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

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Showing 21 - 30 of 123 results

Status:
Investigational
Source:
INN:cirazoline
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Cirazoline is an agonist of alpha1A adrenergic receptor, a partial agonist of alpha1B and alpha1D receptors, and an antagonist of alpha2 adrenergic receptors. Cirazoline was used to study the biologic function of adrenergic receptors. Injection of cirazoline into to the paravenricular hypothalamic nucleus of rats suppressed food and water intake. Cirazoline caused a large renal vasopressor response in rats. Systemic administration of cirazoline impaired spatial working memory in monkeys.
Status:
Investigational
Source:
NCT03557138: Not Applicable Interventional Unknown status Type2 Diabetes Mellitus
(2017)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Investigational
Source:
NCT03408899: Phase 1 Interventional Completed HIV Infections
(2018)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


MIV-150 is a tight-binding, allosteric inhibitor of reverse transcriptase that is active against HIV-1 and HIV-2. MIV-150 has been shown to inactivate viruses that are resistant to other antiviral drugs, including non-nucleoside reverse transcriptase inhibitors, nucleoside reverse transcriptase inhibitors, and protease inhibitors. MIV-150 effectively inactivated free virus. Combination of MIV-150 and Carraguard demonstrated an additive antiviral effect. Seminal fluid had no effect on the antiviral activity of MIV-150 or Carraguard. The average concentration that blocks 50% of infection (EC50) for PC-815 was approximately 10 times stronger than Carraguard for the different clinical isolates used in the study.
Status:
Investigational
Source:
NCT01524666: Not Applicable Human clinical trial Completed Small Fiber Neuropathy
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Status:
Investigational
Source:
NCT02286518: Phase 1 Interventional Completed Clinical Pharmacology
(2014)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Meisoindigo ((E)-1,1'-dimethyl-[3,3'-biindolinylidene]-2,2'-dione) is a derivative of Indigo Naturalis, that has been used in China for chronic myeloid leukemia. In vitro cell line studies have shown that this agent might induce apoptosis and myeloid differentiation of acute myeloid leukemia (AML). Meisoindigo has been a routine therapeutic agent in the clinical treatment of chronic myelogenous leukemia (CML) in China since the 1980s. In phase III clinical trial of Meisoindigo involving 402 patients, it was shown that Meisoindigo was equally efficient for both newly diagnosed and previously treated CML patients after oral administration. The hematological complete response (CR) and partial response (PR) rates, respectively, were 45.0 and 39.3% for newly diagnosed patients and 35.9 and 41.4% for previously treated patients. Meisoindigo was generally well tolerated. The most frequent side‑effects were bone, joint and/or muscle pain of varying degrees when the dosage was more than the suitable one.
Idazoxan is an alpha2 receptor antagonist which also shows activity at imidazoline I1 and I2 receptors and modulates the release of dopamine. Idazoxan was in phase II development in the US. Later the development of idazoxan for schizophrenia was discontinued. It was also in clinical trials for cognition disorders in United Kingdom, and was also discontinued. Idazoxan is used in scientific research as a tool for the study of alpha 2-adrenoceptors.
Status:
Investigational
Source:
INN:mivazerol [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Mivazerol is a new and selective alpha 2-adrenoceptor agonist, devoid of hypotensive effects, which has been designed to prevent adverse cardiac outcome in perioperative patients with, or at risk coronary artery disease. This compound, which lacks hypotensive effects, has been demonstrated to prevent hyperadrenergic activity and myocardial ischemia in perioperative patients and tachycardia in rats at emergence from halothane anesthesia. This type of ischemia, frequently encountered in postoperative patients, is considered to be a consequence of stress-induced hyperactivation of the sympathetic system. Anti-ischemic effects of this compound have been demonstrated in different animal models of myocardial ischemia, and Mivazerol has also been shown to improve exercise-induced ischemia in patients with angina pectoris.