Rilmenidine differs from clonidine in that it lacks histamine-like activity

¹Department of Pharmacology, University of Melbourne, Vic., Australia.

The Journal of Pharmacy and Pharmacology

|July 1, 1989

Summary

Rilmenidine, an antihypertensive drug, does not activate histamine H2-receptors, unlike clonidine. Studies on guinea-pig atria and rat uterus confirm rilmenidine lacks histamine-like activity, differentiating it from clonidine.

Area of Science:

Pharmacology
Cardiovascular Research
Histamine Receptor Studies

Background:

Rilmenidine is a novel antihypertensive agent.
Clonidine shares a similar mechanism of action with rilmenidine.
Histamine H2-receptor agonists elicit specific physiological responses.

Purpose of the Study:

To investigate if rilmenidine exhibits histamine-like activity.
To compare the histamine H2-receptor activity of rilmenidine and clonidine.
To determine the effect of cimetidine on rilmenidine's activity.

Main Methods:

Isolated guinea-pig atria were used to assess chronotropic effects.
Isolated rat uterus (stilboestrol-treated, KCl-contracted) was used to assess relaxant effects.
Concentration-response curves were generated in the presence and absence of cimetidine (histamine H2-receptor antagonist).

Main Results:

Histamine and clonidine induced positive chronotropic effects in guinea-pig atria, blocked by cimetidine.
Rilmenidine caused a negative chronotropic effect in guinea-pig atria, unaffected by cimetidine.
Histamine and clonidine induced relaxations in rat uterus, blocked by cimetidine.
Rilmenidine induced relaxation in rat uterus, not affected by cimetidine.

Conclusions:

Rilmenidine does not activate histamine H2-receptors.
Unlike clonidine, rilmenidine lacks histamine-like activity on guinea-pig atria and rat uterus.
This study differentiates the pharmacological profile of rilmenidine from clonidine regarding histamine H2-receptor interaction.

Related Experiment Videos

Rilmenidine differs from clonidine in that it lacks histamine-like activity

Related Concept Videos

[Research on the construction and application of an intelligent internet of things-enabled dental chair platform based on dental chair domain interconnection].

[Infectious complications following chimeric antigen receptor T-cell therapy for a hematologic malignancy within 28 days].

[Gene analysis and clinical features of MYH9-related disease].

[Clinicopathological characteristics and prognosis of patients with sporadic multiple primary gastrointestinal stromal tumors].

[Plasma differentially expressed genes and bioinformatics analysis of workers occupationally exposed to mercury].

[The correlation between serum uric acid levels in the third trimester of pregnancy and adverse pregnancy outcomes].

Amorphous particles enhance oral exposure-a case study of a poorly soluble compound in preclinical, toxicology and early clinical studies.

Neuroprotective euglobals from Eucalyptus tereticornis Smith. leaves: quantification, network pharmacology-guided in silico analysis, and experimental validation.

A review of natural plant polysaccharides: the relationship between extraction methods, physicochemical properties, structures, and biological activity.

Acute intravenous antihypertensive and in vitro vasorelaxant effect of the hydroalcoholic stem bark extract of Hymenaea rubriflora Ducke in spontaneously hypertensive rats.

Shanhuang Jiangzhi tablets mitigate atherosclerosis by modulating macrophage polarization and inhibiting foam cell formation via the ROS/TLR4/NF-κB pathway.

Nanocarrier-based targeting strategies in epilepsy: addressing pathophysiological barriers.

Related Experiment Videos

Rilmenidine differs from clonidine in that it lacks histamine-like activity

Area of Science:

Background:

Purpose of the Study:

Main Methods:

Main Results:

Conclusions:

Related Concept Videos

Related Articles