2-Ethynylbenzenealkanamines: a new class of calcium entry blockers with potential antihypertensive and antianginal properties

Journal Article · Wed Mar 05 04:00:00 EST 1986 · Fed. Proc., Fed. Am. Soc. Exp. Biol.; (United States)

OSTI ID:6898829

Brannan, M D; Carson, J R; Gill, A; Keely, S L; Flaim, S F; Sit, S P; Damiano, B P; Carmosin, R R.J.; Gleason, M M; Ludovici, D W; Pitis, P M

2-Ethynylbenzenealkanamines represent a newly discovered class of calcium channel blockers in that they inhibited KCl-stimulated /sup 45/Ca influx and isometric tension development in isolated vascular smooth muscle and prolonged AV-nodal conduction time in canine hearts. Testing revealed optimal activity in the following structure where R1 is aryl, R2 and R4 are methyl, R3 is aralkyl and X is methoxy: compounds in this group lowered arterial pressures in conscious spontaneously hypertensive rats and renal hypertensive dogs following either oral or parenteral administration, and thus are potential antihypertensive agents. These compounds also caused coronary vasodilation at concentrations which did not affect rate or force of contraction in the isolated, perfused guinea pig heart preparation, they increased coronary blood flow and decreased coronary vascular resistance in the anesthetized canine, and thus are potential antianginal agents. In summary, 2-ethynylbenzenealkanamines represent a new class of calcium entry blockers which have potential antihypertensive and antianginal properties.

• Research Organization: McNeil Pharmaceutical, Spring, House, PA
• OSTI ID: 6898829
• Report Number(s): CONF-8604222-
• Journal Information: Fed. Proc., Fed. Am. Soc. Exp. Biol.; (United States), Journal Name: Fed. Proc., Fed. Am. Soc. Exp. Biol.; (United States) Vol. 45:4; ISSN FEPRA
• Country of Publication: United States
• Language: English

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59 BASIC BIOLOGICAL SCIENCES
ALKALINE EARTH ISOTOPES
ALKALINE EARTH METALS
ANIMALS
ANTIHYPERTENSIVE AGENTS
ARTERIES
BETA DECAY RADIOISOTOPES
BETA-MINUS DECAY RADIOISOTOPES
BLOOD PRESSURE
BLOOD VESSELS
BODY
CALCIUM
CALCIUM 45
CALCIUM ISOTOPES
CARDIOVASCULAR AGENTS
CARDIOVASCULAR DISEASES
CARDIOVASCULAR SYSTEM
CHEMICAL PROPERTIES
CORONARIES
DAYS LIVING RADIOISOTOPES
DISEASES
DOGS
DRUGS
ELEMENTS
EVEN-ODD NUCLEI
HEART
HYPERTENSION
INTERMEDIATE MASS NUCLEI
ISOTOPE APPLICATIONS
ISOTOPES
MAMMALS
METALS
MUSCLES
NUCLEI
ORGANS
PATHOGENESIS
RADIOISOTOPES
SYMPTOMS
TRACER TECHNIQUES
VASCULAR DISEASES
VASODILATION
VERTEBRATES