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Restrict the search for
histamine
to a specific field?
Status:
Investigational
Source:
INN:fenethazine [INN]
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
FENETHAZINE was a first-generation phenothiazine-derived antihistamine drug. Promethazine was derived from FENETHAZINE.
Class (Stereo):
CHEMICAL (UNKNOWN)
Libecillide is a specific monovalent penicilloyl hapten inhibitor of allergic reactions to penicillin. A depression of skin hypersensitivity to PPL and/or penicillin and penicillin derivatives sometimes persisting for weeks and months was obvious in numerous allergic patients submitted to combined libecillide-penicillin treatment. A depressing effect on antipenicillin antibody titers detected by passive hemaglutination was also manifest in some patients. The overall tolerance of libecillide in allergic patients has been very good. Nevertheless, the major obstacle to a wider general use of libecillide at the present time appears to be the occurrence of positive skin reactions to that compound in approximately 5 percent of patients allergic to penicillin.
Status:
Investigational
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Cidoxepin is the cis-isomer of the widely prescribed tricyclic compound doxepin. Commercial preparations of the tricyclic anti-depressant doxepin contain 15% of the more active cis-doxepin and 85% of the trans-isomer. Elorac, Inc., a rapidly growing specialty pharmaceutical company focused on the treatment of dermatological disorders, is pleased to announce that it has acquired worldwide rights to the active agent Cidoxepin from Gideon Pharmaceuticals. Cidoxepin appears to be much more potent than doxepin while having less sedative and cholinergic side effects. Elorac plans to develop oral formulations of the drug to treat urticaria and topical formulations for treatment of atopic and contact dermatitis.
Status:
Investigational
Source:
JAN:QUINOTOLAST SODIUM [JAN]
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Quinotolast (also known as FK021) is an orally active mast cell stabilizer which has a cytoprotective effect on the gastric mucosa. Quinotolast was patented in 1985 by Japanese pharmaceutical company Fujisawa Pharmaceutical Co., Ltd. as an antiallergic and antiulcer agent. In preclinical models, Quinotolast potently inhibited such type I allergic reactions as passive cutaneous anaphylaxis (PCA) and anaphylactic bronchoconstriction in rats by both intravenous and oral dosing. Quinotolast inhibited histamine release from rat peritoneal cells, but it had no antagonistic effect on histamine-, serotonin-, platelet activating factor- or bradykinin-induced cutaneous reactions in rats. Moreover, it was clearly demonstrated that quinotolast and DSCG had a cross tachyphylaxis to inhibit PCA in rats, suggesting that these drugs, at least in part, share the same mechanism of action. Quinotolast caused a significant increase in the mucociliary transport rate in quails. Quinotolast significantly depressed the cough reflex induced by citric acid in normal and bronchitic guinea pigs.
Class (Stereo):
CHEMICAL (ACHIRAL)
Tesmilifene is a small-molecule antineoplastic drug and chemopotentiator that was under development by YM BioSciences for the treatment of breast cancer. Tesmilifene was developed as a selective ligand of the antiestrogen binding sites without estrogen receptor affinity. Tesmilifene potentiates the cytotoxicity of a variety of chemotherapy drugs in vitro and in vivo. Tesmilifene in combination with doxorubicin provides an unexpected and very large survival advantage over doxorubicin alone in a randomized trial in phase III clinical trial in advanced breast cancer. Unfortunately, Tesmilifene application associated with high rate disease and treatment-related adverse events and poor quality of life. Based on these results further development of Tesmilifene was discontinued
Status:
Investigational
Source:
INN:furethidine [INN]
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Furethidine, a pethidine analog was studied as an analgesic agent. This compound is not currently used in medicine and is listed in schedules of the single convention on narcotic drugs of 1961 as amended by the 1972 protocol.
Status:
Investigational
Source:
INN:esmirtazapine [INN]
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Esmirtazapine (S-(+)mirtazapine or ORG-50081) is an enantiomer of mirtazapine (REMERON®), a high-affinity antagonist at 5-HT2/5-HT3 and H1 receptors, used in the treatment of depression. Esmirtazapine has a shorter plasma half-life than the R(−) enantiomer. Esmirtazapine is preferentially metabolized into an 8-hydroxy glucuronide. Organon was developing esmirtazapine for the treatment of hot flushes (vasomotor symptoms) associated with the menopause and insomnia.
Status:
Investigational
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Conessine is a plant steroid alkaloid that acts as a potent and specific antagonist of histamine H3 receptors. Conessine displayed high affinity at both rat and human H3 receptors (pKi = 7.61 and 8.27) and generally high selectivity against other sites, including histamine receptors H1, H2, and H4. Conessine was found to efficiently penetrate the CNS and reach very high brain concentrations. Although the very slow CNS clearance and strong binding to adrenergic receptors discouraged focus on conessine itself for further development, its potency and novel steroid-based skeleton motivated further chemical investigation. Modification based on introducing diversity at the 3-nitrogen position generated a new series of H3 antagonists with higher in vitro potency, improved target selectivity, and more favorable drug-like properties. Conessine also has high affinity for the adrenergic receptors. Conessine has being shown to possess anti-malarial activity. In India conessine finds therapeutic use for treatment of dysentery and helminthic disorders.
Status:
Investigational
Source:
INN:closiramine [INN]
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Clorisamine is an antihistamine drug developed by Schering in the 1970s. The drug was evaluated in phase 1 clinical trial on healthy volunteers. The results show that in a therapeutic dose of 2 mg the drug did not have any effects which might lead to an impairment of driving ability.
Status:
Investigational
Class (Stereo):
CHEMICAL (MIXED)
Pyroxamine (also known as AHR 224) is benzhydryl ethers of 3-pyrrolidinol patented by A. H. Robins Co., Inc. as antihistamine with bronchodilation activity. In preclinical studies, Pyroxamine shows moderate inhibition of histamine-induced ulceration in guinea pigs
