Mizolastine (Mizollen) is a long-acting H1 -antihistamine indicated for the symptomatic relief of seasonal allergic rhinoconjunctivitis (hay fever), perennial allergic rhinoconjunctivitis and urticaria. It blocks H1 receptors and is commonly fast-acting. It does not prevent the actual release of histamine from mast cells, just prevents it binding to receptors. Side effects can include dry mouth and throat

Pimethixene is an antihistamine exerting sedative and antitussive properties. Pimethixene displayed high affinity to serotonin 5-HT2A and 2B, histamine H1 and muscarinic acetylcholine M2 receptors. Oral pimethixene used to calm dry cough and irritation coughs in children.

Bamipine (trade name Soventol) is a sedating antihistamine with pronounced sedative effects. Bamipine is a pharmaceutical drug acting as an H1 antihistamine with anticholinergic properties. It is used as an antipruritic ointment. Bamipine hydrochloride has been given by mouth. Bamipine, bamipine lactate, and bamipine salicylate have all been applied topically.

Histapyrrodine was investigated as a neuro-sedative drug for the treatment of anxiety and states of aggression.

Sequifenadine is H1- and 5HT-serotonine receptor antagonist. It has an anti-histamine effect, not only blocking histamine receptors, but also reducing the content of histamine in tissues by accelerating its destruction by diamine oxidase. Sequifenadine did not demonstrate any significant sedative effect. It has a pronounced and prolonged antipruritic and antiexudative effect. It is indicated for the treatment of allergic rhinitis and conjunctivitis, pollinosis, urticaria, angioedema, allergic pruritic dermatosis, including atopic dermatitis. Adverse effects are: dry mouth, pain in the epigastric region, dyspepsia, increased appetite, headache, sleepiness.

Promethazine hydroxyethyl quaternary derivative of promethazine with antihistamine and anticholinergic properties. The drug lacked the sedative properties of promethazine. It was used in the clinic under tradename Aprobit.

Ebastine is an antihistamine which blocks H1-receptors through its carboxylic acid metabolite. Ebastine is indicated for the treatment of allergic rhinitis and chronic idiopathic urticaria.

Deptropine citrate is a well-known H1-histamine receptor antagonist and muscarinic receptor antagonist. It is prescribed frequently for treatment of asthma, although there has been a sharp decrease in prescriptions since 1994. Deptropine is gradually being replaced by inhaled beta 2 adrenergic agonists and glucocorticosteroids as the preferred clinical prescription. Recently deptropine has garnered interest as a potential treatment for breast cancer. In vitro studies have shown deptropine citrate has inhibitory effects on cell viability and mammosphere formation in Breast Cancer Stem Cells (BCSCs). However, it does not seem to inhibit the self-renewal capacity of the breast cancer cell line MDA-MB-231 when it is enriched with Cancer Stem Cells.

Chloropyramine is an antagonist of H1 histamine receptors. It is indicated for the treatment of various forms of allergic reactions. Chloropyramine is a drug capable of (1) inhibiting the biochemical function of VEGFR-3 and FAK, (2) inhibiting proliferation of a diverse set of cancer cell types in vitro, and (3) reducing tumor growth in vivo.

Mebhydrolin (INN) or mebhydroline is a histamine H1-receptor antagonist. It is not available in the United States, but it is available in various other countries under the brand names Bexidal and Diazolin. It is used for symptomatic relief of allergic symptoms caused by histamine release, including nasal allergies and allergic dermatosis.