2-Ethynylbenzenealkanamines. A new class of calcium entry blockers.
A series of 2-(aryl- or alkylethynyl)benzenealkanamines were synthesized. They exhibit antihypertensive activity in spontaneously hypertensive rats and coronary vasodilator activity with minimal negative inotropic activity in the "Langendorff" guinea pig heart in vitro. They have been shown to exert their activity by inhibition of Ca2+ influx across cell membranes. Optimal activity is found among the N-(arylethyl)-5-methoxy-alpha-methyl-2-(phenylethynyl)ben zeneethanamines and -propanamines.
Carson
J R
JR
McNeil Pharmaceutical, Spring House, Pennsylvania 19477-0776.
Almond
H R
HR
Brannan
M D
MD
Carmosin
R J
RJ
Flaim
S F
SF
Gill
A
A
Gleason
M M
MM
Keely
S L
SL
Ludovici
D W
DW
Pitis
P M
PM
D000480:Alkynes / Q000138:chemical synthesis* / Q000494:pharmacology; D000588:Amines / Q000138:chemical synthesis* / Q000494:pharmacology; D000818:Animals; D002121:Calcium Channel Blockers / Q000138:chemical synthesis* / Q000494:pharmacology; D003326:Coronary Circulation / Q000187:drug effects; D006168:Guinea Pigs; D006973:Hypertension / Q000188:drug therapy; D051381:Rats; D011918:Rats, Inbred SHR; D013329:Structure-Activity Relationship; D014664:Vasodilation / Q000187:drug effects
D000480:Alkynes; D000588:Amines; D002121:Calcium Channel Blockers