Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts:   Target Concepts:
Query: UNIPROT:P00790 (PGA)
 2,475 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

The inhibitory effect of various prostaglandin analogues on the anchorage independent growth of murine and human melanoma cells was measured. PGA analogues (which were modified at C-16 and C-18) did not demonstrate any major improvement in activity over PGA alone. These included 16,16-dimethyl PGA1, 16,16-dimethyl-PGA2, 16,16-dimethyl-18-oxa-PGA2 and trans-delta-2-15-alpha acetoxy-16,16-dimethyl-18-oxa-11-deoxy-PGE1-methylester. The thromboxane synthetase inhibitor, U51605, demonstrated weak anti-proliferative activity. PGD2 (with a ketone at C-11 versus C-9 for PGA and PGE) was the most potent prostaglandin tested. Cells from melanoma lines displayed species differences in their sensitivities. PGA1 and PGE1 were the most potent inhibitors of the anchorage independent growth of murine melanoma cells. On human melanoma cells PGD2 was the most active prostaglandin, 2-3 times more potent than PGA1; PGE1 was a very weak inhibitor.
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PMID:In vitro modulation of human and murine melanoma growth by prostanoid analogues. 658 9

Following close intra-arterial administration to the carotid and femoral arterial beds of the anaesthetised dog the rank order of potency for producing vasodilation was PGE greater than 11-deoxy PGE0 greater than PGA greater than PGI2 greater than PGB with the 1- and 2-series prostaglandins equipotent. PGI2 was about 60 times weaker than PGE1. In the mesenteric arterial bed the rank order of potency for producing vasodilation was the same except PGI2 was about equipotent with PGE1. The absolute potency of the prostaglandins, with the exception of PGI, was similar on all three vascular beds. A similar differential action of PGI2 relative to PGE1 was also observed following both left intraventricular and intravenous administration. We suggest that all three arterial beds contain PGE-receptors mediating vasodilatation at which the E-series prostaglandins are potent and PGI2 is weak. In addition the mesenteric bed contains PGI2-receptors which are absent or sparse in the carotid and femoral beds.
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PMID:Comparison of the potencies of some prostaglandins as vasodilators in three vascular beds of the anaesthetised dog. 674 31

In 15 anesthetized rabbits the reflex changes in arterial pressure, heart rate and respiratory rate in response to injections of bradykinin inorganic phosphate and prostaglandins into femoral artery have been studied. Intraarterial injection of bradykinin produced a reflex fall in arterial pressure, bradycardia and tachypnea. The latency of response ranged from 6 to 7 sec. The threshold dose was about 50 ng. This effect was accompanied by a consistent increase in the afferent discharge in the saphenus nerve. Isotonic mixtures of Na2HPO4 and NaH2PO4 at pH 7, PGE1, PGE2, and PGA, when injected into femoral artery even in high doses, failed to produce any significant cardiocirculatory or respiratory reflex responses. Infusion of PGE1 (1 ug/min) into femoral artery, although inactive by itself, enhanced the reflex effect of bradykinin.
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PMID:[Comparative study of cardiocirculatory response and respiratory reflex to the injection of bradykinin, inorganic phosphates and prostaglandins into the femoral artery]. 730 10

Peripheral vascular disease is a common ailment of the aged and diabetic communities. As the numbers of these individuals increase, the need for therapeutic interventions will continue to grow. One of the possible therapies is the use of prostaglandins (PGE(1), prostacyclin and Iloprost) to decrease the vascular tone and increase vascular blood flow. Due to the hydrophobicity of the prostaglandins and prostaglandin analogues, various vehicles have been utilized to maintain the active pharmaceutical ingredient in a stable solution, e.g. alpha-cyclodextrin (Alprostadil, Edex) or emulsified lipid vehicles. In our laboratory, we designed a method for separating and assaying lipid-encapsulated PGE(1). Utilizing organic extraction, automated solid-phase extraction and precipitation techniques, we validated the measurement of the PGE(1) and PGA(1) content of the clinical drug formulation in the microgram per milliliter concentration range with an high performance liquid chromatography (HPLC) assay.
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PMID:A chromatographic method for the quantification of prostaglandin E(1) and prostaglandin A(1) encapsulated in an intravenous lipid formulation. 1192 72


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