sedative

Anxiolytic/nonsedative agent-1 (TCS 1205) is a potent and selective GABAA agonist. Anxiolytic/nonsedative agent-1 shows appreciable affinity for the BzR in bovine brain membranes with Kis of 14, 121, 239 nM for α1β2γ2, α2β2γ2, α5β3γ2, respectively. Anxiolytic/nonsedative agent-1 shows α2 selective efficacy in vitro and anxioselective effects in vivo.

Nerolidol (Peruviol) shows sedative effects in animals, oxidative process plays a crucial role on neuronal pathological consequence. Nerolidol is mainly related to ROS and DNA single strand breaks generated by the presence of oxidative lesions.

Alloepipregnanolone is a pregnane with anesthetic, hypnotic, and sedative properties.

3,5-Dimethoxytoluene (Orcinol dimethyl ether), the main fragrance component in roses, has a sedative effect and can be used as a pest attractant.

Vapitadine is a non-sedative antihistamine compound that relieves itching caused by atopic dermatitis.

2'MeO6MF is a brain-penetrant positive allosteric modulator at α2β1γ2L and all α1-containing GABAA receptors.It offers neuroprotection and improved functional recovery and dampens the stroke-induced inflammatory response. 2'MeO6MF has anxiolytic and sedative effects.

Pazinaclone is a non-benzodiazepine (GABAA) partial agonist with sedative and anxiolytic activity.

Suriclone (RP 31264) is a selective cyclic pyrrolidone analog with sedative and anxiolytic activity, but not significant sedative effects.Suriclone shows its effects by modulating GABA-A receptors.

Fluanisone (Haloanison) is a butyrophenone derivative with sedative properties. It is a typical antipsychotic and is used in the treatment of schizophrenia.

Guaiapate has an antitussive and sedative effect.

Ceruletide Ammonium Salt is a decapeptide, originating from the skin of tropical frogs, which is a potent cholecystokinin receptor agonist and a safe and effective cholecystokinin receptor agonist with direct spasmodic effects on the gallbladder muscle and bile ducts. Ceruletide Ammonium Salt has sedative activity and has been used in the study of chronic schizophrenia.Ceruletide Ammonium Salt is a decapeptide, originating from the skin of tropical frogs.

(Z)-Tenilapine is trans-Tenilapine, cis-Tenilapine has sedative activity.

(E)-Crotylbarbital (Kalypnon), an isomer of Crotylbarbital, is a barbiturate derivative that has sedative, hypnotic, and anticonvulsant effects. (E)-Crotylbarbital can be used in studies to promote mental stability and sleep.

4,4-dimethyl-2,3,4,5-tetrahydro-1H-1,5-benzodiazepin-2-one is a benzodiazepine derivative. It is an orthosteric modulator of the GABAA receptor and selectively binds to the benzodiazepine site of the GABAA receptor. It has anxiolytic, anticonvulsant and sedative activity.

Etoxybamide is a drug candidate for sedative (hypnotic).

Azaphen (Pipofezin hydrochloride) is the reuptake of serotonin inhibitor.with antidepressant action and has sedative effects, suggesting antihistamine activity.

Imidazenil is an modulator of GABA-A that blocks the sedative effects without lowering the convulsion threshold.

Lofendazam (Bu 1014) is a benzodiazepine derivative that has sedative and anxiolytic effects.

AZD 3043 (THRX 918661) is a variant modulator of the γ-aminobutyric acid type A receptor, a novel sedative-hypnotic and a potential short-acting anesthetic that produces hypnosis and EEG suppression in rats.AZD 3043 potentiates the γ-aminobutyric acid type A receptor and inhibits neuronal nicotinic acetylcholine receptors.

Alpidem (Ananxyl) is an anxiolytic drug from the imidazopyridine family. Alpidem does not produce sedative effects at normal doses, and is instead used specifically for the treatment of anxiety. Alpidem has nanomolar binding affinity for both the central benzodiaze

Schisantherin A (Wuweizi ester-A) is a dibenzocyclooctadiene lignan isolated from the fruit of Schisandra sphenanthera, has been used as an antitussive, tonic, and sedative agent.

1. Cinnamaldehyde (Cinnamic Aldehyde) has antipyretic activity. 2. Cinnamaldehyde is a sedative agent. 3. Cinnamaldehyde inhibits invasive capabilities of MDA-MB-435S cells was correlated with down-regulating the expression of miR-27a. 4. Cinnamaldehyde induces the generation of reactive oxygen species and exerts vasodilator and anticancer effects. 5. Cinnamaldehyde appears to be a promising candidate as an adjuvant in combination therapy with 5-fluorouracil (5-FU) and oxaliplatin (OXA), two chemotherapeutic agents used in CRC treatment. The possible mechanisms of its action may involve the regulation of drugmetabolizing genes. 6. Cinnamaldehyde plays a certain role in inhibiting the occurrence and progression of melanoma and its action mechanism may be manifested by inhibiting expression of VEGF and HIF-α, thus blood vessel simulation and formation of new blood vessels of melanoma cells, and growth of tumors accordingly.

Apigenin (NSC 83244) is an aromatic oil extracted from the flowers or leaves of the daisy-like plants. Extracts, oils and teas made from chamomile are used for its soothing qualities as a sedative, mild analgesic and sleep medication. Apigenin has not been implicated in causing serum enzyme elevations or clinically apparent liver injury.

Doxylamine Succinate is a pyridine derivate histamine H1 antagonist with pronounced sedative properties. Doxylamine succinate (Decapryn) competitively blocks the histamine H1 receptor and limits the typical allergic and anaphylactic responses, including bronchoconstriction, vasodilation, increased capillary permeability, and spasmodic contraction of the gastrointestinal smooth muscle, caused by actions of histamine on bronchial and gastrointestinal smooth muscles, and on capillaries. This drug also prevents histamine-induced pain and itching of the skin and mucous membranes.

Eudesmin shows antiinflammatory, neuritogenic, anticonvulsant and sedative effects, the mechanism of eudesmin may be related to up-regulation of GABAA and GAD65 expressions, and anti-apoptosis of neuron the in brain.50 microM (+)-eudesmin can induce neurite outgrowth and enhance nerve growth factor (NGF)-mediated neurite outgrowth from PC12 cells by stimulating up-stream MAPK, PKC and PKA pathways.

Valepotriate (Valtrate) fraction can have sedative effects and affect behavioral parameters related to recognition memory. Valepotriates, a new class of cytotoxic and antitumor agents, they are very potent cytotoxic agents for the HTC hepatoma cells. Valepotriates may have a potential anxiolytic effect on the psychic symptoms of anxiety.

Astemizole (Laridal) is a synthetic piperidinyl-benzimidazol derivative with antiallergic properties, acts as a reversible competitive inhibitor of histamine H1 receptors, with less anticholinergic effects compared to related agents. It is a long-acting, non-sedative antihistaminic used in the treatment of seasonal allergic rhinitis, asthma, allergic conjunctivitis, and chronic idiopathic urticaria.

(+)-Magnoflorine (Thalictrin) has sedative and anxiolytic effects, probably mediated by Magnoflorine through a GABAergic mechanism of action. Magnoflorine and Sinomenine have protective effects, are mediated by some mechanism other than prevention of micelle formation or protection of the erythrocyte membrane against osmotic imbalance.

Detomidine hydrochloride (MPV-253 AII) produce dose-dependent sedative and analgesic effects, mediatated by activation of α2 catecholamine receptors.

Niaprazine is a histamine H1-receptor antagonist with marked sedative properties. Niaprazine has antihistamine and antiserotonin activities and can be used for sleep disorder research[1][2]. Niaprazine exhibits a low affinity for the vesicular monoamine transporter and for D2, α2, β, H1 and mAch receptors. Niaprazine, particularly the (+)stereoisomer, has a higher affinity for α1 (Ki = 77 nM) and 5-HT2 (Ki = 25 nM) binding sites, but is poorly recognized by 5-HT1A and 5-HT1B binding sites[2]. Niaprazine (60 mg/kg; i.p.; once) treatment increases rat brain 5-hydroxyindole acetic acid (5-HIAA) concentrations 30 min after treatment, and reduced them at 3-8 hr after treatment. Niaprazine also produces a short-lasting depletion of rat brain noradrenaline (NA) and dopamine (DA)[3]. Animal Model: Male Sprague-Dawley rats (150-200 g)[3] [1]. D Scherman, et al. Molecular pharmacology of niaprazine. Prog Neuropsychopharmacol Biol Psychiatry. 1988;12(6):989-1001. [2]. P G Rossi, et al. Niaprazine in the treatment of autistic disorder. J Child Neurol. 1999 Aug;14(8):547-50. [3]. P E Keane, et al. The effect of niaprazine on the turnover of 5-hydroxytryptamine in the rat brain. Neuropharmacology. 1982 Feb;21(2):163-9.

Cipepofol (HSK3486) is a GABAA receptor agonist with sedative properties and protective effects in a variety of cardiovascular diseases.Cipepofol activates the Sirtuin1 (Sirt1)/Nrf2 pathway and induces apoptosis in cardiomyocytes, and can be used to study myocardial infarction, myocardial ischemia/reperfusion injury, and octopus pot syndrome.

Tokinolide B may have sedative and spasmolytic properties.

Beclamide (Chlorakon) (N-benzyl-B-chloropropionamide) is a drug that possesses anticonvulsant activity. It is no longer used. It has been used as a sedative and as an anticonvulsant. It was studied in the 1950s for its anticonvulsant properties, as a treatment for generalized tonic-clonic seizures. It was not effective for absence seizures.

4’-hydroxy Trazodone is a metabolite of the antidepressant and sedative trazodone.1It is an inhibitor of organic anion transporter 3 (OAT3; Ki= 16.9 μM) and is selective for OAT3 over OAT1 (Ki= >200 μM).2 1.Yamato, C., Takahashi, T., Fujita, T., et al.Studies on metabolism of trazodone, II. Metabolic fate after intravenous administration and effects on liver microsomal drug-metabolizing enzymes in ratsXenobiotica4(12)765-777(1974) 2.Zou, L., Matsson, P., Stecula, A., et al.Drug metabolites potently inhibit renal organic anion transporters, OAT1 and OAT3J. Pharm. Sci.110(1)347-353(2021)

Chlormethiazole hydrochloride is an anticonvulsant and sedative. It also has neuroprotective.

Pregnanolone is a cell membrane modulator potentially for the treatment of pain. Pregnanolone is an endogenous neurosteroid that is biosynthesized from progesterone. It is a positive allosteric modulator of the GABAA receptor, as well as a negative allost

Scoparinol has sedative, anti-inflammatory, analgesic, and diuretic actions.

Juncusol shows anxiolytic and sedative activities, it shows anxiolytic activity at dosages of 10 mg/kg; it can induce caspase-3-mediated cytotoxicity in HT22 cells. Juncusol has anti-microbial activity, it shows significant activity against MRSA strains.

Epipregnanolone is an endogenous neurosteroid with hypnotic and sedative effects.

(R)-Thalidomide is the R-enantiomer of Thalidomide, has sedative properties.

Bromisoval (Isobromyl) is a mild hypnotic and sedative with potential toxicity.

Galphimine B is a cyclodesiccated triterpenoid from Galphimia Glauca, which can regulate the synaptic transmission of dopaminergic ventral tegmental neurons and has a sedative effect.

Brompheniramine maleate (Dimotane) is an antagonist against histamine H1 receptors.

Tacitin (Benzoctamine Hydrochloride) shows sedative and anti-anxiety properties. Tacitin blocks the central postsynaptic serotonin receptors.

Acebrochol is a neuroactive steroid. It may act as a sedative and hypnotic, by the mechanism of altering ligand-gated ion channels and cell surface receptors.

NCS-382 (sodium) is a potent antagonist of the GABA receptor, exhibiting anti-sedative and anti-hypnotic properties, with applications in neurological disease research [1].

Diproqualone, analogous to methaqualone, exhibits sedative, anxiolytic, anti-inflammatory, and analgesic properties [1].

Cinolazepam is a benzodiazepine derivative drug.It has a powerful sedative effect, so it is mainly used as a hypnotic.

Chelidonic acid (Jervaic acid) is a component of Chelidonium majus L., used as a mild analgesic, an antimicrobial, an acentral nervous system sedative. Chelidonic acid (Jervaic acid) also shows anti-inflammatory activity.

Taglutimide is a sedative-hypnotic derivative of glutarimide.

Ceruletide Ammonium acetate (FI-6934 Ammonium acetate) is a cholecystokinin (CCK) receptor agonist. Ceruletide Ammonium acetate is a safe and effective cholecystokinetic agent and small bowel and exocrine pancreatic stimulant.

Ceruletide (Caerulein) is a potent agonist of cholecystokinin receptor and it also is a safe and effective cholecystokinetic agent. It has a direct spasmogenic effect on the gallbladder muscle and bile ducts.