Lipid-soluble and water-soluble beta-blockers. Comparison of the central nervous system depressant effect

1987 ◽  
Vol 147 (1) ◽  
pp. 39-43 ◽  
Author(s):  
F. M. Gengo
2008 ◽  
Vol 8 (4) ◽  
pp. 448-451 ◽  
Author(s):  
Tasmina Rahman ◽  
Khandaker Ashfaqur Rahman ◽  
Sultana Rajia ◽  
Mahiuddin Alamgir ◽  
Mahmud Tareq Hassan Khan ◽  
...  

2019 ◽  
Vol 4 (1) ◽  
pp. 1
Author(s):  
Dini Kesuma

Synthesis of the 4-chlorobenzoylthiourea compound was carried out by acylating thiourea with 4-chlorobenzoyl chloride. The 4-chlorobenzoylthiourea compound  will increase the lipophilic and the electronic properties other than the lead compounds of benzoylthiourea in order to, by expectation, raise the central nervous system depressant as well. The lipophilic would affect the ability of the compounds in penetrating biological membranes, which is highly dependent on the solubility of the drug within lipid/water. Log P is the most common method used in determining the parameter value. This experiment was to mix two dissolvents (octanol and water) which are immissible. The both levels of the compounds were carefully observed by a spectrophotometer UV-Vis. From the test, the result of log P value of the 4-chlorobenzoylthiourea compound was 2.32, while the theoretical log P value of the compounds, by using the π Hansch-Fujita method is 1.62 and the f Rekker-Mannhold method is 2.225. Consequently, the result of the test shows that there is a significant difference between the progress experiment and both theoretical log P methods. Moreover, in the test of the central nervous system depressant through the potentiation test to thiopental using mice indicates that the 4-chlorobenzoylthiourea compound have potentiation effects to thiopental compared to the lead compounds of benzoylthiourea.


2009 ◽  
Vol 64 (1-2) ◽  
pp. 1-5 ◽  
Author(s):  
Damião P. de Sousa ◽  
Franklin F. F. Nóbrega ◽  
Liana C. S. L. de Morais ◽  
Reinaldo N. de Almeida

Terpinen-4-ol is a monoterpenoid alcohol and component of the essential oils of several aromatic plants. Similarly to terpinen-4-ol, other monoterpenoid alcohols have shown anticonvulsant activity in convulsion animal models. The present study aimed to investigate the anticonvulsant activity of terpinen-4-ol. Treatment of mice with terpinen-4-ol ( 200 mg/kg) caused a signifi cant decrease in the spontaneous motor activity at 30, 60 and 120 min after administration. Terpinen-4-ol (100 and 200 mg/kg) produced a significant dosedependent increase in the duration of sleeping in mice. Pretreatment of mice with terpinen-4- ol at doses of 100, 200 and 300 mg/kg significantly increased the latency of pentylenetetrazole -induced convulsions. Terpinen-4-ol (200 and 300 mg/kg) also inhibited the induced seizures of picrotoxin. In another model, maximal electroshock seizure, terpinen-4-ol decreased the tonic hind convulsions percentage at the dose of 300 mg/kg. From the overall results we can conclude that terpinen-4-ol showed a depressant effect on the central nervous system and significant anticonvulsant activity.


2007 ◽  
Vol 62 (7-8) ◽  
pp. 563-566 ◽  
Author(s):  
Damião Pergentino de Sousa ◽  
Ellen Raphael ◽  
Ursula Brocksom ◽  
Timothy John Brocksom

Many essential oils and monoterpenes are used therapeutically as relaxing drugs and tranquilizers. In this study, ten structurally related monoterpene alcohols, present in many essential oils, were evaluated in mice to investigate their pharmacological potential in the central nervous system. Isopulegol (1), neoisopulegol (2), (±)-isopinocampheol (3), (-)-myrtenol (4), (-)-cis-myrtanol (5), (+)-p-menth-1-en-9-ol (6) and (±)-neomenthol (8) exhibited a depressant effect in the pentobarbital-induced sleep test, indicating a sedative property. (-)- Menthol (7), (+)-dihydrocarveol (9), and (±)-isoborneol (10) were ineffective in this test. The results show that these psychoactive monoterpenes have the profile of sedative drugs, and this pharmacological effect is influenced by the structural characteristics of the molecules


Sign in / Sign up

Export Citation Format

Share Document