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Isoforms Recommended:	5-HT₁ Receptor mLAG-3

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5HT1B receptor

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (133) Adrenergic Receptor (11) Autophagy (1) Dopamine Receptor (6) Drug Metabolite (1) Endogenous Metabolite (2) Histamine Receptor (1) Isotope-Labeled Compounds (18) mAChR (1) NO Synthase (1) P2X Receptor (1) Reference Standards (21) Serotonin Transporter (10) Sigma Receptor (1)
By Research Areas:	Cancer (11) Cardiovascular Disease (16) Infection (1) Inflammation/Immunology (13) Metabolic Disease (3) Neurological Disease (126)

139

Inhibitors & Agonists

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Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-B1517

Alprenolol 5+ Cited Publications (RS)-Alprenolol; dl-Alprenolol	5-HT Receptor	Cardiovascular Disease Cancer
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-15414

Vortioxetine Maximum Cited Publications 10 Publications Verification Lu AA 21004	5-HT Receptor Serotonin Transporter	Infection 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-B0121B

Sumatriptan 5+ Cited Publications GR 43175 free base	5-HT Receptor	Neurological Disease
Sumatriptan (GR 43175) is an orally active 5-HT1 receptor agonist with IC₅₀s of 7.3 nm, 9.3nm and 17.8 nm for 5-HT_1D, 5-HT_1B and 5-HT_1F receptors, respectively. Sumatriptan can be used for migraine headache research .

HY-B1517A

Alprenolol hydrochloride 5+ Cited Publications (RS)-Alprenolol hydrochloride; dl-Alprenolol hydrochloride	5-HT Receptor	Cardiovascular Disease Cancer
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-103152

GR 113808 5+ Cited Publications	5-HT Receptor	Neurological Disease Inflammation/Immunology
GR 113808 is a potent and highly selective *5-HT₄ receptor* antagonist (pK_b= 8.8). GR 113808 shows 300-fold selectivity over 5-HT_1A, 5-HT_1B, 5-HT_2A, 5-HT_2C and 5-HT₃ receptors .

HY-15414A

Vortioxetine hydrobromide Maximum Cited Publications 10 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-101105A

SB-224289 hydrochloride 2 Publications Verification SB-224289A	5-HT Receptor	Neurological Disease
SB-224289 hydrochloride is a selective **5-HT1B receptor** antagonist, with anxiolytic effect.

HY-A0010

Eletriptan hydrobromide 1 Publications Verification Eletriptan HBr; UK-116044 hydrobromide	5-HT Receptor	Neurological Disease
Eletriptan hydrobromide (Eletriptan HBr) is a *5-HT_1B* and 5-HT_1D receptor agonist with antimigraine activity, with K_i of 0.92 nM and 3.14 nM, respectively .

HY-B0229

Zolmitriptan BW-311C90; 311C90	5-HT Receptor Endogenous Metabolite	Neurological Disease
Zolmitriptan (BW-311C90; 311C90) is a **5-HT1B/1D receptor partial agonist that can cross the blood-brain barrier, with K_i*s of 5.01 nM, 0.63 nM, and 63.09 nM for 5-HT1B, 5-HT1D, 5-HT1F receptor*, respectively. Zolmitriptan can be used for the research of migraine .

HY-B0121

Sumatriptan succinate 5+ Cited Publications GR 43175 succinate	5-HT Receptor	Neurological Disease
Sumatriptan succinate (GR 43175) is an orally active 5-HT1 receptor agonist with IC₅₀s of 7.3 nm, 9.3nm and 17.8 nm for 5-HT_1D, 5-HT_1B and 5-HT_1F receptors, respectively. Sumatriptan succinate can be used for migraine headache research .

HY-16688

RU 24969 1 Publications Verification	5-HT Receptor	Neurological Disease
RU 24969 is a preferential *5-HT_1B* agonist, with a K_i of 0.38 nM, but also displays appreciable affinity for the 5-HT_1A receptor (K_i=2.5 nM), and has low affinity for other receptor sites in the brain. RU 24969 could decrease fluid consumption and increase forward locomotion .

HY-100942

5-Carboxamidotryptamine maleate 5-CT maleate	5-HT Receptor	Neurological Disease
5-Carboxamidotryptamine maleate (5-CT maleate) is a potent 5-HT_1A, *5-HT_1B, 5-HT_1D, 5-HT₅* and 5-HT₇ receptors agonist .

HY-B1658A

Frovatriptan succinate hydrate (R)-Frovatriptan succinate hydrate; SB 209509 succinate hydrate; VML 251 succinate hydrate	5-HT Receptor	Neurological Disease
Frovatriptan succinate hydrate ((R)-Frovatriptan succinate hydrate) is a potent, high affinity, selective and orally active *5-HT_1B* (pK₅₀ of 8.2) and 5-HT_1D receptor agonist. Frovatriptan succinate hydrate exhibits >10-fold selectivity for *5-HT_1B* and 5-HT_1D over 5-HT_1A, 5-HT_1F, and 5-HT₇ and >1000-fold selectivity over other 5-HT, dopamine, histamine H₁, and α1-adrenoceptor. Frovatriptan succinate hydrate has the potential for migraine research .

HY-103151

CP94253 hydrochloride	5-HT Receptor	Neurological Disease Metabolic Disease
CP94253 hydrochloride is an orally active, brain-penetrant and selective *5-HT_1B* receptor agonist with an K_i of 2 nM. CP94253 hydrochloride induces antidepressant-like effects, waking enhancement, sleep inhibition, increased sleep latency, hyperlocomotion, and suppressed aggressive behavior. CP94253 hydrochloride can be used for the research of depression and heightened aggressive behavior .

HY-101357A

CP 93129 dihydrochloride	5-HT Receptor	Neurological Disease
CP 93129 dihydrochloride is a potent **5HT_1B receptor** agonist. CP 93129 dihydrochloride has the potential for parkinson's disease research .

HY-10847B

SB-277011 hydrochloride 1 Publications Verification SB-277011A hydrochloride	Dopamine Receptor 5-HT Receptor	Neurological Disease
SB-277011 hydrochloride (SB-277011A hydrochloride) is a potent, selective, orally bioavailable and brain penetrate *dopamine D₃ receptor* (D₃R) antagonist with K_i** 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 pK_is of 8.0, 6.0, <5.2, and 5.9 for D3, D2, 5-HT_1B, and 5-HT_1D receptors, respectively .

HY-19477

SB-616234-A	5-HT Receptor	Neurological Disease
SB-616234-A is a selective and orally bioavailable **5-HT1B receptor** antagonist, with anxiolytic and antidepressant activity.

HY-103156

NAS-181 dimesylate 3 Publications Verification	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-100794

GR127935 hydrochloride	5-HT Receptor	Neurological Disease
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 .

HY-122537A

Arotinolol 2 Publications Verification	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-103142

AS19 1 Publications Verification	5-HT Receptor	Neurological Disease
AS19 is a potent, selective 5-HT₇ receptor agonist with an IC₅₀ value of 0.83 nM and a K_i of 0.6 nM. AS19 is selective for 5-HT₇ over 5-HT_1A, 5-HT_1B, 5-HT_1D, and 5-HT_5A receptors (K_is = 89.7 nM, 490 nM, 6.6 nM and 98.5 nM, respectively). AS19 enhances memory consolidation and reverses Scopolamine- or Dizocilpine-induced amnesia .

HY-W010869

GR 55562 hydrochloride	5-HT Receptor	Neurological Disease
GR 55562 hydrochloride is a selective **5-HT_1B receptor** antagonist. GR 55562 hydrochloride can be used for the research of nerve disease .

HY-103131

PNU-142633	5-HT Receptor	Neurological Disease
PNU-142633 is a high affinity, selective and orally active 5-HT_1D receptor agonist with K_is of 6 nM and > 18 000 nM for human 5-HT_1D receptor and human 5-HT_1B receptor, respectively. PNU-142633 has anti-migraine efficacy .

HY-W795507

Cyanopindolol	Adrenergic Receptor 5-HT Receptor	Neurological Disease
Cyanopindolol is an β3-adrenoceptor antagonist. Cyanopindolol is a potent and selective antagonist at the presynaptic serotonin autoreceptor in the rat brain cortex. Cyanopindolol has binding affinity for 5-HT1A and *5-HT1B* receptor (K_i: 2.1 and 3 nM respectively) .

HY-16688A

RU 24969 succinate 1 Publications Verification	5-HT Receptor	Neurological Disease
RU 24969 succinate is a 5-HT receptor agonist with K_i values of 0.38 and 2.5 nM for 5-HT_1B and 5-HT_1A, respectively. RU 24969 decreases fluid consumption and increases forward locomotion. RU 24969 succinate can be used for the research of neurological disease .

HY-13527

LY310762 1 Publications Verification	5-HT Receptor	Cardiovascular Disease Neurological Disease
LY310762 is a selective 5-HT_1D receptor antagonist (K_i=249 nM) with a weak affinity for *5-HT_1B* receptor. LY310762 effectively abolishes the renal vasodilatory effects of 5-HT

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-123869

GR127935	5-HT Receptor	Neurological Disease
GR127935 is a potent and orally active 5-HT1D and **5-HT1B receptor antagonist with pK_i*s 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 can be used in neurological disease research .

HY-135555

5-Carboxamidotryptamine 5-CT	5-HT Receptor	Neurological Disease
5-Carboxamidotryptamine (5-CT) is a *5-HT_1A, 5-HT_1B,* 5-HT_1D, 5-HT_5A, 5-HT₇** receptor agonist . 5-Carboxamidotryptamine has a K_i value of 4.6 nM for cloned human 5-HT_5A receptor. 5-Carboxamidotryptamine causes a dose-dependent reduction in rectal temperature of mice .

HY-19283

DU125530	5-HT Receptor	Neurological Disease
DU125530 is a potent and selective5-HT1A receptor antagonist with K_i values of 0.7, 890, 1200, 240, 750, 1100 nM for 5-HT1A, 5-HT1B, 5-HT1D, 5-HT2A, 5-HT2C, 5-HT3, respectively. DU125530 shows antidepressant effects .

HY-101100

Anpirtoline hydrochloride D-16949 hydrochloride	5-HT Receptor	Neurological Disease
Anpirtoline (D-16949) hydrochloride is a centrally acting **5-HT_1B receptor** agonist, with K_is of 28 nM (5-HT_1B), 150 nM (5-HT_1A) and 1.49 μM (5-HT2). Anpirtoline hydrochloride has serotonergic, antinociceptive, antidepressant-like effects .

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-101698

Alniditan Alnitidan	5-HT Receptor	Neurological Disease Inflammation/Immunology
Alniditan (Alnitidan) is a potent *5-HT_1B* and 5-HT_1D receptors agonist, with IC₅₀s of 1.7 nM and 1.3 nM for *h5-HT_1B* and h5-HT_1D receptors in HEK293 cells, respectively. Alniditan has migraine-preventive effects .

HY-A0039

Eletriptan UK-116044	5-HT Receptor	Neurological Disease Inflammation/Immunology
Eletriptan (UK-116044) is a highly selective and orally active serotonin *5-HT_1B* and 5-HT_1D receptor agonist, with pK_i values of 8.0 and 8.9, respectively. Eletriptan has inhibitory effects on markers of neurogenic inflammation in rats. Eletriptan can be used for researching migraine .

HY-B1517AR

Alprenolol hydrochloride (Standard) (RS)-Alprenolol hydrochloride (Standard); dl-Alprenolol hydrochloride (Standard)	Reference Standards 5-HT Receptor	Cancer
Alprenolol (hydrochloride) (Standard) is the analytical standard of Alprenolol (hydrochloride). This product is intended for research and analytical applications. 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-A0039S1

Eletriptan-d5	5-HT Receptor	Inflammation/Immunology
Eletriptan-d₅ is the deuterium labeled Eletriptan . Eletriptan (UK-116044) is a highly selective and orally active serotonin 5-HT1B and 5-HT1D receptor agonist, with pKi values of 8.0 and 8.9, respectively. Eletriptan has inhibitory effects on markers of neurogenic inflammation in rats. Eletriptan can be used for researching migraine .

HY-15414AR

Vortioxetine hydrobromide (Standard) Lu AA21004 hydrobromide (Standard)	5-HT Receptor Serotonin Transporter Reference Standards	Neurological Disease Cancer
Vortioxetine (hydrobromide) (Standard) is the analytical standard of Vortioxetine (hydrobromide). This product is intended for research and analytical applications. Vortioxetine (Lu AA 21004) hydrobromide is an antagonist of 5-HT3A and 5-HT7 receptors (Ki: 3.7 nM, 19 nM) and an inhibitor of 5-hydroxytryptamine transporter (SERT) (Ki: 1.6 nM), as well as a 5-HT1A agonist and a partial 5-HT1B agonist (Ki: 15 nM, 33 nM) .

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-101105

SB-224289	5-HT Receptor	Neurological Disease
SB-224289 is a selective **5-HT1B receptor** antagonist, with anxiolytic effect .

HY-101367

GR 55562	5-HT Receptor	Neurological Disease
GR 55562 is a selective **5-HT_1B receptor** antagonist. GR 55562 can be used for the research of nerve disease .

HY-B1658

Frovatriptan (R)-Frovatriptan; SB 209509; VML 251	5-HT Receptor	Neurological Disease
Frovatriptan is a potent *5-HT_1B//D* receptor agonist and has the highest 5-HT_1B potency in the triptan class. Frovatriptan is apparently cerebroselective. Frovatriptan is efficacious and even superior in some endpoints also when taken during the headache phase in migraine attacks with aura .

HY-101698B

Alniditan dihydrochloride Alnitidan dihydrochloride	5-HT Receptor	Neurological Disease Inflammation/Immunology
Alniditan (Alnitidan) dihydrochloride is a potent *5-HT_1B* and 5-HT_1D receptors agonist, with IC₅₀s of 1.7 nM and 1.3 nM for *h5-HT_1B* and h5-HT_1D receptors in HEK293 cells, respectively. Alniditan dihydrochloride has migraine-preventive effects .

HY-B1517B

Alprenolol benzoate	5-HT Receptor	Cardiovascular Disease Cancer
Alprenolol benzoate is an orally active non-selective β-adrenoceptor antagonist and an antagonist of 5-HT1A and *5-HT1B* receptors. Alprenolol benzoate is used as an anti-hypertensive, anti-anginal and anti-arrhythmic agent .

HY-10847

SB-277011 SB-277011A	Dopamine Receptor	Neurological Disease
SB-277011 is a potent and delective dopamine D3 receptor antagonist (pKi values are 8.0, 6.0, 5.0 and <5.2 for D3, D2, 5-HT1D and 5-HT1B respectively); brain penetrant.

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-B1658B

Frovatriptan succinate (R)-Frovatriptan succinate; SB 209509 succinate; VML 251 succinate	5-HT Receptor	Neurological Disease
Frovatriptan succinate ((R)-Frovatriptan succinate) is a potent, high affinity, selective and orally active *5-HT_1B* (pK₅₀ of 8.2) and 5-HT_1D receptor agonist. Frovatriptan succinate exhibits >10-fold selectivity for *5-HT_1B* and 5-HT_1D over 5-HT_1A, 5-HT_1F, and 5-HT₇ and >1000-fold selectivity over other 5-HT, dopamine, histamine H₁, and α1-adrenoceptor. Frovatriptan succinate has the potential for migraine research .

HY-B0229S

Zolmitriptan-d6	Isotope-Labeled Compounds 5-HT Receptor Endogenous Metabolite	Neurological Disease
Zolmitriptan-d₆ is deuterium labeled Zolmitriptan. Zolmitriptan (BW-311C90; 311C90) is a 5-HT1B/1D receptor partial agonist with K_is of 5.01 nM, 0.63 nM, and 63.09 nM for 5-HT1B, 5-HT1D, 5-HT1F receptor, respectively. Zolmitriptan can be used for the research of migraine .

HY-116603

SB-236057	5-HT Receptor	Others
SB-236057 is an inverse agonist of the *5-HT_1B* receptor that exhibits strong skeletal teratogenicity in rodents and rabbits. SB-236057 affects gene expression during embryonic development through interference with the Notch signaling pathway and interaction with r-esp1. SB-236057 induces somatic patterning and tail extension defects in rat embryos during early organogenesis .

HY-B0121R

Sumatriptan succinate (Standard) GR 43175 succinate (Standard)	5-HT Receptor Reference Standards	Neurological Disease
Sumatriptan (succinate) (Standard) is the analytical standard of Sumatriptan (succinate). This product is intended for research and analytical applications. Sumatriptan succinate (GR 43175) is an orally active 5-HT1 receptor agonist with K_is of 17 nM, 27 nM and 100 nM for 5-HT1D, *5-HT1B* and 5-HT1A receptors, respectively. Sumatriptan succinate can be used for migraine headache research .

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 .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-B0229

Zolmitriptan BW-311C90; 311C90	Structural Classification Alkaloids Neurological Disease Classification of Application Fields Endogenous metabolite Disease Research Fields Indole Alkaloids Source Classification	5-HT Receptor Endogenous Metabolite
Zolmitriptan (BW-311C90; 311C90) is a **5-HT1B/1D receptor partial agonist that can cross the blood-brain barrier, with K_i*s of 5.01 nM, 0.63 nM, and 63.09 nM for 5-HT1B, 5-HT1D, 5-HT1F receptor*, respectively. Zolmitriptan can be used for the research of migraine .

Cat. No.	Product Name	Chemical Structure

HY-A0039S1

Eletriptan-d5
Eletriptan-d₅ is the deuterium labeled Eletriptan . Eletriptan (UK-116044) is a highly selective and orally active serotonin 5-HT1B and 5-HT1D receptor agonist, with pKi values of 8.0 and 8.9, respectively. Eletriptan has inhibitory effects on markers of neurogenic inflammation in rats. Eletriptan can be used for researching migraine .

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-B0229S

Zolmitriptan-d6
Zolmitriptan-d₆ is deuterium labeled Zolmitriptan. Zolmitriptan (BW-311C90; 311C90) is a 5-HT1B/1D receptor partial agonist with K_is of 5.01 nM, 0.63 nM, and 63.09 nM for 5-HT1B, 5-HT1D, 5-HT1F receptor, respectively. Zolmitriptan can be used for the research of migraine .

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-A0039S

Eletriptan-d3
Eletriptan-d₃ is the deuterium labeled Eletriptan hydrobromide. Eletriptan hydrobromide is a selective 5-HT1B and 5-HT1D receptor agonist with K_i of 0.92 nM and 3.14 nM, respectively .

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 .

HY-B1658S

Frovatriptan-d3 hydrochloride
Frovatriptan-d₃ (hydrochloride) is the deuterium labeled Frovatriptan . Frovatriptan is a potent 5-HT1B//D receptor agonist and has the highest 5-HT1B potency in the triptan class. Frovatriptan is apparently cerebroselective. Frovatriptan is efficacious and even superior in some endpoints also when taken during the headache phase in migraine attacks with aura .

HY-B0121BS1

Sumatriptan-d6
Sumatriptan-d₆ is the deuterium labeled Sumatriptan. Sumatriptan is an orally active 5-HT1 receptor agonist with Kis of 17 nM, 27 nM and 100 nM for 5-HT1D, 5-HT1B and 5-HT1A receptors, respectively. Sumatriptan can be used for migraine headache research .

HY-B1658BS

Frovatriptan-d3 succinate

Frovatriptan-d₃ (succinate) is deuterium labeled Frovatriptan (succinate). Frovatriptan succinate ((R)-Frovatriptan succinate) is a potent, high affinity, selective and orally active 5-HT1B (pK50 of 8.2) and 5-HT1D receptor agonist. Frovatriptan succinate exhibits >10-fold selectivity for 5-HT1B and 5-HT1D over 5-HT1A, 5-HT1F, and 5-HT7 and >1000-fold selectivity over other 5-HT, dopamine, histamine H1, and α1-adrenoceptor. Frovatriptan succinate has the potential for migraine research .

HY-B0121BS

Sumatriptan-d6 succinate 1 Publications Verification
Sumatriptan-d6 succinate is the deuterium labeled Sumatriptan succinate. Sumatriptan succinate is an orally active 5-HT1 receptor agonist with K_is of 17 nM, 27 nM and 100 nM for 5-HT1D, *5-HT1B* and 5-HT1A receptors, respectively. Sumatriptan succinate can be used for migraine headache research .

HY-A0039S2

Eletriptan-d5 hydrochloride

Eletriptan-d₅ (hydrochloride) is the deuterium labeled Eletriptan hydrochloride . Eletriptan (UK-116044) hydrochloride is a highly selective and orally active serotonin 5-HT1B and 5-HT1D receptor agonist, with pKi values of 8.0 and 8.9, respectively. Eletriptan hydrochloride has inhibitory effects on markers of neurogenic inflammation in rats. Eletriptan hydrochloride can be used for researching migraine .

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-B0121BS2

Sumatriptan-d5
Sumatriptan-d₅ is deuterated labeled Sumatriptan (HY-B0121B). Sumatriptan (GR 43175) is an orally active 5-HT1 receptor agonist with IC₅₀s of 7.3 nm, 9.3nm and 17.8 nm for 5-HT_1D, 5-HT_1B and 5-HT_1F receptors, respectively. Sumatriptan can be used for migraine headache research .

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-B0121BS3

Sumatriptan-d6 formate
Sumatriptan-d₆ (formate) (GR 43175 free base-d₆ (formate)) is deuterium labeled Sumatriptan. Sumatriptan (GR 43175) is an orally active 5-HT1 receptor agonist with IC₅₀s of 7.3 nm, 9.3nm and 17.8 nm for 5-HT_1D, 5-HT_1B and 5-HT_1F receptors, respectively. Sumatriptan can be used for migraine headache research .

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 .

HY-B0383AS

Almotriptan hydrochloride-d6

Almotriptan-d₆ (PNU180638-d₆) hydrochloride is the deuterium labeled Almotriptan hydrochloride. Almotriptan hydrochloride is an orally active, highly selective agonist of the 5-HT_1B/1D receptor (5-HT_1B/1D receptor), with EC₅₀ values of 1.6 nM and 3.1 nM, respectively. Almotriptan hydrochloride shows moderate affinity for the 5-HT1F receptor, and weak affinity for the 5-HT1A, 5-HT6 and 5-HT7 receptors. Almotriptan hydrochloride induces intracranial vasoconstriction, inhibits nociceptive neurotransmission in the trigeminocervical complex, and suppresses the release of vasoactive peptides from trigeminal nerve endings. Almotriptan hydrochloride can be used in research related to migraine.

HY-B0383AS2

Almotriptan-d3 benzoate

Almotriptan-d₃ benzoate (PNU180638 free base-d₃) is deuterated labeled Almotriptan benzoate. Almotriptan benzoate is an orally active, highly selective agonist of the 5-HT_1B/1D receptor (5-HT_1B/1D receptor), with EC₅₀ values of 1.6 nM and 3.1 nM, respectively. Almotriptan benzoate shows moderate affinity for the 5-HT1F receptor, and weak affinity for the 5-HT1A, 5-HT6 and 5-HT7 receptors. Almotriptan benzoate induces intracranial vasoconstriction, inhibits nociceptive neurotransmission in the trigeminocervical complex, and suppresses the release of vasoactive peptides from trigeminal nerve endings. Almotriptan benzoate can be used in research related to migraine.

HY-143797S

Almotriptan-d6 maleate

Almotriptan-d₆ (PNU180638-d₆) maleate is the deuterium labeled Almotriptan maleate. Almotriptan malate is an orally active, highly selective agonist of the 5-HT_1B/1D receptor (5-HT_1B/1D receptor), with EC₅₀ values of 1.6 nM and 3.1 nM, respectively. Almotriptan malate shows moderate affinity for the 5-HT1F receptor, and weak affinity for the 5-HT1A, 5-HT6 and 5-HT7 receptors. Almotriptan malate induces intracranial vasoconstriction, inhibits nociceptive neurotransmission in the trigeminocervical complex, and suppresses the release of vasoactive peptides from trigeminal nerve endings. Almotriptan malate can be used in research related to migraine.

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 .

HY-B0982S

Pindolol-d7
Pindolol-d₇ (LB-46-d7) is the deuterium labeled Pindolol. Pindolol (LB-46) is the antagonist for 5-HT 1A (K_i=33 nM) and *5-HT 1B. Pindolol is the antagonist for β1/β2-adrenergic receptor*. Pindolol exhibits anti-anxiety and antidepressant effects .

HY-132343S

Zolmitriptan N-Oxide-d6
Zolmitriptan N-Oxide-d₆ is a deuterium labeled Zolmitriptan N-Oxide. Zolmitriptan N-Oxide is the major metabolite of Zolmitriptan. Zolmitriptan is a 5-HT1B/1D receptor partial agonist .

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