A - Human Necessities – 61 – K
Patent
A - Human Necessities
61
K
A61K 31/195 (2006.01) A61K 31/00 (2006.01) A61K 31/135 (2006.01) A61K 31/198 (2006.01) A61K 31/40 (2006.01) A61K 31/401 (2006.01) A61K 31/70 (2006.01) A61K 33/24 (2006.01) A61K 45/06 (2006.01)
Patent
CA 2363847
A new class of anti-hypertensive agent is provided by substances that inhibit the breakdown of the endogenous substances, the enkephalins and/or the endorphins. The anti-hypertensive effect of an enkephalin breakdown inhibitor is greatly enhanced by being combined with a .beta. adrenergic blocking agent, herein designated as .beta. blocker. Specifically, D-phenylalanine, en enkephalin breakdown inhibitor when used alone produces excellent blood pressure lowering in animals and man. Use of a combination of D-phenylalanine and the .beta. blocker propranolol provides a greatly enhanced anti- hypertensive effect in the spontaneously hypertensive rat (SHR). Blood pressure lowering by D-phenylalanine, or the latter combination, is very long lasting in the SHR and man. If the blood pressure of the rat or human is normal, D-phenylalanine has little or no effect on blood pressure. The hypotensive effect of D-phenylalanine is prevented by pretreating the SHR with naloxone or naltrexone which are specific antagonists of enkephalins or endorphins.
L'invention concerne une nouvelle catégorie d'agents efficaces contre l'hypertension: ces produits inhibent la destruction des substances endogènes, à savoir les enképhalines ou les endorphines. L'action hypotensive d'un inhibiteur de ces substances est considérablement améliorée si on combine le produit avec un bêtabloquant. Spécifiquement, la D-phénylalanine est un inhibiteur du type considéré, si on l'utilise seule, et cet inhibiteur donne d'excellents résultats quant à la réduction de la pression sanguine chez l'animal et l'homme. La combinaison de D-phénylalanine et de propranolol bêtabloquant améliore considérablement l'action hypotensive chez le rat spontanément hypertendu. La réduction de la pression sanguine par administration de D-phénylalanine, ou par administration de la combinaison susmentionnée, a un effet très durable chez le rat spontanément hypertendu et chez l'homme. Si la pression sanguine chez le rat et chez l'homme est normale, la D-phénylalanine produit un effet réduit ou bien est inopérante sur la pression sanguine. On prévient l'action hypotensive de ce produit en effectuant chez le rat spontanément hypotendu un prétraitement à base de naloxone et de naltrexone, ces deux substances étant des antagonistes spécifiques vis-à-vis des enképhalines ou des endorphines.
Blum Kenneth
Ehrenpreis Seymour
Bereskin & Parr
Blum Kenneth
Ehrenpreis Seymour
LandOfFree
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