L-prolyl-L-leucyl-glycinamide analogues--a new class of peptide antihypertensives. 1986

G Rajakumar, and A N Singh, and F Naas, and S Chiu, and C Y Kwan, and R L Johnson, and R K Mishra

Accumulating evidence suggests that there is an increase in the density (maximum binding sites) of striatal dopamine receptors in the central nervous system of spontaneously hypertensive rats (SHR). A tripeptide of hypothalamic origin, PLG (L-Prolyl-L-Leucyl-Glycinamide) has been found to have modulatory effect on the dopamine receptors in the central nervous system of rats. Two analogues of PLG with cyclic amino-acid residues, L-Prolyl-L-Leucyl-(-)-thiazolidine-2-carboxamide and L-Prolyl-L-Leucyl-(+)-thiazolidine-2-carboxamide, have shown antihypertensive effect at the established phase of hypertension in 16-week old SHRs at a dose of 35 mg/kg per day per 7 days i.p. It was also observed from studies of radioligand [3H]-spiroperidol binding that the laevo-isomer of the PLG analogue has down-regulated the up-regulated dopamine receptors. Our findings confirm the role of central dopaminergic pathways in the pathogenesis of hypertension in SHR.

UI MeSH Term Description Entries
D006973 Hypertension Persistently high systemic arterial BLOOD PRESSURE. Based on multiple readings (BLOOD PRESSURE DETERMINATION), hypertension is currently defined as when SYSTOLIC PRESSURE is consistently greater than 140 mm Hg or when DIASTOLIC PRESSURE is consistently 90 mm Hg or more. Blood Pressure, High,Blood Pressures, High,High Blood Pressure,High Blood Pressures
D008297 Male Males
D009075 MSH Release-Inhibiting Hormone A hypothalamic tripeptide, enzymatic degradation product of OXYTOCIN, that inhibits the release of MELANOCYTE-STIMULATING HORMONES. MSH Release-Inhibiting Factor,Melanocyte-Stimulating Hormone Release-Inhibiting Hormone,Prolyl-Leucyl-Glycinamide,H-Pro-Leu-Gly-NH2,MIF-1,MIF-I,Melanocyte-Stimulating Hormone Release-Inhibiting Factor,Melanostatin,Oxytocin (7-9),Pro-Leu-Gly-NH2,Pro-Leu-Glyamide,Prol-Leu-Gly-NH2,Prolylleucylglycinamide,Prol Leu Gly NH2,Prolyl Leucyl Glycinamide
D011918 Rats, Inbred SHR A strain of Rattus norvegicus with elevated blood pressure used as a model for studying hypertension and stroke. Rats, Spontaneously Hypertensive,Rats, SHR,Inbred SHR Rat,Inbred SHR Rats,Rat, Inbred SHR,Rat, SHR,Rat, Spontaneously Hypertensive,SHR Rat,SHR Rat, Inbred,SHR Rats,SHR Rats, Inbred,Spontaneously Hypertensive Rat,Spontaneously Hypertensive Rats
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D000959 Antihypertensive Agents Drugs used in the treatment of acute or chronic vascular HYPERTENSION regardless of pharmacological mechanism. Among the antihypertensive agents are DIURETICS; (especially DIURETICS, THIAZIDE); ADRENERGIC BETA-ANTAGONISTS; ADRENERGIC ALPHA-ANTAGONISTS; ANGIOTENSIN-CONVERTING ENZYME INHIBITORS; CALCIUM CHANNEL BLOCKERS; GANGLIONIC BLOCKERS; and VASODILATOR AGENTS. Anti-Hypertensive,Anti-Hypertensive Agent,Anti-Hypertensive Drug,Antihypertensive,Antihypertensive Agent,Antihypertensive Drug,Anti-Hypertensive Agents,Anti-Hypertensive Drugs,Anti-Hypertensives,Antihypertensive Drugs,Antihypertensives,Agent, Anti-Hypertensive,Agent, Antihypertensive,Agents, Anti-Hypertensive,Agents, Antihypertensive,Anti Hypertensive,Anti Hypertensive Agent,Anti Hypertensive Agents,Anti Hypertensive Drug,Anti Hypertensive Drugs,Anti Hypertensives,Drug, Anti-Hypertensive,Drug, Antihypertensive,Drugs, Anti-Hypertensive,Drugs, Antihypertensive
D051381 Rats The common name for the genus Rattus. Rattus,Rats, Laboratory,Rats, Norway,Rattus norvegicus,Laboratory Rat,Laboratory Rats,Norway Rat,Norway Rats,Rat,Rat, Laboratory,Rat, Norway,norvegicus, Rattus
D053778 Thiazolidines Reduced (protonated) form of THIAZOLES. They can be oxidized to THIAZOLIDINEDIONES. Thiazolidine

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