hypersensitivity

Thonzylamine (neohetramine) is an antihistamine and anticholinergic drug. It is available as combination products with Clofedanol or Phenylephrine for temporary relief of symptoms of common cold, hay fever (allergic rhinitis) or other upper respiratory allergies.

Oxatomide (Oxatomida) is a potent and orally active dual H1 histamine receptor and P2X7 receptor antagonist with antihistamine and antiallergic activity.Oxatomide can be used to block ATP-induced currents in the human P2X7 receptor with an IC50 value of 0.95 μM.Oxatomide has an inhibitory effect on ATP-induced Ca2+ inward currents with an IC50 value of 0.43 μM.Oxatomide inhibits 5-hydroxytryptamine. Oxatomide inhibits 5-hydroxytryptamine with an IC50 of 0.43 μM.Oxatomide is used in the treatment of immune system diseases and in the study of hypersensitivity reactions.

Dimiracetam (NT-11624) is an orally active anti-neuropathy compound that inhibits hypersensitivity and neurological alterations and may be used in the study of cognitive disorders, depression and neuropathic pain.

Docetaxel trihydrate (RP-56976 Trihydrate) is an antineoplastic agent that has a unique mechanism of action as an inhibitor of cellular mitosis and that currently plays a central role in the therapy of many solid tumor including breast and lung cancer. Therapy with docetaxel has been associated with a low rate of serum enzyme elevations and rarely to instances of acute hepatic necrosis generally due to severe hypersensitivity reactions or sepsis.

Diphenhydramine hydrochloride (DPH) is a histamine H1 antagonist used as an antitussive and antiemetic. It is also used for pruritus and dermatoses, for hypersensitivity reactions, as an antiparkinson, a hypnotic, and as an ingredient in common cold preparations.

Quinine is a natural cinchona alkaloid that has been used for centuries in the prevention and therapy of malaria. Quinine is also used for idiopathic muscle cramps. Quinine therapy has been associated with rare instances of hypersensitivity reactions which can be accompanied by hepatitis and mild jaundice.

N,N'-Diacetyl-L-cystine (DiNAC) is the disulphide dimer of N-acetylcysteine with immunomodulating properties. N,N'-diacetyl-L-cystine also has antiatherosclerotic effects in Watanabe-heritable hyperlipidemic rabbit (WHHL) rabbits. N,N'-diacetyl-L-cystine is also an effective and orally active modulator of contact sensitivity delayed-type hypersensitivity reactions in rodents.

Adenosine A1 receptor activator T62 is an allosteric enhancer of the adenosine A1 receptor, producing antinociception in animal models of acute pain and reducing hypersensitivity in models of inflammatory and nerve-injury pain[1][2][3].

AB21 HCl is a selective antagonist of the σ1 receptor, with Kis of 13 nM for σ1 receptor and 102 nM for σ2 receptor. AB21 HCl is known for its ability to reduce mechanical hypersensitivity.

Cyclo(L-Pro-L-Ile) is a bis-ketopiperazine from Bacillus thuringiensis that induces a moderate hypersensitivity reaction and can be used to study pine wilt.

CLP257 is a selective K+-Cl− cotransporter KCC2 activator (EC50: 616 nM) and it is inactive against NKCC1, GABAA receptors, KCC1, KCC3 or KCC4. CLP257 alleviates hypersensitivity in rats with neuropathic painc and it also modulates plasmalemmal KCC2 protein turnover post-translationally. CLP257 restores impaired Cl− transport in neurons with diminished KCC2 activity.

Delgocitinib (JTE-052) is a specific JAK (Janus kinase) inhibitor with IC50 values of 2.8, 2.6, 13, and 58 nM for JAK1, JAK2, JAK3, and Tyk2 respectively. Delgocitinib is involved in various inflammatory and autoimmune diseases through JAK-dependent cytokines and can effectively suppress multiple cytokine signaling while inhibiting itching caused by cytokines. It is widely used to treat various inflammatory diseases, including autoimmune diseases and hypersensitivity reactions.

Draflazine is an ENT1 inhibitor. It completely reverses the hypersensitivity in the complete Freund's adjuvant (CFA) model of mechanical hyperalgesia. Draflazine also completely reverses the hypersensitivity of the carrageenan inflammation model of therma

Eact is a selective and potent TMEM16A activator that directly activates the TRPV1 channels in sensory nociceptors, thereby producing itch, acute nociception, and thermal hypersensitivity (brackets).

PD 173212 is a blocker that blocks N-type voltage sensitive calcium channel (Cav2.2). PD173212 (0.0017-1.7 μmol kg, Intraperitoneal Injection.) dose-dependently reduced DNBS-induced visceral hypersensitivity in mice.

TGR5 is a potent TGR5(GPCR19) agonist.

Sulfamethoxazole-NO (SMX-NO) is a SMX-NO derivative that is a major immunogen for sulfonamide hypersensitivity reactions, is cytotoxic, and is immunogenic in rodents.

PD-217014 is an α2δ ligand that exhibits visceral analgesic activity and can suppress visceral hypersensitivity. Its antihyperalgesic effects are dose-dependent.

LY-266097, a selective 5-HT2BR antagonist, effectively reduces tactile hypersensitivity and demonstrates potential therapeutic effects in alleviating pain caused by nerve injury. Additionally, it decreases the upregulation of 5-HT2B receptors in the dorsal root ganglia and spinal cord following nerve damage. Research indicates that LY-266097 may play a potential role in the development of neuropathic pain pathways.

Loxanast is an inhibitor employed in animal models to suppress delayed-type hypersensitivity reactions. It effectively inhibits the chemotactic activity of macrophages.

UKH-1114 is a potent σ2 receptor Tmem97 agonist with a Ki value of 46 nM, demonstrating antinociceptive effects against mechanical hypersensitivity. This compound alleviates mechanical hypersensitivity in mice caused by nerve injury without inducing motor impairment and is a promising candidate for neuropathic pain research.

Phaseolin, a protein from red kidney bean (Phaseolus vulgaris L.), plays a pivotal role in hypersensitivity induction.

Dimethindene maleate (SU 6518) is a histamine H1 antagonist and can be used in studies about the treatment of hypersensitivity reactions, pruritus and rhinitis.

TC-SP 14, also known as compound 14, is a highly active and potent S1P1 agonist with oral bioavailability. It exhibits an EC50 value of 0.042 μM, indicating its strong binding affinity to the S1P1 receptor. Notably, its interaction with the S1P3 receptor is minimal, as evidenced by an EC50 value of 3.47 μM. TC-SP 14 demonstrates significant pharmacological effects, including a marked reduction in blood lymphocyte counts and the attenuation of delayed type hypersensitivity response to antigen challenge [1].