Document Detail

The antihypertensive property of NIP-121, a novel potassium channel opener in rats.
MedLine Citation:
PMID:  1717778     Owner:  NLM     Status:  MEDLINE    
The antihypertensive effects of NIP-121, a novel potassium channel opener, were examined in comparison with cromakalim and its active enantiomer, lemakalim. In experiments by direct blood pressure measurements, orally administered NIP-121 dose-relatedly decreased arterial blood pressure in conscious spontaneously hypertensive rats (SHRs), and the ED20 values (the doses to produce 20% decrease of the mean blood pressure) of NIP-121 and cromakalim were 0.010 and 0.11 mg/kg, respectively, NIP-121 thus being about ten times more potent than cromakalim. The duration of the hypotensive effect by NIP-121 was longer than that by cromakalim. The hypotensive effect of NIP-121 was stronger in SHRs than in normotensive rats. All three drugs showed tachycardia that was antagonized by a beta-blocker, propranolol. Intravenously administered NIP-121 also showed a more potent hypotensive action with longer duration than cromakalim in conscious SHRs. The ED20 values for hypotension by NIP-121, cromakalim, and lemakalim were 0.017, 0.040, and 0.016 mg/kg, respectively. The intravenous hypotensive potency of NIP-121 but not cromakalim was similar to that of p.o. administration. The repeated treatments with NIP-121 (0.025, 0.05, and 0.1 mg/kg p.o. once a day) for 15 days did not modify the degree of the hypotensive action. In the anesthetized SHRs, pretreatment with glibenclamide but not other antagonists (atropine, propranolol, diphenhydramine + cimetidine, or indomethacin) suppressed the decrease in blood pressure induced by NIP-121.(ABSTRACT TRUNCATED AT 250 WORDS)
Y Masuda; C Arakawa; T Yokoyama; K Shigenobu; S Tanaka
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Publication Detail:
Type:  Comparative Study; Journal Article    
Journal Detail:
Title:  Journal of cardiovascular pharmacology     Volume:  18     ISSN:  0160-2446     ISO Abbreviation:  J. Cardiovasc. Pharmacol.     Publication Date:  1991 Aug 
Date Detail:
Created Date:  1991-11-08     Completed Date:  1991-11-08     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  7902492     Medline TA:  J Cardiovasc Pharmacol     Country:  UNITED STATES    
Other Details:
Languages:  eng     Pagination:  190-7     Citation Subset:  IM    
Shiraoka Research Station of Biological Science, Nissan Chemical Industries, Ltd., Saitama, Japan.
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MeSH Terms
Administration, Oral
Antihypertensive Agents / pharmacology*
Benzopyrans / pharmacology
Blood Pressure / drug effects
Dose-Response Relationship, Drug
Heart Rate / drug effects
Injections, Intravenous
Oxadiazoles / pharmacology*
Piperidines / pharmacology*
Potassium Channels / drug effects*
Pyrroles / pharmacology
Rats, Inbred SHR
Rats, Inbred Strains
Rats, Inbred WKY
Species Specificity
Reg. No./Substance:
0/Antihypertensive Agents; 0/Benzopyrans; 0/Oxadiazoles; 0/Piperidines; 0/Potassium Channels; 0/Pyrroles; 135244-62-1/NIP 121; 94470-67-4/Cromakalim

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