agonist (K_i: 15 nM, 33 nM) .

HY-15414S2

Vortioxetine-d4 Lu AA 21004-d₄	Isotope-Labeled Compounds 5-HT Receptor Serotonin Transporter	Neurological Disease
Vortioxetine-d₄ (Lu AA 21004-d₄) is the deuterium labeled Vortioxetine (HY-15414). Vortioxetine is an antagonist of 5-HT3A and 5-HT7 receptors (K_i: 3.7 nM, 19 nM) and an inhibitor of serotonin transporter (SERT) (K_i: 1.6 nM), as well as a 5-HT1A agonist and a partial agonist of 5-HT1B (K_i: 15 nM, 33 nM) .

HY-15414AS

Vortioxetine-d8 hydrobromide Lu AA21004-d₈ hydrobromide	Isotope-Labeled Compounds 5-HT Receptor Serotonin Transporter	Neurological Disease
Vortioxetine-d₈ (Lu AA 21004-d₈) hydrobromide is the deuterated form of Vortioxetine. Vortioxetine (Lu AA 21004) is an antagonist of 5-HT_3A and 5-HT₇ receptors (K_i: 3.7 nM, 19 nM) and an inhibitor of 5-hydroxytryptamine transporter (SERT) (K_i: 1.6 nM), as well as a *5-HT_1A agonist and a partial 5-HT_1B* agonist (K_i: 15 nM, 33 nM) .**

HY-122537

Arotinolol hydrochloride	Adrenergic Receptor 5-HT Receptor	Cardiovascular Disease
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 *5HT_1B*-serotonergic receptor sites . Arotinolol hydrochloride is an antihypertensive agent for the treatment of a variety of cardiovascular pathologies as well as non-cardiovascular diseases .

HY-122537A

Arotinolol	Adrenergic Receptor 5-HT Receptor	Cardiovascular Disease
Arotinolol is a nonselective α/β-adrenergic receptor blocker and a vasodilating β-blocker . Arotinolol also shows potency for inhibiting the binding of the radioligand ¹²⁵I-ICYP to *5HT_1B*-serotonergic receptor sites . Arotinolol is an antihypertensive agent for the treatment of a variety of cardiovascular pathologies as well as non-cardiovascular diseases .

HY-15414S3

Vortioxetine-d3 Lu AA 21004-d₃	Isotope-Labeled Compounds 5-HT Receptor Serotonin Transporter	Neurological Disease Cancer
Vortioxetine-d₃ (Lu AA 21004-d₃) is a deuterium labeled Vortioxetine (HY-15414). Vortioxetine (Lu AA 21004) is an antagonist of 5-HT_3A and 5-HT₇ receptors (K_i: 3.7 nM, 19 nM) and an inhibitor of serotonin transporter (SERT) (K_i: 1.6 nM), as well as a *5-HT_1A agonist and a partial agonist of 5-HT_1B* (K_i: 15 nM, 33 nM) .**

HY-15414S1

Vortioxetine-d6 Lu AA 21004-d₆	Serotonin Transporter 5-HT Receptor Isotope-Labeled Compounds	Neurological Disease Cancer
Vortioxetine-d6 (Lu AA 21004-d6) is the deuterium labeled Vortioxetine (HY-B1490A). Vortioxetine (Lu AA 21004) is an antagonist of 5-HT_3A and 5-HT₇ receptors (K_i: 3.7 nM, 19 nM) and an inhibitor of serotonin transporter (SERT) (K_i: 1.6 nM), as well as a *5-HT_1A agonist and a partial agonist of 5-HT_1B* (K_i: 15 nM, 33 nM) .**

HY-W653969

Arotinolol-d5 hydrochloride	Isotope-Labeled Compounds Adrenergic Receptor 5-HT Receptor	Cardiovascular Disease
Arotinolol-d₅ (hydrochloride) is deuterium labeled Arotinolol. Arotinolol is a nonselective α/β-adrenergic receptor blocker and a vasodilating β-blocker . Arotinolol also shows potency for inhibiting the binding of the radioligand ¹²⁵I-ICYP to *5HT_1B*-serotonergic receptor sites. Arotinolol is an antihypertensive agent for the treatment of a variety of cardiovascular pathologies as well as non-cardiovascular diseases .

HY-122537AR

Arotinolol (Standard)	Adrenergic Receptor 5-HT Receptor	Cardiovascular Disease
Arotinolol (Standard) is the analytical standard of Arotinolol. This product is intended for research and analytical applications. Arotinolol is a nonselective α/β-adrenergic receptor blocker and a vasodilating β-blocker . Arotinolol also shows potency for inhibiting the binding of the radioligand 125I-ICYP to 5HT1B-serotonergic receptor sites . Arotinolol is an antihypertensive agent for the treatment of a variety of cardiovascular pathologies as well as non-cardiovascular diseases .

HY-134807

Indophagolin	P2X Receptor 5-HT Receptor Autophagy	Cancer
Indophagolin is a potent, indoline-containing autophagy inhibitor (IC₅₀=140 nM). Indophagolin antagonizes the purinergic receptor P2X₄ as well as P2X₁ and P2X₃ with IC₅₀s of 2.71, 2.40 and 3.49 μM, respectively. Indophagolin also antagonizes the G_q-protein-coupled P2Y₄, P2Y₆, and P2Y₁₁ receptors (IC₅₀s =3.4~15.4 μM). Indophagolin has a strong antagonistic effect on serotonin receptor 5-HT₆ (IC₅₀=1.0 μM) and a moderate effect on receptors 5-HT_1B, 5-HT_2B, 5-HT_4e, and 5-HT₇ .

HY-103149

SB-216641A SB-216641 hydrochloride	5-HT Receptor	Neurological Disease
SB-216641A (SB-216641 hydrochloride) is a selective antagonist of **5-HT_1B/D receptor*. SB-216641A shows high affinity and selectivity for h5-HT_1B* receptors over h5-HT_1D receptors. SB-216641A inhibits the function of SKF-99101H .

HY-121562

SB 714786	5-HT Receptor	Neurological Disease
SB 714786 is a potent and selective 5-hydroxytryptamine 1D (5-HT1D) receptor antagonist. It was developed from the previously reported series of dual 5-HT1 selective 5-hydroxytryptamine reuptake inhibitors (5HT1-SSRIs). SB 714786 is the first reported highly potent and selective 5-HT1D receptor antagonist, providing an extremely useful pharmacological tool for further understanding the role of 5-HT1 receptor subtypes. It has no or very low intrinsic activity against all three receptors. SB 714786 has pKi values of 6.5, 6.7, 9.1 and 6.5 for 5-HT1A, 5-HT1B, 5-HT1D and SerT receptors, respectively, showing high selectivity for 5-HT1D receptors. These properties make SB 714786 a potential tool compound for studying the function of 5-HT1D receptors and the treatment of related diseases.

HY-B0197

Naratriptan GR-85548A	5-HT Receptor	Cardiovascular Disease Neurological Disease Inflammation/Immunology
Naratriptan is an orally active and selective **5-HT1B/1D receptor** agonist. Naratriptan is peripherally active and has good oral bioavailability, inducing cranial artery vasoconstriction by activating 5-HT1B/1D receptors (EC₅₀=0.11 μM for dog basilar artery). Naratriptan also inhibits trigeminal nerve-mediated dural neurogenic plasma extravasation and reduces sterile inflammation. Naratriptan is mainly used in the research of acute migraine, targeting cranial vascular and neuroinflammatory mechanisms .

HY-B0197A

Naratriptan hydrochloride 2 Publications Verification GR-85548A hydrochloride	5-HT Receptor	Cardiovascular Disease Neurological Disease Inflammation/Immunology
Naratriptan (GR-85548A) hydrochloride is a selective **5-HT1B/1D receptor** agonist. Naratriptan hydrochloride is peripherally active and has good oral bioavailability, inducing cranial artery vasoconstriction by activating 5-HT1B/1D receptors (EC₅₀=0.11 μM for dog basilar artery). Naratriptan hydrochloride also inhibits trigeminal nerve-mediated dural neurogenic plasma extravasation and reduces sterile inflammation. Naratriptan hydrochloride is mainly used in the research of acute migraine, targeting cranial vascular and neuroinflammatory mechanisms .

HY-B0197S

Naratriptan-d3 GR-85548A-d₃-1	5-HT Receptor	Cardiovascular Disease Neurological Disease Inflammation/Immunology
Naratriptan-d₃ (GR-85548A-d₃) is the deuterium labeled Naratriptan (HY-B0197). Naratriptan is a selective **5-HT1B/1D receptor** agonist. Naratriptan is peripherally active and has good oral bioavailability, inducing cranial artery vasoconstriction by activating 5-HT1B/1D receptors (EC₅₀=0.11 μM for dog basilar artery). Naratriptan also inhibits trigeminal nerve-mediated dural neurogenic plasma extravasation and reduces sterile inflammation. Naratriptan is mainly used in the research of acute migraine, targeting cranial vascular and neuroinflammatory mechanisms .

HY-B0197AR

Naratriptan hydrochloride (Standard) GR-85548A hydrochloride (Standard)	Reference Standards 5-HT Receptor	Cardiovascular Disease Neurological Disease Inflammation/Immunology
Naratriptan (GR-85548A) hydrochloride (Standard) is the analytical standard of Naratriptan hydrochloride (HY-B0197A). This product is intended for research and analytical applications. Naratriptan is a selective **5-HT1B/1D receptor** agonist. Naratriptan is peripherally active and has good oral bioavailability, inducing cranial artery vasoconstriction by activating 5-HT1B/1D receptors (EC₅₀=0.11 μM for dog basilar artery). Naratriptan also inhibits trigeminal nerve-mediated dural neurogenic plasma extravasation and reduces sterile inflammation. Naratriptan is mainly used in the research of acute migraine, targeting cranial vascular and neuroinflammatory mechanisms .

HY-B0197AS

Naratriptan-d3 hydrochloride GR-85548A d₃	5-HT Receptor	Cardiovascular Disease Neurological Disease Inflammation/Immunology
Naratriptan-d₃ (GR-85548A-d₃) is the deuterium labeled Naratriptan hydrochloride (HY-B0197A). Naratriptan hydrochloride is a selective **5-HT1B/1D receptor** agonist. Naratriptan hydrochloride is peripherally active and has good oral bioavailability, inducing cranial artery vasoconstriction by activating 5-HT1B/1D receptors (EC₅₀=0.11 μM for dog basilar artery). Naratriptan hydrochloride also inhibits trigeminal nerve-mediated dural neurogenic plasma extravasation and reduces sterile inflammation. Naratriptan hydrochloride is mainly used in the research of acute migraine, targeting cranial vascular and neuroinflammatory mechanisms .

Cat. No.	Product Name	Chemical Structure

HY-15414AS

Vortioxetine-d8 hydrobromide
Vortioxetine-d₈ (Lu AA 21004-d₈) hydrobromide is the deuterated form of Vortioxetine. Vortioxetine (Lu AA 21004) is an antagonist of 5-HT_3A and 5-HT₇ receptors (K_i: 3.7 nM, 19 nM) and an inhibitor of 5-hydroxytryptamine transporter (SERT) (K_i: 1.6 nM), as well as a *5-HT_1A agonist and a partial 5-HT_1B* agonist (K_i: 15 nM, 33 nM) .**

HY-W653969

Arotinolol-d5 hydrochloride
Arotinolol-d₅ (hydrochloride) is deuterium labeled Arotinolol. Arotinolol is a nonselective α/β-adrenergic receptor blocker and a vasodilating β-blocker . Arotinolol also shows potency for inhibiting the binding of the radioligand ¹²⁵I-ICYP to *5HT_1B*-serotonergic receptor sites. Arotinolol is an antihypertensive agent for the treatment of a variety of cardiovascular pathologies as well as non-cardiovascular diseases .

Arotinolol-d5 hydrochloride

Arotinolol-d₅ (hydrochloride) is deuterium labeled Arotinolol. Arotinolol is a nonselective α/β-adrenergic receptor blocker and a vasodilating β-blocker . Arotinolol also shows potency for inhibiting the binding of the radioligand ¹²⁵I-ICYP to 5HT_1B-serotonergic receptor sites. Arotinolol is an antihypertensive agent for the treatment of a variety of cardiovascular pathologies as well as non-cardiovascular diseases .

HY-15414S

Vortioxetine-d8
Vortioxetine-d₈ (Lu AA 21004-d₈) is a deuterated version of Vortioxetine. Vortioxetine (Lu AA 21004) is an antagonist of 5-HT_3A and 5-HT₇ receptors (K_i: 3.7 nM, 19 nM) and an inhibitor of 5-hydroxytryptamine transporter (SERT) (K_i: 1.6 nM), as well as a 5-HT_1A agonist and a partial 5-HT_1B agonist (K_i: 15 nM, 33 nM) .

HY-15414S2

Vortioxetine-d4
Vortioxetine-d₄ (Lu AA 21004-d₄) is the deuterium labeled Vortioxetine (HY-15414). Vortioxetine is an antagonist of 5-HT3A and 5-HT7 receptors (K_i: 3.7 nM, 19 nM) and an inhibitor of serotonin transporter (SERT) (K_i: 1.6 nM), as well as a 5-HT1A agonist and a partial agonist of 5-HT1B (K_i: 15 nM, 33 nM) .

HY-15414S3

Vortioxetine-d3
Vortioxetine-d₃ (Lu AA 21004-d₃) is a deuterium labeled Vortioxetine (HY-15414). Vortioxetine (Lu AA 21004) is an antagonist of 5-HT_3A and 5-HT₇ receptors (K_i: 3.7 nM, 19 nM) and an inhibitor of serotonin transporter (SERT) (K_i: 1.6 nM), as well as a *5-HT_1A agonist and a partial agonist of 5-HT_1B* (K_i: 15 nM, 33 nM) .**

HY-15414S1

Vortioxetine-d6
Vortioxetine-d6 (Lu AA 21004-d6) is the deuterium labeled Vortioxetine (HY-B1490A). Vortioxetine (Lu AA 21004) is an antagonist of 5-HT_3A and 5-HT₇ receptors (K_i: 3.7 nM, 19 nM) and an inhibitor of serotonin transporter (SERT) (K_i: 1.6 nM), as well as a *5-HT_1A agonist and a partial agonist of 5-HT_1B* (K_i: 15 nM, 33 nM) .**

HY-B0197S

Naratriptan-d3
Naratriptan-d₃ (GR-85548A-d₃) is the deuterium labeled Naratriptan (HY-B0197). Naratriptan is a selective **5-HT1B/1D receptor** agonist. Naratriptan is peripherally active and has good oral bioavailability, inducing cranial artery vasoconstriction by activating 5-HT1B/1D receptors (EC₅₀=0.11 μM for dog basilar artery). Naratriptan also inhibits trigeminal nerve-mediated dural neurogenic plasma extravasation and reduces sterile inflammation. Naratriptan is mainly used in the research of acute migraine, targeting cranial vascular and neuroinflammatory mechanisms .

Naratriptan-d3

Naratriptan-d₃ (GR-85548A-d₃) is the deuterium labeled Naratriptan (HY-B0197). Naratriptan is a selective 5-HT1B/1D receptor agonist. Naratriptan is peripherally active and has good oral bioavailability, inducing cranial artery vasoconstriction by activating 5-HT1B/1D receptors (EC₅₀=0.11 μM for dog basilar artery). Naratriptan also inhibits trigeminal nerve-mediated dural neurogenic plasma extravasation and reduces sterile inflammation. Naratriptan is mainly used in the research of acute migraine, targeting cranial vascular and neuroinflammatory mechanisms .

HY-B0197AS

Naratriptan-d3 hydrochloride
Naratriptan-d₃ (GR-85548A-d₃) is the deuterium labeled Naratriptan hydrochloride (HY-B0197A). Naratriptan hydrochloride is a selective **5-HT1B/1D receptor** agonist. Naratriptan hydrochloride is peripherally active and has good oral bioavailability, inducing cranial artery vasoconstriction by activating 5-HT1B/1D receptors (EC₅₀=0.11 μM for dog basilar artery). Naratriptan hydrochloride also inhibits trigeminal nerve-mediated dural neurogenic plasma extravasation and reduces sterile inflammation. Naratriptan hydrochloride is mainly used in the research of acute migraine, targeting cranial vascular and neuroinflammatory mechanisms .

Naratriptan-d3 hydrochloride

Naratriptan-d₃ (GR-85548A-d₃) is the deuterium labeled Naratriptan hydrochloride (HY-B0197A). Naratriptan hydrochloride is a selective 5-HT1B/1D receptor agonist. Naratriptan hydrochloride is peripherally active and has good oral bioavailability, inducing cranial artery vasoconstriction by activating 5-HT1B/1D receptors (EC₅₀=0.11 μM for dog basilar artery). Naratriptan hydrochloride also inhibits trigeminal nerve-mediated dural neurogenic plasma extravasation and reduces sterile inflammation. Naratriptan hydrochloride is mainly used in the research of acute migraine, targeting cranial vascular and neuroinflammatory mechanisms .

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