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

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Showing 481 - 490 of 609 results

Status:
Investigational
Source:
INN:domazoline
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Domazoline is anticholinergic agent. It is antazoline derivative. Domazoline is antihistaminic, local vasoconstrictor and nasal decongestant. As a hair stiffener, it was used in depilatory preparations.
Status:
Investigational
Source:
NCT00495677: Phase 2 Interventional Completed HIV
(2007)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

PF-232798 is a potent oral CCR5 antagonist with a primary and selectivity/safety pharmacology profile similar to maraviroc (MVC). PF-232798 shows increased binding affinity and improved oral absorption compared to maraviroc. In addition, it retains activity against a laboratory generated maraviroc-resistant HIV-1 strain, indicating an alternative drug resistance profile. PF-232798 binds to the same pocket as MVC within the transmembrane region of CCR5, but shows additional interactions at the ECL2 hinge region. PF-232798 is well tolerated in normal volunteers. PF-232798 had been in a phase-II clinical trial for the treatment of HIV infections. However, this development was discontinued.
Status:
Investigational
Source:
INN:avitriptan
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Avitriptan (BMS-180048), a new 5-HT 1B/1D receptor agonist, has been studied in phase II clinical trials in patients with migraine headaches. Later experiments have confirmed antimigraine activity together with coronary side-effect potential that is why further studies were discontinued.
Status:
Investigational
Source:
JAN:SEMOTIADIL FUMARATE [JAN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Semotiadil (also known as sesamodil or SD 3211) is a (+)-(R)-stereoisomer, the corresponding (−)-(S)-stereoisomer is called levosemotiadil. Semotiadil, a benzothiazine derivative was developed as a novel Ca2+ channel blocker with antiplatelet activity. Experiments on rodents have revealed that the drug had an advantage in the treatment of angina with regard to long-lasting action and selectivity for coronary artery and myocardium. In addition, semotiadil improved survival of rats with monocrotaline-induced pulmonary hypertension: comparison with diltiazem. Semotiadil was studied in phase II clinical trials for the treatment of angina pectoris and hypertension in Europe, and in Japan for the treatment of arrhythmias. However, the further development of semotiadil has now been discontinued.
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: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:
INN:cevipabulin [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Targets:


Cevipabulin is a synthetic, water-soluble tubulin-binding agent with potential antineoplastic activity. Cevipabulin appears to bind at the vinca-binding site on tubulin but seems to act more similar to taxane-site binding agents in that it enhances tubulin polymerization and does not induce tubulin depolymerization. The disruption in microtubule dynamics may eventually inhibit cell division and reduce cellular growth.
Status:
Investigational
Source:
INN:trecetilide
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Trecetilide is a class III antiarrhythmic agent developed for the treatment of atrial flutter and fibrillation. Trecetilide probably has effects on the cardiac myocyte membrane that are similar to ibutilide. It is being developed for both oral and intravenous administration. Unlike ibutilide, trecetilide has good oral bioavailability. Trecetilide has a good metabolic stability. As with ibutilide, its mechanism of class III action may involve both rectifier K+ current blockade and other mechanisms of prolonging repolarization.
Status:
Investigational
Source:
INN:zicronapine [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Zicronapine (formerly known as Lu 31-130), an oral antipsychotic that was studied for the treatment of schizophrenia. The drug was used in a phase III clinical trial.

Showing 481 - 490 of 609 results