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

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Atenolol is a Beta-1 cardio-selective adreno-receptor blocking agent discovered and developed by ICI in 1976. Atenolol was launched in the market under the trade name Tenormin in 1976, and became the best-selling Beta-blocker in the world in the 1980s and 1990s. TENORMIN is indicated for the treatment of hypertension, to lower blood pressure; also for the long-term management of patients with angina pectoris and also is indicated in the management of hemodynamically stable patients with definite or suspected acute myocardial infarction to reduce cardiovascular mortality. Like metoprolol, atenolol competes with sympathomimetic neurotransmitters such as catecholamines for binding at beta(1)-adrenergic receptors in the heart and vascular smooth muscle, inhibiting sympathetic stimulation. This results in a reduction in resting heart rate, cardiac output, systolic and diastolic blood pressure, and reflex orthostatic hypotension. Higher doses of atenolol also competitively block beta(2)-adrenergic responses in the bronchial and vascular smooth muscles. Hypotensive mechanism of atenolol is very complex. Decrease in CO and inhibition of renin-angiotensin-aldosterone system may mainly be responsible for hypotension. It is likely that potassium retaining action of atenolol partly contributes to its hypotensive action. It is also hypothetized that renal kallikrein-kinin system may play a role in modulating the hypotensive action of atenolol.

Class (Stereo):
CHEMICAL (ACHIRAL)

Isopropanolamine (1-Amino-2-propanol) is a colorless to yellowish liquid with an amine-like odor. It is miscible in water. Intermediate used in the production of dyes, lubrification oils, corrosion inhibitor, detergents, cutting fluids.
Status:
Investigational
Source:
INN:turofexorate isopropyl [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Turofexorate Isopropyl (XL335) is a potent, selective, and orally bioavailable FXR agonist. Binds to the ligand-binding domain (LBD) of human FXR. Turofexorate Isopropyl resides in a predominately hydrophobic pocket with only a few polar atoms making contact with WAY-362450. Turofexorate Isopropyl promotes transcription of the human BSEP, human SHP, and mouse IBABP genes utilizing reporter constructs with EC50 of 17, 230, and 33 nM, respectively in promoter assays. Turofexorate Isopropyl had been in phase I clinical trials for the treatment of hyperlipidemia. This compound was originally discovered by Exelixis Pharmaceuticals, then licensed to Wyeth (now a wholly-owned subsidiary of Pfizer). However, the studies were discontinued.
Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)

Status:
Other

Class (Stereo):
CHEMICAL (RACEMIC)

Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)



ASP-2535 is a glycine transporter-1 (GlyT1) inhibitor which was developed by Astellas Pharma for the treatment of Schizophrenia and Alzheimer's disease. Although ASP-2535 was shown to improve cognitive impairment in animal models, it is no longer in the company pipeline.