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benzodiazepine receptors

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By Targets:	Adrenergic Receptor (1) Akt (1) Apoptosis (1) Cholecystokinin Receptor (2) ERK (1) GABA Receptor (57) Histamine Receptor (6) iGluR (1) Imidazoline Receptor (1) Isotope-Labeled Compounds (2) JNK (1) Lipoxygenase (1) Monoamine Oxidase (2) nAChR (2) Opioid Receptor (1)
By Research Areas:	Cancer (3) Cardiovascular Disease (1) Endocrinology (8) Inflammation/Immunology (9) Metabolic Disease (2) Neurological Disease (65)
Click Chemistry:	Azide (1) Alkynes (1)

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Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-100369A

DMCM hydrochloride	GABA Receptor	Neurological Disease
DMCM hydrochloride is a nonselective full inverse agonist of *benzodiazepine. DMCM shows bnding afinity at human recombinant GABAA αxβ3γ2 receptor* subtypes with K_is of 10 nM, 13 nM, 7.5 nM, 2.2 nM for α1, α2, α3, and α5 ?receptors, respectively .

HY-105791

Sulazepam	Others	Inflammation/Immunology
Sulazepam, a benzodiazepine, is a selective ovarian cancer G protein-coupled receptor (OGR1) agonist. Sulazepam has anticonvulsive action and has the potential for airway hyperresponsiveness (AHR) research .

HY-101059

FGIN 1-27	Others	Neurological Disease
FGIN 1-27, an indoleacetamide, is a specific *peripheral benzodiazepine* receptor (PBR) ligand with a K_i** of 5.0 nM. FGIN 1-27 can penetrate the blood brain barrier (BBB). FGIN 1-27 inhibits the onset of Isoniazid-induced convulsions .

HY-19945

DAA-1106 1 Publications Verification	GABA Receptor	Neurological Disease
DAA1106 is a potent and selective ligand for peripheral benzodiazepine receptor (PBR), as a potent and selective agonist at the peripheral benzodiazepine receptor.

HY-103476

Ro15-4513	GABA Receptor	Neurological Disease
Ro15-4513, imidazobenzodiazepinone derivative, is a partial inverse agonist of benzodiazepine receptor (BZR) . Ro15-4513 is a potent ethanol antagonist . Ro15-4513 has anti-anxiety effect . Ro15-4513 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.

HY-111194

Ro 22-8515	Others	Others
Ro 22-8515 is a ligand of Benzodiazepine receptor .

HY-118259

L-663581 FG-8205	GABA Receptor	Neurological Disease
L-663581 (FG-8205) is an agonist of benzodiazepine receptor, acting as a partial agonist at GABA A receptor .

HY-119605

DAA-1097	Others	Neurological Disease
DAA-1097 is an orally active and selective agonist for the *peripheral benzodiazepine* receptor (PBR)**. DAA-1097 has anxiolytic effects .

HY-100248

Sarmazenil Ro 15-3505	GABA Receptor	Neurological Disease
Sarmazenil is a **benzodiazepine receptor** antagonist.

HY-19065

Ru-32514	GABA Receptor	Neurological Disease
Ru-32514 is an agonist of benzodiazepine receptor.

HY-19250

U-101017 PNU 101017	GABA Receptor	Neurological Disease
U-101017 is a partial agonist of **benzodiazepine receptor** and GABAA receptor, with anxiolytic effects.

HY-B0009

Flumazenil 3 Publications Verification Ro 15-1788	GABA Receptor	Neurological Disease
Flumazenil is a competitive GABAA receptor antagonist, used in the treatment of benzodiazepine overdoses.

HY-U00033

Iomazenil	Others	Neurological Disease
Iomazenil is a benzodiazepine receptor antagonist with partial inverse agonist activity. Iomazenil can assess the binding potential of central benzodiazepine receptors in the cerebral cortex and may reflect neuronal function in viable tissue. Iomazenil use is associated with improved cognitive function in adult patients with ischemic cerebral pathology after indirect revascularization surgery. Iomazenil demonstrated restoration of benzodiazepine receptor binding potential in the affected hemisphere after surgery on brain SPECT imaging .

HY-17617

Nastorazepide Z-360	Cholecystokinin Receptor	Endocrinology Cancer
Nastorazepide (Z-360), selective, orally available, 1,5-benzodiazepine derivative, is a gastrin/cholecystokinin 2 (CCK-2) receptor antagonist with potential antitumor activity .

HY-19308

RWJ-51204	GABA Receptor	Neurological Disease
RWJ-51204 is a partial agonist of GABA(A) receptor, with K_i of 0.2-2 nM to the benzodiazepine site on GABA(A) receptors.

HY-14575

Nastorazepide hemicalcium Z-360 hemicalcium	Cholecystokinin Receptor	Endocrinology Cancer
Nastorazepide (Z-360) hemicalcium, selective, orally available, 1,5-benzodiazepine derivative, is a gastrin/cholecystokinin 2 (CCK-2) receptor antagonist with potential antitumor activity .

HY-106316

CGS 20625	GABA Receptor	Neurological Disease
CGS 20625 is a potent, selective and orally active partial agonist for the central **benzodiazepine receptor*. CGS 20625 inhibits [3H]-flunitrazepam binding to central benzodiazepine* receptors with an IC₅₀ of 1.3 nM. CGS 20625 can be used for the research of pentylenetetrazol-induced seizures .

HY-100924

β-CCB	GABA Receptor	Neurological Disease
β-CCB is a ligand for benzodiazepine receptor, which inhibits the binding of [ ³H]flunitrazepam and ethyl (3-[ ³H]carboline-3-carboxylate to benzodiazepine receptors, with K_i of 3-4 nM. β-CCB exhibits proconvulsant and anxiogenic effects .

HY-100140

Pipequaline 1 Publications Verification PK-8165	GABA Receptor	Neurological Disease
Pipequaline (PK 8165) is a partial **benzodiazepine receptor** agonist with anxiolytic activity .

HY-N6648

Cirsimaritin	GABA Receptor	Neurological Disease
Cirsimaritin binds weakly to the benzodiazepine site on GABA_A receptors, with antidepressant, anxiolytic and antinociceptive activities.

HY-118308

AHN-683	GABA Receptor	Neurological Disease
AHN-683 is a luciferin-derived ligand that targets the peripheral benzodiazepine receptor (BDR).

HY-124225

RU 33965	GABA Receptor	Neurological Disease
RU 33965 is an orally active **benzodiazepine receptor** weak partial inverse agonist .

HY-100291

SX-3228	GABA Receptor	Neurological Disease
SX-3228 is a selective *benzodiazepine1* (BZ1) receptor agonist with an IC₅₀ of 17 nM.

HY-100140A

Pipequaline hydrochloride PK-8165 hydrochloride	GABA Receptor	Neurological Disease
Pipequaline hydrochloride (PK-8165 hydrochloride) is a partial **benzodiazepine receptor** agonist with anxiolytic activity .

HY-116813

ZK 93423	GABA Receptor	Neurological Disease
ZK 93423 is a potent benzodiazepine GABAA receptor agonist with a certain cooling effect on rodents .

HY-110399

Cirsiliol	Lipoxygenase	Neurological Disease
Cirsiliol is a potent and selective 5-lipoxygenase inhibitor and a competitive low affinity benzodiazepine receptor ligand.

HY-106635

Suriclone RP31264	GABA Receptor	Neurological Disease
Suriclone (RP31264) is a GABA receptor agonist. Suriclone is an anxiolytic agent with a high affinity for the benzodiazepine receptors. Suriclone has oral activity .

HY-106851

Panadiplon FG 10571; PNU 78875	GABA Receptor	Neurological Disease
Panadiplon (FG 10571; PNU 78875), a benzodiazepine receptor, is a 5GABAA partial agonist. Panadiplon exhibits selectivity for 5GABAA receptors versus 1GABAA receptors .

HY-U00215

Ro 41-3290	GABA Receptor	Neurological Disease
Ro 41-3290 is the desethylated derivative of Ro 41-3696, which is a nonbenzodiazepine partial agonist at the **benzodiazepine receptor**.

HY-111481

Flutazolam MS 4101; Ro 7-6102	GABA Receptor	Neurological Disease
Flutazolam (MS 4101; Ro 7-6102) is a medicine acts on benzodiazepine receptors of the brain and relieves anxiety or tension.

HY-124467

Difludiazepam Ro 07-4065	GABA Receptor	Neurological Disease
Difludiazepam (Ro 07-4065), a benzodiazepine, has binding affinity (0.613) to GABA_A receptors .

HY-139145

Etbicyphat Trimethylopropane phosphate	GABA Receptor	Neurological Disease
Etbicyphat (Trimethylopropane phosphate) is a potent GABA(A) receptors competitive antagonist. Etbicyphat induces epileptiform activities in hippocampal CA1 neurons, and binds to the GABA(A)-benzodiazepine receptors .

HY-167658

Tuclazepam KC 1956	GABA Receptor	Neurological Disease
Tuclazepam (KC 1956) is a derivative of benzodiazepines that has anti-anxiety and sedative effects .

HY-103225

S-8510 phosphate SB-737552 phosphate	GABA Receptor	Neurological Disease
S-8510 (phosphate) is an inverse **Benzodiazepine (BDZ) receptor** agonist, with K_is of 34.6 nM, 36.2 nM for –GABA and +GABA respectively.

HY-121877

Valnoctamide 1 Publications Verification Valmethamide	GABA Receptor	Neurological Disease
Valnoctamide (Valmethamide), a derivative of valproate, suppresses benzodiazepine-refractory status epilepticus. Valnoctamide (Valmethamide) acts directly on GABA_A receptors .

HY-14953

Imepitoin AWD 131-138	GABA Receptor	Neurological Disease
Imepitoin (AWD 131-138) is a new low-affinity partial benzodiazepine receptor agonist with potent anticonvulsant and anxiolytic properties in rodent models.

HY-106917

Lirequinil Ro 41-3696	GABA Receptor	Neurological Disease
Lirequinil (Ro 41-3696) is an orally active partial agonist of the **benzodiazepine (BDZ) receptor**. Lirequinil has the effect of promoting sleep .

HY-N1951

Miltirone 1 Publications Verification	GABA Receptor	Neurological Disease
Miltirone is a natural compound present in the root of Salvia miltiorrhiza. Miltirone is a central **benzodiazepine receptor partial agonist, with an IC₅₀** of 0.3 μM .

HY-114685

S-8510 free base SB-737552 free base	GABA Receptor	Neurological Disease
S-8510 free base is an inverse **Benzodiazepine (BDZ) receptor** agonist, with K_is of 34.6 nM, 36.2 nM for –GABA and +GABA respectively.

HY-121877S

Valnoctamide-d5	Isotope-Labeled Compounds GABA Receptor	Neurological Disease
Valnoctamide-d₅ is the deuterium labeled Valnoctamide. Valnoctamide (Valmethamide), a derivative of valproate, suppresses benzodiazepine-refractory status epilepticus. Valnoctamide (Valmethamide) acts directly on GABAA receptors[1][2].

HY-B0009R

Flumazenil (Standard)	GABA Receptor	Neurological Disease
Flumazenil (Standard) is the analytical standard of Flumazenil. This product is intended for research and analytical applications. Flumazenil is a competitive GABAA receptor antagonist, used in the treatment of benzodiazepine overdoses.

HY-B0548

Hydroxyzine	Histamine Receptor	Inflammation/Immunology Endocrinology
Hydroxyzine, a benzodiazepine antihistamine agent, acts as an orally active *histamine H1-receptor* and serotonin antagonist. Hydroxyzine has anxiolytic effect and can be used for the research of generalised anxiety disorder .

HY-19371

Lorediplon	GABA Receptor	Neurological Disease
Lorediplon is a novel non-benzodiazepine drug acting as a GABAA receptor modulator, differentially active at the alpha1-subunit, associated with promoting sleep.

HY-19082

Y-23684	GABA Receptor	Neurological Disease
Y-23684 is a partial agonist of benzodiazepine receptor (BZR) with anticonvulsant and anxiolytic activities. Y-23684 can be used in the research of treatment of anxiety disorders .

HY-139145S

Etbicyphat-13C3 Trimethylopropane phosphate-¹³C₃	GABA Receptor	Neurological Disease
Etbicyphat- ¹³C₃ is the ¹³C labeled Etbicyphat (HY-139145). Etbicyphat is a potent GABA(A) receptors competitive antagonist. Etbicyphat induces epileptiform activities in hippocampal CA1 neurons, and binds to the GABA(A)-benzodiazepine receptors[1][2].

HY-B0548A

Hydroxyzine dihydrochloride	Histamine Receptor	Inflammation/Immunology Endocrinology
Hydroxyzine dihydrochloride, a benzodiazepine antihistamine agent, acts as a orally active *histamine?H1-receptor* and serotonin antagonist. Hydroxyzine dihydrochloride has anxiolytic effect and can be used forthe research of generalised anxiety disorder .

HY-15527

Emapunil 3 Publications Verification AC-5216; XBD-173	Others	Neurological Disease Metabolic Disease
Emapunil (AC-5216), an orally active and selective TSPO (a mitochondrial benzodiazepine receptor) ligand, produces anti-anxiety and antidepressant-like effects in various animal models .

HY-121116

CGS 8216	GABA Receptor	Neurological Disease
CGS 8216, a **benzodiazepine receptor** antagonist, inhibits ³H-flunitrazepam ( ³H-FLU) binding to rat synaptosomal membranes in vitro at subnanomolar concentrations .

HY-19006

ZK-91296	Others	Neurological Disease
ZK-91296 is a GABA receptor agonist with anxiolytic activity. ZK-91296 can reduce anxiety in animals without causing sedation. ZK-91296 may have pharmacological selectivity for interaction with specific types of benzodiazepine receptors .

HY-106025

Radequinil AC-3933	GABA Receptor	Neurological Disease
Radequinil (AC-3933) is a benzodiazepine receptor (BzR) partial inverse agonist. AC-3933 binds to GABA(-) and GABA(+) ligand with K_is of 5.15 and 6.11 nM, respectively .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N6648

Cirsimaritin	Structural Classification Flavonoids Flavones Leguminosae Source classification Phenols Polyphenols Abrus precatorius Linn. Plants	GABA Receptor
Cirsimaritin binds weakly to the benzodiazepine site on GABA_A receptors, with antidepressant, anxiolytic and antinociceptive activities.

HY-110399

Cirsiliol	Structural Classification Flavonoids Flavones Leguminosae Source classification Phenols Polyphenols Abrus precatorius Linn. Plants	Lipoxygenase
Cirsiliol is a potent and selective 5-lipoxygenase inhibitor and a competitive low affinity benzodiazepine receptor ligand.

HY-N1951

Miltirone 1 Publications Verification	Structural Classification Terpenoids Labiatae Samanea saman (Jacq.) Merr. Source classification Diterpenoids Plants	GABA Receptor
Miltirone is a natural compound present in the root of Salvia miltiorrhiza. Miltirone is a central **benzodiazepine receptor partial agonist, with an IC₅₀** of 0.3 μM .

HY-Y0265

Isatin Indoline-2,3-dione	Cardiovascular Disease Alkaloids Structural Classification other families Neurological Disease Classification of Application Fields Source classification Plants Disease Research Fields Indole Alkaloids	Monoamine Oxidase Apoptosis
Isatin (Indoline-2,3-dione) is a potent inhibitor of monoamine oxidase (MAO) with an IC₅₀ of 3 μM. Also binds to central benzodiazepine receptors (IC₅₀ against clonazepam, 123 μM) . Also acts as an antagonist of both atrial natriuretic peptide stimulated and nitric oxide-stimulated guanylate cyclase activity . Shows effect on the serotonergic system .

HY-101392

Harmane 1 Publications Verification	Alkaloids Structural Classification other families Source classification Pyridine Alkaloids Plants Indole Alkaloids	Imidazoline Receptor Monoamine Oxidase Adrenergic Receptor nAChR GABA Receptor Opioid Receptor
Harmane is an inhibitor that binds to **benzodiazepine receptors (with an IC₅₀ value of 7 μM), has an IC₅₀** of 24 μM for muscarinic acetylcholine receptors (QNB), an IC₅₀ of 2.8 μM for opioid receptors, and IC₅₀ values of 163 and 101 μM for spironolactone and serotonin, respectively. Harmane is a selective monoamine oxidase inhibitor (with IC₅₀ values of 0.5 μM for MAO A and 5 μM for MAO B). Harman inhibits dopamine biosynthesis by decreasing tyrosine hydroxylase (TH) activity and enhancing levodopa (L-DOPA)-induced toxicity in PC12 cells. Harmane lowers blood pressure in rats through the I1 imidazoline receptor (I1 receptor) and has antidepressant, anxiolytic, anticonvulsant, and analgesic effects. Harmane enhances the mutagenicity induced by 2-acetylaminofluorene (AAF) .

HY-N7110

6-Hydroxyflavone	Structural Classification Monophenols Flavonoids Classification of Application Fields Flavones Labiatae Source classification Phenols Plants Medicago truncatula Gaertn. Inflammation/Immunology Disease Research Fields	Akt ERK JNK GABA Receptor
6-Hydroxyflavone is an orally effective flavonoid compound. 6-Hydroxyflavone can inhibit LPS (HY-D1056) -induced NO production and has anti-inflammatory effects. 6-Hydroxyflavone promotes osteoblast differentiation by activating AKT, ERK 1/2 and JNK signaling pathways. 6-Hydroxyflavone has an inhibitory effect on bovine hemoglobin (BHb) glycosylation. 6-Hydroxyflavone has a kidney protective effect. In addition, 6-Hydroxyflavone enhances GABA-induced current through the Benzodiazepine sites of γ-aminobutyric acid (GABA_A) receptors. 6-Hydroxyflavone shows a clear preference for α2 - and α3 - subtypes, which play an anti-anxiety role .

Cat. No.	Product Name	Chemical Structure

HY-B0548AS1

Hydroxyzine-d4' dihydrochloride
Hydroxyzine-d₄ (dihydrochloride) is the deuterium labeled Hydroxyzine dihydrochloride. Hydroxyzine dihydrochloride, a benzodiazepine antihistamine agent, acts as a orally active histamine H1-receptor and serotonin antagonist. Hydroxyzine dihydrochloride has anxiolytic effect and can be used forthe research of generalised anxiety disorder[1][2].

HY-121877S

Valnoctamide-d5
Valnoctamide-d₅ is the deuterium labeled Valnoctamide. Valnoctamide (Valmethamide), a derivative of valproate, suppresses benzodiazepine-refractory status epilepticus. Valnoctamide (Valmethamide) acts directly on GABAA receptors[1][2].

HY-139145S

Etbicyphat-13C3
Etbicyphat- ¹³C₃ is the ¹³C labeled Etbicyphat (HY-139145). Etbicyphat is a potent GABA(A) receptors competitive antagonist. Etbicyphat induces epileptiform activities in hippocampal CA1 neurons, and binds to the GABA(A)-benzodiazepine receptors[1][2].

HY-B0548AS2

Hydroxyzine-d8 dihydrochloride
Hydroxyzine-d₈ (dihydrochloride) is the deuterium labeled Hydroxyzine dihydrochloride. Hydroxyzine dihydrochloride, a benzodiazepine antihistamine agent, acts as a orally active histamine H1-receptor and serotonin antagonist. Hydroxyzine dihydrochloride has anxiolytic effect and can be used forthe research of generalised anxiety disorder[1][2].

HY-16579AS2

Etifoxine-d5
Etifoxine-d₅ is the deuterium labeled Etifoxine. Etifoxine, a non-benzodiazepine GABAergic compound, is a positive allosteric modulator of α1β2γ2 and α1β3γ2 subunit-containing GABAA receptors. Etifoxine reveals anxiolytic and anticonvulsant properties in rodents[1][2][3].

Cat. No.	Product Name		Classification

HY-103476

Ro15-4513		Azide
Ro15-4513, imidazobenzodiazepinone derivative, is a partial inverse agonist of benzodiazepine receptor (BZR) . Ro15-4513 is a potent ethanol antagonist . Ro15-4513 has anti-anxiety effect . Ro15-4513 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.

HY-123249

HZ166		Alkynes
HZ166 is a GABAA receptor subtype-selective benzodiazepine site agonist with preferential activity at α2- and α3-GABAA receptors. HZ166 shows anti-hyperalgesic effects . HZ166 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

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benzodiazepine receptors

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