Mechanism of prostaglandin E2-, F2alpha- and latanoprost acid-induced relaxation of submental veins. 1997

M Astin, and J Stjernschantz
Glaucoma Research Laboratories, Pharmacia and Upjohn, Uppsala, Sweden.

The mechanism of prostaglandin E2-, prostaglandin F2alpha- and latanoprost acid (13,14-dihydro-17-phenyl-18,19,20-trinor-prostaglandin F2alpha)-induced relaxation of the rabbit submental vein was studied. Prostaglandin E2 caused maximum relaxation of endothelin-1 precontracted vessels (EC50: 1.8 x 10(-8) M). Much of the relaxation could be abolished by denuding the endothelium with the nitric oxide synthase inhibitor, L-NAME (N(G)-Nitro-L-arginine methylester). CGRP-(8-37) (calcitonin gene-related peptide fragment (8-37)), a calcitonin gene-related peptide receptor antagonist, exhibited a partial blocking effect, whereas the tachykinin NK1 receptor blocker, GR 82334 ([D-Pro9[Spiro-gamma-Lactam]Leu10,Trp11]physalaemin (1-11)), markedly attenuated the response. Both prostaglandin F2alpha and the relatively selective FP receptor agonist, latanoprost acid, caused relaxation of the veins to about 50% of the precontracted state in the presence of GR 32191B ([1R-[1alpha(Z),2beta,3beta,5alpha]]-(+)-7-[5-([1,1'-b iphenyl]-4-ylmethoxy)-3-hydroxy-2-(1-piperidinyl)cyclopentyl]-4-he ptenoic acid), a thromboxane receptor antagonist (EC50: for prostaglandin F2alpha 7.9 x 10(-9) M, and for latanoprost acid 4.9 x 10(-9) M). L-NAME, as well as denuding the endothelium, completely abolished the effect. In addition, most or at least a large part of the relaxation was also blocked by CGRP-(8-37) as well as GR 82334. These results indicate that the FP receptor-mediated relaxation of veins is based on release of nitric oxide in addition to involvement of calcitonin gene-related peptide and substance P, or some other tachykinin, probably released from perivascular sensory nerves. The more pronounced relaxation induced by prostaglandin E2 could be due to vasodilator EP receptors in the smooth muscle layer of the veins.

UI MeSH Term Description Entries
D008297 Male Males
D009126 Muscle Relaxation That phase of a muscle twitch during which a muscle returns to a resting position. Muscle Relaxations,Relaxation, Muscle,Relaxations, Muscle
D009131 Muscle, Smooth, Vascular The nonstriated involuntary muscle tissue of blood vessels. Vascular Smooth Muscle,Muscle, Vascular Smooth,Muscles, Vascular Smooth,Smooth Muscle, Vascular,Smooth Muscles, Vascular,Vascular Smooth Muscles
D011461 Prostaglandins F, Synthetic Analogs or derivatives of prostaglandins F that do not occur naturally in the body. They do not include the product of the chemical synthesis of hormonal PGF. PGF Synthetic,Prostaglandin F Analogs,Prostaglandin F Analogues,Synthetic Prostaglandins F,Analogs, Prostaglandin F,Analogues, Prostaglandin F,Synthetic, PGF
D011817 Rabbits A burrowing plant-eating mammal with hind limbs that are longer than its fore limbs. It belongs to the family Leporidae of the order Lagomorpha, and in contrast to hares, possesses 22 instead of 24 pairs of chromosomes. Belgian Hare,New Zealand Rabbit,New Zealand Rabbits,New Zealand White Rabbit,Rabbit,Rabbit, Domestic,Chinchilla Rabbits,NZW Rabbits,New Zealand White Rabbits,Oryctolagus cuniculus,Chinchilla Rabbit,Domestic Rabbit,Domestic Rabbits,Hare, Belgian,NZW Rabbit,Rabbit, Chinchilla,Rabbit, NZW,Rabbit, New Zealand,Rabbits, Chinchilla,Rabbits, Domestic,Rabbits, NZW,Rabbits, New Zealand,Zealand Rabbit, New,Zealand Rabbits, New,cuniculus, Oryctolagus
D004791 Enzyme Inhibitors Compounds or agents that combine with an enzyme in such a manner as to prevent the normal substrate-enzyme combination and the catalytic reaction. Enzyme Inhibitor,Inhibitor, Enzyme,Inhibitors, Enzyme
D005260 Female Females
D000077221 Calcitonin Gene-Related Peptide Receptor Antagonists Pharmacologic agents that block NOCICEPTIVE PAIN signaling from CALCITONIN GENE-RELATED PEPTIDE RECEPTORS. They may be useful for the treatment of pain associated with MIGRAINE DISORDERS and OSTEOARTHRITIS. CGRP Receptor Antagonist,CGRP-R Inhibitor,CGRP-R Inhibitors,Calcitonin Gene-Related Peptide Receptor Antagonist,GEPANT,CGRP Receptor Antagonists,GEPANTS,Antagonist, CGRP Receptor,Antagonists, CGRP Receptor,CGRP R Inhibitor,CGRP R Inhibitors,Calcitonin Gene Related Peptide Receptor Antagonist,Calcitonin Gene Related Peptide Receptor Antagonists,Inhibitor, CGRP-R,Inhibitors, CGRP-R,Receptor Antagonist, CGRP,Receptor Antagonists, CGRP
D000077338 Latanoprost A prostaglandin F analog used to treat OCULAR HYPERTENSION in patients with GLAUCOMA. PHXA41,PhXA34,Xalatan
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

Related Publications

M Astin, and J Stjernschantz
April 1998, Journal of ocular pharmacology and therapeutics : the official journal of the Association for Ocular Pharmacology and Therapeutics,
M Astin, and J Stjernschantz
February 2002, Graefe's archive for clinical and experimental ophthalmology = Albrecht von Graefes Archiv fur klinische und experimentelle Ophthalmologie,
M Astin, and J Stjernschantz
January 1974, Gynakologische Rundschau,
M Astin, and J Stjernschantz
September 1977, Wiener medizinische Wochenschrift (1946),
M Astin, and J Stjernschantz
January 1974, Gynakologische Rundschau,
M Astin, and J Stjernschantz
April 1978, Pflugers Archiv : European journal of physiology,
M Astin, and J Stjernschantz
September 1976, Comprehensive therapy,
M Astin, and J Stjernschantz
January 1978, Journal of dental research,
M Astin, and J Stjernschantz
August 1976, Pflugers Archiv : European journal of physiology,
Copied contents to your clipboard!