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|Title: ||Effects of two newly synthesized analogues of lidocaine on rat arterial blood pressure and heart rate|
|Authors: ||Al Rasheed, N.M.|
Al Zuhair, H.H.
Al Obaid, A.R.M.
|Issue Date: ||2001 |
|Publisher: ||Academic Press|
|Citation: ||Pharmacological Research: 43 (4); 313-319|
|Abstract: ||Two new analogues of lidocaine were synthesized at the College of Pharmacy, King Saud University:
compound I (Methyl-2-[2-(N,N-diethylamino) acetamido]-3-cyano-4,5-dimethylbenzoate)
and compound II (Methyl-2-[2-(piperidino) acetamido]-3-cyano-4,5-dimethylbenzoate). Their
influence on the arterial blood pressure and the heart rate of urethane-anaesthetized rats was studied
and compared with the actions of lidocaine. Compounds I, II and lidocaine induced significant
dose-dependent decreases in the arterial blood pressure and heart rate, which usually returned
to basal values within 3–5 min. There were significant differences in the potency of the three
compounds in producing their effects on blood pressure and heart rate (P < 0:0001, ANOVA).
Compound II was 14 and 6 times more potent in reducing blood pressure and 8 and 2 times more
capable of reducing the heart rate than lidocaine and compound I, respectively. The results of
this study also indicated the ineffectiveness of antagonists of autonomic, histaminergic and 5-HT
receptor, and various vasodilators in blocking the actions of the three compounds on blood pressure
and heart rate. Pretreatment with CaCl2 significantly reduced the hypotension and bradycardia
induced by the three compounds, suggesting the involvement of calcium channels, probably of the
L type. Several possible mechanisms are postulated. In conclusion, the results direct attention to
the capability of the two new compounds to decrease blood pressure and heart rate; affects that may
have clinical potential.|
|Appears in Collections:||College of Pharmacy|
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