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

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Showing 71 - 80 of 2237 results

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

Class (Stereo):
CHEMICAL (ACHIRAL)

Piberaline (EGYT-475) is the antidepressant drug. Piberaline antagonized the reserpine-induced dopamine depletion in the olfactory tubercle of rats. Piberaline in contrast to tricyclic antidepressants does not impair the acquisition of avoidance conditioning but rather improves it while it does not facilitate the extinction of learned behavior but considerably delays it. EGYT-2760, an active metabolite of EGYT-475, has a central serotoninomimetic action which involves 5-HT uptake-inhibition and 5-HT1 receptor agonistic effect.
Status:
Investigational
Source:
INN:lerisetron
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Lerisetron is a 5-hydroxytryptamine3 receptor antagonist. It was under development by FAES Farma for the potential treatment of emesis resulting from chemotherapy. Lerisetron specifically binds to 5-HT3 receptors, located peripherally on vagus nerve terminals and centrally in the chemoreceptor trigger zone (CTZ) of the area postrema, which may result in suppression of chemotherapy-induced nausea and vomiting. Lerisetron had been in phase III clinical trials for the treatment of emesis. However, this study was discontinued.
Status:
Investigational
Source:
USAN:Amicibone
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Amicibone is an antitussive agent.
Status:
Investigational
Source:
INN:ciglitazone
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Ciglitazone, 5-[4-(1-methylcyclohexylmethoxy) benzyl]-thiazolidine-2,4-dione, is a hypoglycemic agent and a thiazolidenedione derivative. Ciglitazone binds to the PPAR gamma receptor and possesses agonist activity. This drug was in clinical trials in Japan for the treatment Diabetes mellitus, but that study has been discontinued. Ciglitazone was able to decrease the production of vascular endothelial growth factor (VEGF) in an in vitro human granulosa cell model. That result together with the pivotal role of VEGF in ovarian hyperstimulation syndrome suggests that ciglitazone may have a high potential as a therapeutic agent.
Status:
Investigational
Source:
INN:palosuran [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Palosuran, also known as ACT-058362, a potent and specific antagonist of the human UT receptor. Urotensin inhibition with palosuran was a promising alternative in pulmonary arterial hypertension. Palosuran inhibits binding to primate UT receptors in cell membranes but demonstrates differential activity in intact cells and vascular tissues. Palosuran improves pancreatic and renal function in diabetic rats. Phase-II clinical trials for diabetic nephropathies and cardiovascular disorders were discontinued.
Status:
Investigational
Source:
INN:abitesartan
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Abitesartan is an angiotensin II receptor antagonist, antihypertensive (non-peptidic) agent.
Status:
Investigational
Source:
INN:dioxifedrine
Source URL:

Class (Stereo):
CHEMICAL (UNKNOWN)

Dioxifedrine is the putative metabolite of 3,4-methylenedioxymethamphetamine. It is the sympathomimetic agent and beta-2 -adrenergic agonist with bronchodilator activity. Dioxifedrine selectively binds to and activates beta-2 adrenergic receptors in bronchiolar smooth muscle, thereby causing stimulation of adenyl cyclase, the enzyme that catalyzes the conversion of adenosine triphosphate (ATP) to cyclic-3',5'-adenosine monophosphate (cAMP). Increased intracellular cAMP levels cause relaxation of bronchial smooth muscle. In stimulatory studies dioxifedrine increased locomotor activity from 15 to 30 min following the drug administration. Following intracerebroventricular injection dioxifedrine rapidly reduced blood pressure and heart rate.
Status:
Investigational
Source:
INN:bipenamol [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Conditions:

Bipenamol is a benzenemethanol derivative used to prepare novel semicarbazide-derived inhibitors of human dipeptidyl peptidase I.
Status:
Investigational
Source:
NCT02845271: Phase 2 Interventional Completed Osteoarthritis
(2016)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Status:
Investigational
Source:
NCT04461509: Phase 2 Interventional Active, not recruiting Prostatic Neoplasms
(2021)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)