TERTATOLOL

Details

Stereochemistry	RACEMIC
Molecular Formula	C16H25NO2S
Molecular Weight	295.44
Optical Activity	( + / - )
Defined Stereocenters	0 / 1
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CC(C)(C)NCC(O)COC1=CC=CC2=C1SCCC2

InChI

InChIKey=HTWFXPCUFWKXOP-UHFFFAOYSA-N

InChI=1S/C16H25NO2S/c1-16(2,3)17-10-13(18)11-19-14-8-4-6-12-7-5-9-20-15(12)14/h4,6,8,13,17-18H,5,7,9-11H2,1-3H3

HIDE SMILES / InChI

Description
Sources: https://www.ncbi.nlm.nih.gov/pubmed/7686633 | https://www.ncbi.nlm.nih.gov/pubmed/8093601 | https://www.ncbi.nlm.nih.gov/pubmed/7903216 | https://www.ncbi.nlm.nih.gov/pubmed/7903218 | https://www.ncbi.nlm.nih.gov/pubmed/7903214 | https://www.ncbi.nlm.nih.gov/pubmed/3541611 | http://www.doctissimo.fr/medicament-ARTEX.htm

Tertatolol is a beta-blocker with unique renal vasodilatatory effects, mainly at the level of the microcirculation. The mechanisms of this renal vasodilatation are not fully understood but might involve renal 5-HT1A receptor stimulation. It is a potent competitive antagonist of 5-HT1A and 5-HT1B receptors. Tertatolol inhibits human mesangial cell proliferation. Biochemical surveillance did not show any adverse metabolic effects of tertatolol. Tertatolol is rapidly and totally absorbed by the gastro-intestinal tract with a low presystemic metabolism, and the bioavailability is not affected by food intake. It is used as antihypertension agent.

Approval Year

PubMed

Title	Date	PubMed
Stereoselectivity for interactions of agonists and antagonists at mouse, rat and human beta3-adrenoceptors.	2004-01-26	14744619
Specific labelling of serotonin 5-HT(1B) receptors in rat frontal cortex with the novel, phenylpiperazine derivative, [3H]GR125,743. A pharmacological characterization.	2002-04	11888550
Renal and systemic effects of atenolol and tertatolol in renal transplant recipients on cyclosporine A.	1998-02	9509456
Post-synaptic 5-HT1A receptor involvement in yawning and penile erections induced by apomorphine, physostigmine and mCPP in rats.	1995-08	8539317
Nicardipine decreases blood pressure and heart rate at nucleus tractus solitarii of spontaneously hypertensive rats.	1989-11	2481182

Patents

Sample Use Guides

In Vivo Use Guide

One tablet (5 mg) a day in the morning. Tertatolol tablet can be taken before, during, or after breakfast.

Route of Administration: Oral

Name

Type

Language

TERTATOLOL

Official Name

English

TERTATOLOL [MI]

Preferred Name

English

tertatolol [INN]

Common Name

English

(±)-1-(TERT-BUTYLAMINO)-3-(THIOCHROMAN-8-YLOXY)-2-PROPANOL

Systematic Name

English

Tertatolol [WHO-DD]

Common Name

English

Classification Tree Code System Code

WHO-ATC

C07AA16