sedative

Pheniramine maleate (Trimetose), an alkylamine derivative with antihistaminic and vasodilatory properties, binds to histamine H1 receptors, thereby inhibiting phospholipase A2 and production of the endothelium-derived relaxing factor, nitric oxide.

Clomethiazole (Distraneurin) is an orally active GABAA agonist and it is an anticonvulsant agent. It also has the potential for treating convulsive status epilepticus. Chlormethiazole inhibits cytochrome P450 isoforms: CYP2A6 and CYP2E1 in human liver microsomes.

(E)-3,4,5-Trimethoxycinnamic acid (O-Methylsinapic acid) is a natural compound derived from the roots and rhizomes of Notopterygium incisum.

1. Skimmianine (Chloroxylonine) is a spasmolytic agent. 2. Skimmianine (Chloroxylonine) shows pharmacol. props. similar to 2-(Methylamino)-1-phenyl-1-propanol BCJ45-G.

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.

(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.

Guaiapate has an antitussive and sedative effect.

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

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.

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

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.

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

Clopipazan is an antipsychotic and antidepressant compound.Clopipazan has sedative and anxiolytic activity, possibly due to selective GABergic blockade of certain interneurons.

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

Hydroxyzine Pamoate (Bobsule) is a histamine H1 receptor antagonist that is effective in the treatment of chronic urticaria, dermatitis, and histamine-mediated pruritus. Unlike its major metabolite CETIRIZINE, it does cause drowsiness. It is also effective as an antiemetic, for relief of anxiety and tension, and as a sedative.

Clemastine fumarate (Meclastine (fumarate)) is a synthetic ethanolamine with anticholinergic, sedative, and histamine H1 antagonistic properties.

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

Chlorobutanol (Chlortran) is a chemical preservative, sedative hypnotic and weak local anaesthetic. It has Antibacterial and Antifungal properties. Chlorobutanol is typically used at a concentration of 0.5% where it lends long-term stability to multi-ingredient formulations.

Phenytoin (5,5-Diphenylhydantoin) is a hydantoin derivative and a non-sedative antiepileptic agent with anticonvulsant activity. It potentially acts by promoting sodium efflux from neurons in the motor cortex, reducing post-tetanic potentiation at synapses. This prevents cortical seizure foci from spreading to adjacent areas and stabilizes the threshold against hyperexcitability. Additionally, it appears to reduce muscle spindle sensitivity to stretch, causing muscle relaxation.

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.

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.

Tripelennamine hydrochloride (Pyribenzamine hydrochloride) is a histamine H1 antagonist with low sedative action but frequent gastrointestinal irritation.

Pizotifen (Pizotyline) is a strong serotonin and tryptamine antagonist, with weak anticholinergic, anti-histaminic and anti-kinin effects. It also possesses sedative and appetite-stimulating properties. Pizotifen hydrochloride is an active ingredient in Sandomigran, which is used for the prophylactic management of migraine. Sandomigran is available in number of countries excluding the United States.