Laquinimod is a new orally available carboxamide derivative, which is currently developed for relapsing remitting (RR) and chronic progressive (CP) forms of multiple sclerosis (MS; RRMS or CPMS) as well as neurodegenerative diseases. The mechanism of action of laquinimod is not fully elucidated because the molecular target is not known. Treatment with laquinimod led to a significant and persistent increase in brain-derived neuroprotective factor (BDNF) serum levels compared to placebo treatment. In human studies, a decrease of pro-inflammatory and an increase of anti-inflammatory cytokines have been measured. After commercial launch the unexpected severe cardiac adverse events (AEs) such as serositis, pericarditis, and myocardial infarction were detected.

Mesulfen is a drug that was used for the treatment of seborrhea, seborrheic eczema and acne. Now the drug is presumably withdrawn from the market.

Arpromidine is a potent histamine H2-receptor agonist and weak NPY Y1 antagonist. In the isolated aperfused heart, arpromidine was more potent in increasing cardiac contractile force and coronary flow but less effective on heart rate and less arrhythmogenic. Arpromidine may be considered a new lead for the development of "cardiohistaminergics". In the arpromidine series the order of potency found in guinea-pig atria was in good agreement with the results from isolated perfused guinea-pig hearts. In particular, the two-fold halogenated arpromidine analogues proved to be more potent positive inotropic agents than impromidine with lower stimulating effects on heart rate and reduced arrhythmogenic properties.

Piprinhydrinate is compositon of Diphenylpyraline and 8-chloroteophylline. 8-Chlorotheophylline is a stimulant drug of the xanthine chemical class, with physiological effects similar to caffeine. Diphenylpyraline is an antihistamine that prevents, but does not reverse, responses mediated by histamine alone. Diphenylpyraline antagonizes most of the pharmacological effects of histamine, including urticaria and pruritus. Also, diphenylpyraline may exhibit anticholinergic actions (as do most of the antihistamines) and may thus provide a drying effect on the nasal mucosa. 8-Chlorotheophylline main use is in combination with Diphenylpyraline or diphenhydramine in the antiemetic Piprinhydrinate and dimenhydrinate. Diphenylpyraline (or diphenhydramine) reduces nausea but causes drowsiness, and the stimulant properties of 8-Chlorotheophylline help ward off that side-effect.

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

Zepastine is antihistamine antiallergic drug developed in the late 1960-s.

CP-20,961 [N,N-dioctadecyl-N',N'-bis (2-hydroxyethyl) propanediamine, or Avridine) is a non-immunogenic adjuvant, which was investigated as an antiviral drug with low acute toxicity in mice. This compound is able to stimulate nasal interferon and was studied in patients with rhinovirus, but the results had shown, that CP-20,961 had yielded both fairly good results and only fair or poor results. CP-20,961 is also used to induce arthritis in rodents.

Homochlorcyclizine (INN) is an antihistamine which has been marketed in Japan since 1965. It is used in the treatment of Itching sensation resulting from skin diseases (eczema or dermatitis, pruritus, drug eruption, toxic erythema and infant strophulus), urticaria and allergic rhinitis. Homochlorcyclizine hydrochloride possesses several pharmacological properties: 1) inhibits bradykinin-induced contractions of isolated guinea pig ileum; 2)partially blocks SRS-A (slow-reacting substance of anaphylaxis )- induced contractions in isolated guinea pig il eum. 3) Homochlorcyclizine hydrochloride completely inhibits histamine-induced contractions at a concentration of 0.1μg/mL, while it completely inhibits serotonin or acetylcholine- induced contractions at a concentration of 1μg/mL.

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.

Romurtide (Muroctasin) is a non-specific immune stimulant derived from muramyl dipeptide, which is obtained from gram-positive bacterial cell walls. Muroctasin stimulates macrophages, which release interleukin-l, which in turn increases production of colony-stimulating factors; muroctasin also evokes an increased production of neutrophils. It is used in Japan for chemotherapy-induced leukopenia.