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Results for "

Insomnia

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (4) Cytochrome P450 (1) Drug Metabolite (1) Endogenous Metabolite (2) GABA Receptor (4) Histamine Receptor (4) iGluR (2) Isotope-Labeled Compounds (1) Melatonin Receptor (4) Neurokinin Receptor (1) Orexin Receptor (OX Receptor) (10) Tryptophan Hydroxylase (1)
By Research Areas:	Cancer (4) Endocrinology (6) Inflammation/Immunology (2) Metabolic Disease (1) Neurological Disease (26)

Inhibitors & Agonists

Screening Libraries

Natural
Products

Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-152843

Fazamorexant YZJ-1139	Orexin Receptor (OX Receptor)	Neurological Disease
Fazamorexant (YZJ-1139) is a potent orexin receptor antagonist. Fazamorexant can be used for insomnia research .

HY-106246

Pruvanserin EMD 281014 free acid; LY 2422347	5-HT Receptor	Neurological Disease Metabolic Disease
Pruvanserin (EMD 281014 free acid) is a selective 5-HT2A receptor antagonist. Pruvanserin alleviates tactile allodynia in diabetic rats. Pruvanserin can also be used for research of insomnia .

HY-135359

RP 48497	Drug Metabolite	Neurological Disease
RP 48497, an impurity of Eszopiclone, is a photodegradation product of Eszopiclone. Eszopiclone is a non-benzodiazepine agent used in the treatment of insomnia .

HY-136922

Orexin receptor antagonist 2	Orexin Receptor (OX Receptor)	Neurological Disease
Orexin receptor antagonist 2 (compound 30) is a potent orexin receptor antagonist with pK_is of 7.69 and 9.78. Orexin receptor antagonist 2 has the potential for the research of insomnia .

HY-A0014

Ramelteon Maximum Cited Publications 7 Publications Verification TAK-375	Melatonin Receptor	Neurological Disease Endocrinology Cancer
Ramelteon is a potent, highly selective, and orally active agonist of MT1/MT2 with Ki values of 14 and 112 pM, respectively. Ramelteon has the potential for the research of insomnia. Ramelteon consistently reduces sleep onset after long-term treatment, with no next-morning residual effects or rebound insomnia or withdrawal symptoms upon discontinuation .

HY-101260

DORA-22	Orexin Receptor (OX Receptor)	Neurological Disease
DORA-22 is an orally active dual orexinergic receptor antagonist, and improves the sleep disruption and memory impairment. DORA-22 can be used for study of insomnia .

HY-123737

MK-8133	Orexin Receptor (OX Receptor)	Neurological Disease
MK-8133 is an orexin-2 receptor antagonist. MK-8133 can be used in the study of insomnia .

HY-115139

Fenadiazole	Others	Neurological Disease
Fenadiazole acts as a central nervous system agent to manage insomnia and dreaminess .

HY-U00051

Propiomazine	Histamine Receptor	Neurological Disease
Propiomazine is an orally active antihistamine agent with sedative effects. Propiomazine can be used in the research of insomnia .

HY-U00051A

Propiomazine hydrochloride	Histamine Receptor
Propiomazine hydrochloride is an orally active antihistamine agent with sedative effects. Propiomazine hydrochloride can be used in the research of insomnia .

HY-A0014R

Ramelteon (Standard)	Melatonin Receptor	Neurological Disease Endocrinology Cancer
Ramelteon (Standard) is the analytical standard of Ramelteon. This product is intended for research and analytical applications. Ramelteon is a potent, highly selective, and orally active agonist of MT1/MT2 with Ki values of 14 and 112 pM, respectively. Ramelteon has the potential for the research of insomnia. Ramelteon consistently reduces sleep onset after long-term treatment, with no next-morning residual effects or rebound insomnia or withdrawal symptoms upon discontinuation .

HY-139559

Vornorexant ORN-0829; TS-142	Orexin Receptor (OX Receptor)	Neurological Disease
Vornorexant (ORN-0829; TS-142) is a potent dual OX1R and OX2R antagonist with IC50 values of 1.05 nM and 1.27 nM, respectively. Vornorexant exhibits potent sleep-promoting effects in vivo and can be used for insomnia research research.

HY-19914

MK-1064 2 Publications Verification	Orexin Receptor (OX Receptor)	Endocrinology Cancer
MK-1064 is a selective and orally active OX₂R antagonist (K_i: 0.5 nM, IC₅₀: 18 nM). MK-1064 promotes sleep in vivo. MK-1064 can be used in the research of insomnia .

HY-113555

DORA 42	Orexin Receptor (OX Receptor)	Neurological Disease
DORA 42 is a dual orexin 1 and orexin 2 receptor antagonist with sleep efficacy in rats. DORA 42 is promising for research of insomnia .

HY-101834

ACT-462206	Orexin Receptor (OX Receptor)	Others
ACT-462206 is an orally active and potent dual Orexin 1/Orexin 2 receptor antagonist with IC₅₀s of 60 nM (Orexin 1) and 11 nM (Orexin 2), respectively. ACT-462206 exhibits brain penetration properties, and can be used for insomnia, stress/anxiety-related disorders and addiction research .

HY-101629

(E)-Crotylbarbital	Others	Neurological Disease
(E)-Crotylbarbital is the isomer of Crotylbarbital. Crotylbarbital is a barbiturate derivative and can be used for the research of insomnia.

HY-N0659

Jujuboside A 3 Publications Verification	GABA Receptor	Neurological Disease
Jujuboside A is a glycoside extracted from Semen Ziziphi Spinosae, a Chinese herbal medicine used to treat insomnia and anxiety.

HY-A0014S

Ramelteon-d5 TAK-375-d₅	Isotope-Labeled Compounds Melatonin Receptor	Neurological Disease Endocrinology Cancer
Ramelteon-d₅ is deuterium labeled Ramelteon. Ramelteon is a potent, highly selective, and orally active agonist of MT1/MT2 with Ki values of 14 and 112 pM, respectively. Ramelteon has the potential for the research of insomnia. Ramelteon consistently reduces sleep onset after long-term treatment, with no next-morning residual effects or rebound insomnia or withdrawal symptoms upon discontinuation[1][2].

HY-12140

Vestipitant GW597599	Neurokinin Receptor	Neurological Disease
Vestipitant (GW597599) is a neurokinin-1 receptor antagonist (pKi: 9.4, hNK1) with hypnotic effects and the ability to suppress primary insomnia. Vestipitant can effectively block substance P-mediated extracellular regulated kinase phosphorylation and relieve anxiety and possible depression induced by the agonist GR73632 (HY-P1192) in gerbils. Vestipitant can also improve functional dyspnea, anxiety, insomnia, irritable bowel disease, gastroesophageal reflux disease, tinnitus and antiemetic effects .

HY-101456

PCPA methyl ester hydrochloride 2 Publications Verification 4-Chloro-DL-phenylalanine methyl ester hydrochloride	Tryptophan Hydroxylase 5-HT Receptor	Neurological Disease
PCPA methyl ester hydrochloride (4-Chloro-DL-phenylalanine methyl ester hydrochloride), a reversible tryptophan hydroxylase inhibitor, is a serotonin (5-HT) synthesis inhibitor. PCPA methyl ester hydrochloride crosses the blood brain barrier and reduces 5-HT central availability .

HY-103522

AA29504	GABA Receptor	Neurological Disease
AA29504 is a ethyl carbamate with γ-aminobutyric acid (GABA_A(HY-L120) receptor activity. AA29504 inhibits the delivery of the neurotransmitter gamma-aminobutyric acid in the central nervous system. AA29504 can be used to research anxiety, insomnia and other neuropsychiatric diseases .

HY-129105

Clomethiazole 2 Publications Verification	GABA Receptor Cytochrome P450	Neurological Disease
Chlormethiazole is an potent and orally active GABA_A agonist . Chlormethiazole inhibits cytochrome P450 isoforms: CYP2A6 and CYP2E1 in human liver microsomes. Chlormethiazole is an anticonvulsant agent and has the potential for treating convulsive status epilepticus .

HY-16505

Triclofos sodium	Others	Neurological Disease
Triclofos sodium is a drug used to suppress insomnia and for sedation and has sedative activity. Triclofos sodium is used in children for sedation during painless medical procedures, particularly in children with neurocognitive disorders. Triclofos sodium has similar physiological and pharmacological properties to chloral and therefore can be used as a substitute when necessary. The safety and efficacy of Triclofos sodium have been demonstrated in pediatric populations with high rates of neurocognitive disorders .

HY-109012

Seltorexant 1 Publications Verification JNJ-42847922	Orexin Receptor (OX Receptor)	Neurological Disease Endocrinology
Seltorexant (JNJ-42847922) is an orally active, high-affinity, and selective orexin-2 receptor (OX2R) antagonist (pK_i values of 8.0 and 8.1 for human and rat OX2R). Seltorexant (JNJ-42847922) crosses the blood-brain barrier and quickly occupies OX2R binding sites in the rat brain .

HY-109012A

Seltorexant hydrochloride 1 Publications Verification JNJ-42847922 hydrochloride	Orexin Receptor (OX Receptor)	Neurological Disease Endocrinology
Seltorexant hydrochloride (JNJ-42847922 hydrochloride) is an orally active, high-affinity, and selective OX2R antagonist (pK_i values of 8.0 and 8.1 for human and rat OX2R). Seltorexant hydrochloride crosses the blood-brain barrier and quickly occupies OX2R binding sites in the rat brain .

HY-106136

TIK-301 PD-6735; LY-156735	Melatonin Receptor 5-HT Receptor	Neurological Disease
TIK-301 (PD-6735) is a chlorinated melatonin derivative and a potent, high-affinity and orally active melatonin MT₁ and MT₂ receptors agonist with K_is of 0.081 nM and 0.042 nM, respectively. TIK-301 is also a 5-HT_2B/5-HT_2C receptors antagonist with antidepressant action. TIK-301 has the potential for sleep disorders and other circadian rhythm disorders treatment .

HY-138110

Toladryl 4-Methyldiphenhydramine	Endogenous Metabolite iGluR Histamine Receptor	Neurological Disease Inflammation/Immunology
Toladryl is a derivative of Diphenhydramine (HY-B0303), capable of penetrating the blood-brain barrier and possessing oral activity, as well as antihistamine and anticholinergic activities. The anticholinergic activity of Toladryl is approximately one-tenth that of Diphenhydramine (HY-B0303), and its protective effect against lethal doses of histamine in guinea pigs is 2 to 4 times that of Diphenhydramine (HY-B0303). The side effects of Toladryl are fewer and milder than those of Diphenhydramine (HY-B0303), but at higher doses, it may cause central nervous system symptoms such as insomnia, agitation, and disorientation. Toladryl can be used for research in allergic diseases .

HY-W050162

(E)-3,4,5-Trimethoxycinnamic acid TMCA	GABA Receptor 5-HT Receptor	Neurological Disease
(E)-3,4,5-Trimethoxycinnamic acid (TMCA) is a cinnamic acid substituted by multi-methoxy groups. (E)-3,4,5-Trimethoxycinnamic acid is an orally active and potent GABA_A/BZ receptor agonist. (E)-3,4,5-Trimethoxycinnamic exhibits favourable binding affinity to 5-HT_2C and 5-HT_1A receptor, with IC₅₀ values of 2.5 and 7.6 μM, respectively. (E)-3,4,5-Trimethoxycinnamic acid shows anticonvulsant and sedative activity. (E)-3,4,5-Trimethoxycinnamic acid can be used for the research of insomnia, headache and epilepsy .

HY-138110R

Toladryl (Standard)	Endogenous Metabolite iGluR Histamine Receptor	Neurological Disease Inflammation/Immunology
Toladryl (Standard) is the analytical standard of Toladryl. This product is intended for research and analytical applications. Toladryl is a derivative of Diphenhydramine (HY-B0303), capable of penetrating the blood-brain barrier and possessing oral activity, as well as antihistamine and anticholinergic activities. The anticholinergic activity of Toladryl is approximately one-tenth that of Diphenhydramine (HY-B0303), and its protective effect against lethal doses of histamine in guinea pigs is 2 to 4 times that of Diphenhydramine (HY-B0303). The side effects of Toladryl are fewer and milder than those of Diphenhydramine (HY-B0303), but at higher doses, it may cause central nervous system symptoms such as insomnia, agitation, and disorientation. Toladryl can be used for research in allergic diseases .

Cat. No.	Product Name

HY-L120

GABA Receptor Compound Library	150 compounds
GABA receptors are a class of receptors that respond to the neurotransmitter gamma-aminobutyric acid (GABA), the chief inhibitory neurotransmitter in the vertebrate central nervous system. There are two classes of GABA receptors: GABAA and GABAB. GABAA receptors are ligand-gated ion channels (also known as ionotropic receptors), whereas GABAB receptors are G protein-coupled receptors (also known asmetabotropic receptors). GABA receptors are significant drug targets in the treatment of neuropsychiatric disorders such as epilepsy, insomnia, and anxiety, as well as in anesthesia in surgical operations. MCE offers a unique collection of 150 GABA receptors inhibitors and activators, which is an efficient tool for neuropsychiatric disorders drugs discovery.

GABA Receptor Compound Library

150 compounds

GABA receptors are a class of receptors that respond to the neurotransmitter gamma-aminobutyric acid (GABA), the chief inhibitory neurotransmitter in the vertebrate central nervous system. There are two classes of GABA receptors: GABAA and GABAB. GABAA receptors are ligand-gated ion channels (also known as ionotropic receptors), whereas GABAB receptors are G protein-coupled receptors (also known asmetabotropic receptors). GABA receptors are significant drug targets in the treatment of neuropsychiatric disorders such as epilepsy, insomnia, and anxiety, as well as in anesthesia in surgical operations.

MCE offers a unique collection of 150 GABA receptors inhibitors and activators, which is an efficient tool for neuropsychiatric disorders drugs discovery.

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N0659

Jujuboside A 3 Publications Verification	Triterpenes Structural Classification Terpenoids Ziziphus jujuba Mill. var. spinosa (Bunge) Hu ex H.F.Chow. Source classification Plants Rhamnaceae	GABA Receptor
Jujuboside A is a glycoside extracted from Semen Ziziphi Spinosae, a Chinese herbal medicine used to treat insomnia and anxiety.

Cat. No.	Product Name	Chemical Structure

HY-A0014S

Ramelteon-d5
Ramelteon-d₅ is deuterium labeled Ramelteon. Ramelteon is a potent, highly selective, and orally active agonist of MT1/MT2 with Ki values of 14 and 112 pM, respectively. Ramelteon has the potential for the research of insomnia. Ramelteon consistently reduces sleep onset after long-term treatment, with no next-morning residual effects or rebound insomnia or withdrawal symptoms upon discontinuation[1][2].

Ramelteon-d5

Ramelteon-d₅ is deuterium labeled Ramelteon. Ramelteon is a potent, highly selective, and orally active agonist of MT1/MT2 with Ki values of 14 and 112 pM, respectively. Ramelteon has the potential for the research of insomnia. Ramelteon consistently reduces sleep onset after long-term treatment, with no next-morning residual effects or rebound insomnia or withdrawal symptoms upon discontinuation[1][2].

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