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

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Showing 641 - 650 of 11247 results

Status:
Investigational
Source:
INN:mefenidil
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Mefenidil has been reported to be a selective cerebral vasodilator. It significantly increased cerebral blood flow (without stimulation of O2 uptake) and lowered cerebral vascular resistance without having significant effects in other circulatory regions. Increase in cerebral blood flow is not mediated via the beta-adrenergic receptor as the effect was not blocked by propranolol. However, the clinical usefulness of mefenidil as a cerebral vasodilator may be limited by the accompanying arterial hypotension due to systemic vasodilation, which was most prominent in heart and gut.
Status:
Investigational
Source:
INN:prothixene [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Prothixene is a thioxanthene derivative patented by Swiss multinational healthcare F. Hoffmann-La Roche & Co. as an antiemetic and neuroleptic agent. In preclinical models, prothixene shows patent antihistaminic activity. The central depressant activity of prothixene in the rotating rod test and the potentiation of thiopental narcosis and hypothermia in white mice (H strain) is one order lower than in the case of chlorprothixene. Prothixene has a higher protective effect in the supramaximal electric shock test with mice than promethazine and chlorprothixene. However, it has no effect on the reserpine ptosis in mice nor on the ulcerogenic action of reserpine in rats (Wistar strain). Its anti-serotonin activity is higher in vivo and in vitro than that of promethazine. The local irritation, tested on rabbits, is lower by 52% after prothixene application than after promethazine. Prothixene applied parenterally is more toxic to mice than promethazine. In oral administration, to mice, no differences in toxicity were found.
Status:
Investigational
Source:
INN:dichloroxylenol [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Dichloroxylenol is a bactericide, preservative and deodorant. It is often used in the preparation of antiseptic and deodorant lotions and bath preparations. Dichloroxylenol also showed slightly greater activity against S. aureus Oxoid 701/1 Lot 610254 than against Escherichia coli and Salmonella typhi, indicating a probable role for cell wall in the susceptibility of bacteria to dichloroxylenol. The efficacy of either povidone-iodine (Betadine) or dichloroxylenol (Septocid) intrauterine infusions on the treatment of endometritis and/or cervicitis in cows was examined. The recovery and conception rates obtained after Betadine treatment were better than those obtained after Septocid. Moreover, healthy cows and those inseminated before post-partum day 180, having no more than 4-7 previous services, responded well to either Betadine or Septocid treatment.
Status:
Investigational
Source:
INN:picumeterol
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Picumeterol (GR114297A) is a potent and highly selective beta2-adrenoceptor agonist with a longer duration of action than salbutamol, but shorter than salmeterol. Picumeterol is the (R)-isomer of the racemic entity GR63411B, and picumeterol has been shown to be about 40 times more potent than the (S)-isomer (GR114744A) in various in vitro pharmacological models of beta2-agonist activity. Picumeterol is of potential value in the treatment of asthma and related diseases in man following inhalation administration. In the clinical studies, the bronchodilator potencies of picumeterol and GR 63411B were similar. However, both drugs were short-acting, which is at odds with their activity in vitro. These compounds display dissociation between bronchodilator activity and protection against methacholine-induced bronchoconstriction.
Status:
Investigational
Source:
NCT00427856: Phase 2 Interventional Completed Lymphoma, Follicular
(2007)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Obatoclax (GX15-070) is a novel BH3 mimetic pan Bcl- 2 inhibitor. The clinically studied formulation is as obatoclax mesylate (Box 1), a salt. It is only under study as an intravenous preparation. It functions to block BH3-mediated binding of Bcl-2, Bcl-XL, Mcl-1 and A1 to Bax and Bak. Bax and Bak thus are unopposed and able to dimerize to allow initiation of intrinsic apoptosis. Preclinically, obatoclax has been shown to reverse inhibition of Bax or Bak by Bcl-2, Bcl-XL, Bcl-w and Mcl-1. Obatoclax was discovered by Gemin X, which was acquired by Cephalon, which has since been acquired by Teva Pharmaceuticals. Obatoclax had been in phase III clinical trials by Gemin X Biotechnologies (subsidiary of Teva) for the treatment of non-small lung cancer (NSCLC). The compound received orphan drug designation in the U.S. in 2004 for the treatment of chronic lymphocytic leukemia (CLL). However, Teva discontinued the development of obatoclax in 2013.
Status:
Investigational
Source:
NCT01644682: Phase 3 Interventional Completed Cost-effective and Sustainable Vector Control Methods Will be Established to Reduce VL in India, Bangladesh and Nepal
(2012)
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Status:
Investigational
Source:
INN:intriptyline
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Intriptyline is a dibenzocycloheptene derivative and mixed monoamine reuptake inhibitor patented by Laboratoires du Docteur Jacques Auclair as tricyclic antidepressant.
Status:
Investigational
Source:
INN:dimelazine [INN]
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Dimelazine is a sedative, antihistaminic agent.
Status:
Investigational
Source:
NCT00503360: Phase 1 Interventional Completed Ocular Hypertension
(2007)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

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

Class (Stereo):
CHEMICAL (ACHIRAL)

Clociguanil (BRL 50216, WR 38839) is an antimalarial compound, a derivative of N-benzyloxydihydrotriazine, developed by Beecham Pharmaceuticals. Mode of action studies indicated that clociguanil is a dihydrofolate reductase inhibitor of Plasmodium and is capable of marked potentiation with a selected sulphonamide against both the sensitive N strain and the cycloguanil-resistant B line of P. berghei. A combination of clociguanil and sulphadiazine prevented the development of parasitemia caused by P. falciparum in humans. The subsequent development of clociguanil was discontinued because of a relatively short half-life in man and lack of suppression of pre-erythrocytic schizogony of a strain of P. falciparum resistant to chloroquine, pyrimethamine, and proguanil.