U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

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Showing 31 - 40 of 283 results

Status:
Investigational
Source:
INN:sopromidine [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Sopromidine is a neuroprotective drug. Sopromidine is a potent and stereoselective isomer of the achiral H2-agonist impromidine. The chiral impromidine isomer sopromidine is of special interest as the (R)-configurated compound behaves as gpH2R agonist, whereas the (S)-configurated counterpart is devoid of agonist activity. Both Sopromidine and its S enantiomer acted as antagonists of histamine at H3-autoreceptors with similar potencies (Ki = 5.6 X 10(-8) M and 4.5 X 10(-8) M), whereas Sopromidine acted as an H2-receptor agonist and the S-enantiomer as an H2-receptor antagonist.
Status:
Investigational
Source:
INN:guabenxan
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Guabenxan was developed as an oral antihypertensive drug.
Status:
Investigational
Source:
INN:primycin
Source URL:

Class (Stereo):
CHEMICAL (UNKNOWN)

Primycin is a topical antibiotic developed in Hungary for the local treatment of certain superficial and deep infections of the skin and subcutaneous tissue. Primycin is a complex of macrocyclic antibiotics comprising 20 compounds. Primycin possesses good in vitro activity against Staphylococcus aureus and coagulase-negative staphylococci, but its activity against Sirepiococctts pyogenes and enterococci is moderate. It is active against Micrococcus and Bacillus spp. but is inactive against Corynebacterium spp. It is inactive against Enterofojcterwceae and Pseudomonas aeruginosa, yeasts, and dermatophytes. The median lethal dose in the mouse is greater than 3,000 mg/kg of body weight orally and 56 mg/kg intraperitoneally. No skin lesions have been observed after chronic cutaneous applications (90 days) in the rabbit.
Status:
Investigational
Source:
INN:tresperimus
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Tresperimus is a new stable immunosuppressive analog of 15-deoxyspergualin (DSG) obtained by organic chemical synthesis. It was initially developed as an antitumor agent. Tresperimus has been designed to be chemically stable in aqueous solution. Tresperimus controlled alloreactivity in a fully major histocompatibility complex (MHC) mismatched rat cardiac transplant model and also induced donor-specific long-lasting unresponsiveness. Posttransplant tresperimus therapy effectively protected mice from lethal graft-versus-host disease (GVHD) in a dose-related manner. It has been shown to suppress graft rejection as efficiently as cyclosporine A. Indeed, a short course of tresperimus has similar or better effects compared to the effects of cyclosporine in bone marrow, cardiac, and skin transplant models. Prevention of rejection is related to the induction of donor-specific tolerance without affecting immunity to third-party antigens. In addition, CD4+ T-cells from tresperimus-treated animals can transfer donorspecific tolerance to naive animals, an effect not seen with cyclosporine or other traditional immunosuppressive drugs. The mechanism by which tolerance is induced is not clear. Tresperimus binds to Hsc70, a heat shock protein– chaperoned peptide that, among other effects, inhibits nuclear localization of nuclear factor (NF)-kB, which is required for CD40 and CD28 ligation signaling in antigen-presenting cells, an important early step in T-cell costimulation. Locally administered tresperimus appears to be a potential immunosuppressive agent in the management of intraocular inflammation. Tresperimus had been in phase III clinical trial for the treatment of graft-versus-host disease. However, this development was discontinued.
Status:
Investigational
Source:
INN:timegadine [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Timegadine Is a quinolylguanidine derivative patented by Loevens Kemiske Fabrik Produktionsaktieselskab as an anti-arthritic agent. Timegadine acts as a potent, competitive inhibitor of cyclo-oxygenase and lipo-oxygenase. Timegadine significantly inhibits both the primary and secondary lesions of rats adjuvant arthritis when the treatment is initiated on the day of the disease induction and continues for 28 days. Timegadine is able specifically to prevent the development of the swelling of the non-injected paw until 28 days after the adjuvant injection when administered for 5 days prior to and 5 days after the induction of the disease, in analogy with the effect of cyclophosphamide. In clinical trials, Timegadine significantly improves both biochemical and clinical markers of disease activity, i.e. ESR, serum IgG and IgM, leukocyte and platelet counts, duration of morning stiffness, Ritchie index, number of swollen joints and pain. Timegadine treatment associated with gastrointestinal and allergic side effects.
Status:
Investigational
Source:
INN:guanacline [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Guanacline was studied in the treatment of hypertension. However, information about the current use of this compound is not available.
Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)

Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)