Hypotensive activities

Neurotensin. This hormone has been isolated and characterized from acid—acetone extracts of bovine hypothalamus (118) on the basis of its hypotensive activity. Immunoreactive neurotensin is present in mammalian gut and is distributed throughout the central nervous system its highest concentration is in the hypothalamus and in the substantia gelatinosa of the spinal cord (119). Its overall brain distribution is not unlike that of enkephalin ( ) ... 

Similarly, hypotensive activity is found in other analogues of hydralazine, including the very active endralazine (461) (79AF1835, 79AF1843), a pyrido[4,3-c]pyridazine. 

The association of a specific pharmacologic activity with certain functionality was remarked on earlier. The guanidino group, for example, often yields compounds that show hypotensive activity because of peripheral sympathetic blockade (see, for example, bethanidine). Attachment of a piperidine group to the side chain proves compatible with retention of this activity. 

It is thus of note that a rather simple aminoquinoline shows hypotensive activity. 

During the course of a short and efficient total synthesis of (-) -dendrobine (3-76), an alkaloid which exhibits antipyretic and hypotensive activities [37], a new domino radical sequence has been exploited by Cassayre and Zard which involves the cycli-... 

Perivine 25 exhibits an enhanced local anesthetic activity with respect to cocaine in the rabbit-comea test (230). Tabersonine (67) shows 25% of the hypotensive activity of reserpine on cats, ( )-vincadifformine shows 50% activity, whereas (—)-vincadifformine (ent-10) is inactive (231). 

Alkoxyhexadehydroyohimbanes (618) and 17-alkoxydecadehydroyohim-banes (619) have analgesic and hypotensive activities (356, 357). On the other hand, 16,17,18-trialkoxyhexadehydroyohimbanes (620) are useful as hypotensive and vasodilating agents (358). 

Figure 23. Effect of extension of the imidazoline ring to six-, seven-, and eight-membered rings on hypotensive activity in rabbits...

Figure 24. Hypotensive activity of clonidine derivatives with annel-lated hetero-rings...

Another potent peripheral vasodilator with hypotensive activity is minoxidil (U-10,858, XXXI). The drug was developed at the Upjohn Corporation, apparently as a follow-up of a previous clinical candidate, diallylmelamine -N-oxide (U-20,388, XXXII). The amine precursor, diallylmelamine (U-7720, XXXIII), is active in rats and dogs but not in man because the active... 

A Hungarian research group reported on the hypotensive activity of 3-(pyrazol-l-yl)pyridazines of type (72) in rats [253-256]. The activity of these compounds (in which both of the hydrazino nitrogen atoms are incorporated into a five-membered aromatic ring system) has been found to be mediated by inhibition of prostaglandin-catabolizing enzymes. 

Marked hypotensive activities have been observed with 4-alkoxy-5-fu-roylpiperazinylpyridazin-3(2//)-ones (94) which have been prepared in Spain [356,383,384]. Hypotensive diarylpyridazinones of type (95) have been synthesized in India [385]. Regression analysis has been applied to the hypotensive activities of pyridazinones [386]. 

Pharmacological actions - 5-Alkyl derivatives of (LXVI) are also cited as having diuretic activity [431]. Certain 1,3-dimethyl-6-alkylaminouracils are reported to have diuretic activity similar to that of theophylline [432]. 1,3-Dimethyl-5-ethyl-6-(methylamino)uracil (LXVII) was found to be among the most active of the compounds tested. Diuretic and hypotensive activity are also claimed with anils of 5-amino derivatives, such as (LXVIII) [433]. 

Verapamil possesses antiarrhythmic, antianginal, and hypotensive activity. It reduces the myocardial need of oxygen by reducing contractibility of the myocardium and slowing the freqnency of cardiac contractions. It canses dilation of coronary arteries and increases... 

It does not have a substantial effect on nonvascular smooth musculature or cardiac tissues. Homeostatic circulatory reflexes remain natural, and the resulting hypotension activates cardiovascular reflexes, which are expressed as an increase of heart work, power, and volume of cardiac output. Therefore, it is most effectively used in combination with )3-blockers. 

Information concerning the chemistry of meso-ionic 3-alkyl- and 3-aryl-l,2,3,4-oxatriazol-5-ones (271) is limited, but further investigation may well be encouraged by reports of pronounced hypotensive activity. 3-Cyclohexyl-1,2,3,4-oxatriazol-5-one (271, R = cyclohexyl) is resistant to attack by dilute mineral acid, but warm concentrated sulfuric acid gives cyclohexanol and carbon dioxide. In contrast, acid hydrolysis of 3-phenyl-l,2,3,4-oxatriazol-5-one (271, R = Ph) yields phenyl azide. Meso-ionic 3-cyclohexyl-l,2,3,4-oxatriazol-5-one shows two unusual reactions its photoirradiation in benzene gives cyclohexanone and heating with diphenylacetylene )delds l-cyclohexyl-4,5-diphenyl-1,2,3-triazole (276) rather than the expected 2-cyclohexyl-4,5-diphenyl-1,2,3-triazole. 

Hypotensive activity. Fruit juice, administered by intravenous infusion to dogs at a dose of 10 mL/minute for 30 minutes, was active Water extract of the fresh leaf and stem, administered intravenously to dogs at a dose of 0.1 mL/kg, was active " . Hypothermic activity. Ethanol (50%) extract of the leaf, administered intraperi-toneally to mice at a dose of 0.375 mg/kg, was inactive . 

Hypotensive activity. Essential oil, administered intravenously to dogs at a dose of 3 p,L/kg, was active. The ethanol (70%) extract, administered intravenously to dogs at a dose of 75 mg/kg, was active. There was a dip followed by rise in blood pressure° . Ethanol (80%) extract of the aerial parts, at a dose of 10 mg/kg, was not blocked by atropine. The extract did not inhibit pressor response of norepinephrine either . Ethanol (95%) extract of the seed, administered intravenously to dogs at a dose of 10 mg/kg, produced a transient effect that was blocked by atropine ". Petroleum ether fraction chromatographed and fraction eluted with chloroform, administered intravenously to rabbits at a dose of 0.80 mg/kg, was inactive. Methanol extract, administered intravenously to dogs and rabbits at a... 

Hypotensive activity. Tincture of the gland, administered intravenously to rabbits, was active " """. Water extract of the dried gum resin, administered intravenously to dogs at variable doses, was active " """. Gum extract, administered to anaesthetized rats at doses of 0.3-2.2 mg/100 g body weight, significantly reduced the mean arterial blood pressure " """. 

OE104 Kosak, R., and P. Stern. Examination of the hypotensive activity of folium olivae. Acta Pharm Jugosl 1956 6 ... 

Hypotensive activity. Ethanol (50%) extract of the fresh leaf, administered intragastrically to rats at a dose of 40 mL/kg, was active . 

Hypotensive activity. Methanol (50%) extract of the dried rhizome, administered intravenously to rats at doses of 0.25 and 0.5 g/kg (dry weight of plant), was active ° k Hypothermic activity. Hot water extract of a mixture of Pinellia ternata (Tu), Magnolia obovata (Bk), Perilla frutescens (Aer), Zin ber officinale (Rh), and Poria cocos (Fr) (6, 3, 2, 1, and 5 g, respectively), adminis-... 

Mechanism of Action A synthetic analog of prostaglandin with ocular hypotensive activity. Tiicrapcutic Effect Reduces intraocularpressure(lOP) by increasing the outflow of aqueous humor. 

Use of Bombax ceiba leaves to reduce blood sugar levels is common in North Pakistan Saleem et al. tried an evaluation of the hypotensive activities (and hypoglycemic effect) of the shamimin, a new C-glycosylflavone isolated from this plant. This compound caused 81, 67, and 51%i falls in blood pressure at the doses of 15, 3, and 1 mg/kg, respectively. The effect lasted for 2 to 4 min. Shamimin also produced a significant hypoglycemic effect in Sprague-Dawley rats at the dose of 500 mg/kg the decrease remained constant for the next 4 h. Plasma sugar levels showed a decline of 26%. 

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