Vasodilator activity of adenosine analogs

|January 1, 1978

Summary

Researchers explored adenosine analogs for smooth muscle vasodilation. Two analogs showed similar potency to adenosine but longer duration, while a third exhibited significant activity.

Area of Science:

Pharmacology
Cardiovascular Research
Medicinal Chemistry

Background:

Adenosine is a known vasodilator.
Developing novel vasodilators with improved duration of action is crucial for cardiovascular therapies.
Adenosine analogs offer potential for modified pharmacological profiles.

Purpose of the Study:

To evaluate various adenosine analogs as potential smooth muscle vasodilators.
To compare the potency and duration of action of these analogs against adenosine.
To identify adenosine analogs with enhanced vasodilator properties.

Main Methods:

Initial screening of adenosine analogs using a dog hindlimb preparation.
Assessment of coronary vasodilator effects on an isolated rabbit heart.
Evaluation of the duration of action for potent vasodilator compounds.

Main Results:

Most tested adenosine analogs were less potent vasodilators than adenosine.
5'-Deoxy-5'-chloroadenosine and 5'-deoxy-5'-bromoadenosine demonstrated equipotency to adenosine.
These two analogs exhibited a longer duration of action compared to adenosine.
2',3',5'-Trideoxy-3',5'-dichloroadenosine showed significant vasodilator activity.

Conclusions:

Certain adenosine analogs possess significant smooth muscle vasodilator activity.
Specific modifications, such as halogenation at the 5' position, can prolong the duration of action.
2',3',5'-Trideoxy-3',5'-dichloroadenosine represents a promising vasodilator candidate.

Related Experiment Videos

Vasodilator activity of adenosine analogs

Related Concept Videos

Trimethoprim resistance of dihydrofolate reductase variants from clinical isolates of Pneumocystis jirovecii.

Dihydrofolate reductase as a target for chemotherapy in parasites.

Comparison of ternary complexes of Pneumocystis carinii and wild-type human dihydrofolate reductase with coenzyme NADPH and a novel classical antitumor furo[2,3-d]pyrimidine antifolate.

Synthesis of 2,4-diamino-6-(thioarylmethyl)pyrido[2,3-d]pyrimidines as dihydrofolate reductase inhibitors.

Synthesis, antifolate, and antitumor activities of classical and nonclassical 2-amino-4-oxo-5-substituted-pyrrolo[2,3-d]pyrimidines.

Design, synthesis, and X-ray crystal structure of a potent dual inhibitor of thymidylate synthase and dihydrofolate reductase as an antitumor agent.

Experimental and computational study of pMDI aerosol delivery in mucus-coated pediatric airways: Effects of inhalation flow and actuation timing.

Pharmaceutical assessment of low global warming potential alternatives to HFA-134a in a budesonide, glycopyrrolate, and formoterol fumarate pressurized metered dose inhaler.

Biophysical investigations into the impact of crystallization conditions on monoclonal antibody properties and purification.

Implementing scientifically sound practices during drug development: An industry perspective from analytical development.

Block the bitter: Microencapsulation of zidovudine as a taste masking technique for drug inclusion into an oral thin film.

Understanding vial strain during freezing of aqueous solutions-Part II: Identification of influencing formulation, vial and freezing parameters and strain-mitigating strategies.

Synthesis of polyhydroquinoline derivatives as potent antidiabetic and antioxidant agents: in vitro biological activities and computational studies.

An integrated approach: green extraction technique optimization, mechanistic study, and bioactivity profiling of four flavonoids from Epimedium sagittatum.

In silico and In vitro studies of EGFR kinase and Anilide derivatives as inhibitors against Breast Cancer.

LNMGAT: a laplacian regularized pseudo-negative mining graph attention network for robust drug-target interaction prediction under multi-scenario cold-start settings.

Comparative metabolomic and protective effects of Quercus leucotrichophora leaf and acorn extracts against doxorubicin-induced oxidative and inflammatory injury.

Detection of Nitazenes in the Illicit Drug Supply Utilizing Precursor Ion Scan Methods With Paper Spray Mass Spectrometry.

Related Experiment Videos

Vasodilator activity of adenosine analogs

Area of Science:

Background:

Purpose of the Study:

Main Methods:

Main Results:

Conclusions:

Related Concept Videos

Related Articles