histamine H1 receptors: nootropics and compounds | sci-wiki

Cyproheptadine

Cyproheptadine is a first-generation antihistamine that also has strong antiserotonergic activity, along with anticholinergic and appetite-stimulating effects. Long marketed under the brand name Periactin, it is used to treat allergic conditions and is also employed to stimulate appetite and promote weight gain, to prevent migraines, and as an antidote for serotonin syndrome. Chemically it is a tricyclic piperidine compound, and it was approved for medical use in the early 1960s.

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Antihistamine

Hydroxyzine

Hydroxyzine is a first-generation antihistamine of the piperazine class, one of the oldest antihistamines still in wide use. Because it blocks histamine H1 receptors and readily enters the brain, it serves both for allergic itching and hives and as a sedating anti-anxiety medication and pre-procedure premedication. It is sold under brand names such as Atarax and Vistaril, and the body converts part of it into cetirizine, itself a well-known antihistamine.

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Antihistamine

Ketotifen

Ketotifen is an antihistamine and mast cell stabilizer used to treat allergic conditions. As eye drops it relieves the itching of allergic conjunctivitis, and taken by mouth it is used to prevent the symptoms of asthma and other allergic disorders [1][3]. It combines two actions in one molecule, blocking the H1 histamine receptor and stabilizing mast cells so that they release fewer inflammatory chemicals [1][4].

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Antihistamine

Promethazine

Promethazine is a first-generation antihistamine of the phenothiazine family, used for allergies, nausea and vomiting, motion sickness, and as a sedative. It blocks the histamine H1 receptor and also has anticholinergic and mild antidopaminergic effects, which give it strong sedating and anti-sickness properties. Introduced in the early 1950s and sold under names such as Phenergan, it is a widely used generic, although it carries important safety warnings, including a caution against use in young children.

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Antipsychotic

Quetiapine

Quetiapine is an atypical, or second-generation, antipsychotic used to treat schizophrenia, bipolar disorder, and, as an add-on, major depression. Its effects are strongly shaped by dose and by its active metabolite norquetiapine, which inhibits the norepinephrine transporter and modulates several serotonin receptors, giving quetiapine genuine antidepressant activity; at low doses its dominant action is sedating H1-antihistamine blockade with little dopamine occupancy, while antipsychotic dopamine blockade emerges only at higher doses. Marketed originally as Seroquel and now generic, it is on the World Health Organization list of essential medicines and is also widely, though generally discouraged, prescribed off-label as a sedative for insomnia.

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