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PubMed2002

Relaxant effect of oxygen free radicals on rabbit tracheal smooth muscle.

We investigated the effect of exogenously generated superoxide anions (O(2)(-)), hydrogen peroxide (H(2)O(2)) and hydroxyl radicals (.OH) on isolated rabbit tracheal smooth muscle suspended in Krebs-Ringer solution. The ability of oxygen free radicals (OFRs) to affect acetyicholine (Ach)-induced contraction in these muscles was also investigated. OFRs, in general, produced a concentration-dependent relaxation of the tracheal smooth muscle in the doses used. However, in large concentrations, O(2)(-) and H(2)O(2) produced effects which were smaller than those obtained with lower concentrations. The relaxant effects of these oxyradicals were progressive and lasted throughout the 20min observation period. At all concentrations used, the OFRs tended to abolish or reduce Ach-induced contraction in a concentration-dependent manner. O(2)(-) was more potent than H(2)O(2) or DHF in relaxing the Ach-precontracted muscle and in inhibiting the response of the muscle to Ach. OFR-induced relaxation of the Ach-contracted muscle was not due to inactivation of the Ach by OFRs. Relaxation produced by OFRs was greater in preparations with intact epithelium than in those denuded of epithelium. The relaxant effects were blocked by indomethacin, a cyclooxygenase inhibitor. OFRs in the presence of indomethacin produced contraction only in the preparations with intact epithelium, suggesting a release of contractile factor(s) from epithelium. These results suggest that OFRs relax rabbit tracheal smooth muscle. The relaxation appears to be mediated through the synthesis and release of prostaglandins from the epithelium and smooth muscles.

Analysis of Variance↗
PubMedDate not supplied

Biphasic relaxant curves to glyceryl trinitrate in rat aortic rings. Evidence for two mechanisms of action.

The concentration-effect curve for the relaxant effects of glyceryl trinitrate (GTN) in rat aortic rings consisted of two phases with IC50 values of 0.1 microM for Phase I and 14 microM for Phase II. Incubation of tissues with oxyhaemoglobin or the induction of tolerance to GTN abolished responses occurring in Phase I but were without effect on Phase II relaxant responses. Both phases of the relaxant curve appeared to involve cyclic GMP since responses were (i) potentiated by the cyclic GMP phosphodiesterase inhibitor zaprinast (M & B 22948) and (ii) inhibited by methylene blue and LY83583, agents which inhibit soluble guanylate cyclase. The latter agents inhibited Phase I responses in a non-surmountable manner while Phase II responses were shifted to the right without effect on the maximal response. Neither phase of relaxation involved stimulation of the Na+/K+ ATPase pump since treatment of tissues with ouabain or K+-free solutions did not alter the GTN biphasic curve. Phase I relaxant responses to GTN resembled those to the endothelium-dependent relaxant acetylcholine, since oxyhaemoglobin and methylene blue were non-surmountable antagonists; however there was no cross tolerance to acetylcholine in GTN tolerant tissues. Phase II relaxant responses resembled those obtained with sodium nitroprusside (SNP) since neither oxyhaemoglobin nor the induction of tolerance to GTN altered the response to SNP. These results indicate that there are two distinct mechanisms of relaxation for GTN in rat aortic rings; however both mechanisms appear to involve cyclic GMP as the second messenger.

3',5'-Cyclic-GMP Phosphodiesterases↗
PubMedDate not supplied

Participation of nitric oxide in the relaxation of the rat gastric corpus.

Nitric oxide is an important mediator of the relaxation in the rat gastric fundus. The present study investigates the role of NO in the rat gastric corpus in vitro, since the corpus differs from the fundus with regard to its physiological function and its spontaneous motor behaviour. In the presence of guanethidine electrically induced relaxations of circular, mucosa-free corpus strips precontracted with bethanechol were concentration-dependently reduced by the NO-synthase inhibitors L-NG-nitro-arginine (L-NNA) or L-NG-nitro-arginine-methyl-ester (L-NAME). The D-enantiomers were markedly less active. The inhibitory effect of L-NAME could be prevented by L-arginine. L-NNA and L-NAME, however, did not influence spontaneous motility or the bethanechol-induced contraction. Vasoactive intestinal polypeptide or sodium nitroprusside also relaxed the muscle strips, but these relaxations were not affected by L-NAME. When the corpus strips were stimulated electrically from baseline, they reacted with a contraction followed by relaxation. L-NNA or L-NAME blocked the relaxatory and enhanced the contractile component. In strips that also reacted with a rebound contraction, it was blunted by L-NAME. These effects of the NO-synthase inhibitors were abolished in the presence of atropine. Apamin increased the electrically induced contraction of the muscle strips. Inhibition of the relaxation together with a further shift to contraction could only be seen when apamin was combined with L-NNA. The inhibitory action of apamin and apamin + L-NNA was not influenced by atropine. The results demonstrate a role of NO in the relaxation of the circular muscle of the rat gastric corpus both at a postsynaptic site and via inhibition of acetylcholine release. The relaxation induced by vasoactive intestinal polypeptide does not involve NO.

Animals↗
PubMed1991

The role of nitric oxide in serotonin-induced relaxations in the canine terminal ileum and ileocolonic junction.

The role of nitric oxide (NO) in 5-HT-induced non-adrenergic non-cholinergic (NANC) relaxations was studied on circular muscle strips of the canine ileocolonic junction (ICJ) and terminal ileum. During an acetylcholine-induced contraction, NO (10(-5) M) evoked a transient relaxation, whereas 5-HT (10(-4) M) caused an initial NANC relaxation followed by a contraction. This initial relaxation to 5-HT, but not the relaxation to NO, was significantly inhibited by the stereospecific inhibitors of the NO biosynthesis NG-monomethyl-L-arginine (L-NMMA) and NG-nitro-L-arginine (L-NNA). L-arginine, but not D-arginine, prevented the inhibitory effect of L-NMMA and L-NNA. The enantiomer of L-NMMA, D-NMMA, had no effect. Hemoglobin abolished the NO-induced relaxations and significantly inhibited the relaxation to 5-HT. From these experiments it is concluded that the 5-HT-induced NANC relaxation is mediated by NO or a NO releasing substance.

Acetylcholine↗
PubMed1990

Relaxation by adenosine and its analogs of potassium-contracted human coronary arteries.

The present study was an attempt to characterize the adenosine receptor in human coronary arteries, and to establish the dependence of the relaxations mediated by this receptor on a functional endothelium. Human coronary arteries were obtained from organ donors. Adenosine and its analogs (5'-N-ethyl-carboxamido-adenosine, NECA; N6-L-phenylisopropyladenosine, L-PIA; 2-chloroadenosine, CAD), all inhibited the contraction induced by 25 mmol/l KCl in a concentration-dependent manner and the order of potency was found to be: NECA greater than CAD greater than L-PIA greater than adenosine. These relaxations were antagonized by 8-phenyltheophylline (8PT). At higher concentrations of KCl, the relaxations were attenuated. In rings which relaxed in response to endothelium-dependent relaxing agents (bradykinin and A23187), NECA and CAD produced relaxations similar to those produced in rings which did not show endothelium-dependent responses. The results suggest that the coronary adenosine receptor (probably A2) mediates relaxations which may not be dependent on the relaxing function of the endothelium.

2-Chloroadenosine↗
PubMed1990

The rate of tetanic relaxation is correlated with the density of calcium ATPase in the terminal cisternae of thyrotoxic skeletal muscle.

The density of calcium ATPase was measured in the terminal cisternae of extensor digitorum longus (EDL) and soleus muscles from normal and thyrotoxic rats. The experiments tested the hypothesis that the rate of relaxation of these muscles following contraction, at temperatures above 22 C, is correlated with the density of calcium ATPase in the sarcoplasmic reticular membrane. In soleus fibres there was a progressive increase in calcium ATPase density, measured with immuno-electronmicroscopic techniques, of more than two-fold after 3 weeks of daily injections with triiodothyronine (T3). There was a parallel decrease in the relaxation time (from 80% to 20% of peak tension) of the tetanus: the parameters were closely correlated (r = 0.998) during the 3-week period. The rate of relaxation of the twitch also doubled and was correlated with the increase in gold particle density at the end of the 3-week injection period. However, twitch relaxation slowed during the 1st week of T3 injection and was not correlated with gold particle density at that time. The changes in calcium ATPase density and relaxation times in EDL fibres were small and largely insignificant. In contrast to relaxation, an increase in the rate of rise of tension is soleus was complete after only 2 weeks of T3 injection. The results show that the relaxation of tetanic tension is closely correlated with the calcium uptake capacity of the sarcoplasmic reticulum and that thyroid hormone acts more rapidly on factors regulating the rate of rise of tension than on those regulating tension relaxation and the density of calcium ATPase in the terminal cisternae.

Animals↗
PubMed1990

The role of transient internal sphincter relaxation in faecal incontinence?

Twenty-five (18%) of 140 incontinent patients and 6 (17%) of 35 normal controls showed episodes of spontaneous internal sphincter relaxation during 30 min multiport manometric and electromyographic recording under resting conditions. The episodes lasted at least 15 s and reduced the pressure in the outermost anal channels by at least 20 cm of water. Patients exhibited more episodes of relaxation than controls (4.3 +/- 0.6 vs 2.3 +/- 0.2 per subject; mean +/- SEM; p less than 0.05) and the pressures fell to lower values (19 +/- 1 vs 42 +/- 5 cm water, p less than 0.01), but the duration of relaxation was not significantly different (53 +/- 4 vs 40 +/- 7 s). Episodes of spontaneous relaxation were associated with simultaneous rectal contractions in 33% of the normal subjects and 45% of incontinent patients. Unlike normal subjects, most of the episodes of transient relaxation recorded in the incontinent group were not associated with compensatory increases in the electrical activity of the external anal sphincter (77% vs 17%; p less than 0.05). Over 50% of the incontinent patients who showed spontaneous relaxation also showed post squeeze or post-strain IAS relaxations whereas these were seen in less than 6% of the normal subjects with spontaneous relaxation.(ABSTRACT TRUNCATED AT 250 WORDS)

Adult↗
PubMed1988

Influence of pH on isometric force development and relaxation in skinned vascular smooth muscle.

The effects of pH (from pH values 6.50-7.10) on isometric tension development and relaxation were investigated in Triton X-100 "skinned" rat caudal artery. Helically cut skinned strips contracted in 21 microM Ca2+ were studied with respect to maximal isometric tension (Po) and rate of contraction (T0.5 C), and following relaxation in 18 nm Ca2+, the rate of relaxation (T0.5 R). Acidic pH (pH 6.50) decreased Po to 87% of isometric force obtained at pH 6.90, and increased the rate of contraction as shown by a decrease of T0.5 C to 80%. In contrast, T0.5 R increased 4.5-fold, indicating that with a change of only 0.40 pH units, relaxation rates were dramatically decreased. pCa-tension curves at pH values 6.50, 6.70, 6.90 and 7.10 indicated no significant shift in half maximal activation (pCa50) between pH 6.50 and 6.70, but a significant (P less than 0.01) shift in pCa50 between pH 6.70 [( Ca2+] = 0.46 microM) and pH 7.10 [( Ca2+] = 0.87 microM). Compared to contractions at pH 6.90, myosin light chain (LC20) phosphorylation at pH 6.50 was significantly greater at 30 and 60 s into contraction but not significantly different at 3-10 min. At both pH 6.50 and 6.90, dephosphorylation was rapid and substantially preceded relaxation; LC20 dephosphorylation and relaxation occurred more rapidly at pH 6.90 than at 6.50. At pH 6.50 and 6.90, relax solutions made with increased Ca2+ buffering capacity showed no effect in enhancing T0.5 R, suggesting the difference between relaxation rates was not due to Ca2+ diffusion limitations from the skinned strip.(ABSTRACT TRUNCATED AT 250 WORDS)

Animals↗
PubMed1981

Relaxation of tetanized canine tracheal smooth muscle.

As is the case for striated muscle, relaxation in smooth has been little studied and is less understood. We report studies of load bearing capacity during relaxation of airway smooth muscle. The model employed was the canine tracheal smooth muscle (TSM). The effect of load on the time course of relaxation was analyzed either by comparing afterloaded contractions against various loads or by imposing abrupt alterations in load (load clamps). Unlike mammalian cardiac muscle in which relaxation was reported sensitive to loading conditions, relaxation in TSM was largely independent of loading conditions. In this it resembled frog heart muscle and mammalian cardiac muscle cells without functioning calcium sequestering systems. This type of relaxation which is not influenced by manipulation of loading conditions, has been termed "inactivation-dependent' relaxation. It appears to operate in muscle tissue in which the calcium sequestering apparatus is poorly developed and the dissipation of activation (removal of activating calcium, detachment of force generating sites, etc.) appears to be the rate limiting step during relaxation.

Animals↗
PubMed1984

The process of muscle relaxation by the combined action of MgAMPPNP and ethylene glycol.

Insect flight muscle fibres were relaxed by the combined action of MgAMPPNP and ethylene glycol, as measured by the stiffness of the fibres. Relaxation occurred over a small range of glycol concentration. Addition of Ca2+ raised the glycol required for relaxation. The speed at which the stiffness measurement was made did not influence the glycol concentration at which relaxation occurred. Glycol in excess of that needed to relax the muscle caused a slight rise in high-frequency stiffness. Removal of the glycol restored the rigor stiffness. Under glycol-relaxed conditions, much of the AMPPNP bound in muscle fibres was retained during cold-chase (elution of [3H] AMPPNP by nonradioactive AMPPNP); the intensity ratio of the inner equatorial X-ray diffraction peaks rose upon glycol relaxation to a value slightly below that characteristic of natural relaxation. The results are interpreted in terms of cooperative attachment of the crossbridges to actin.

Adenosine Triphosphate↗
PubMed1987

The role of lysolecithin in the relaxation of vascular smooth muscle.

The effect of lysolecithin (lysophosphatidylcholine) on the relaxation of rabbit aortic strip closely resembled that produced by acetylcholine (ACh) which releases the endothelium-derived relaxing factor (EDRF). Relaxation induced by lysolecithin depended on the presence of endothelium and was inhibited by hemoglobin and methylene blue. It appeared to be mediated by the second messenger, c-GMP. Lysolecithin induced relaxation was slower but more persistent than that resulting from the endothelium-derived relaxing factor (EDRF) produced by acetylcholine (ACh). Like lysolecithin, Triton X-100, a non-ionic detergent, also preferentially relaxed aortic strips with intact endothelium. The results demonstrate the importance of phospholipids derived from cell membranes in vascular smooth muscle relaxation. Endothelium-derived relaxing factors appear as a group of heterogeneous substances.

Animals↗
PubMed1992

Saphenous vein endothelium-dependent relaxation in patients with peripheral vascular disease.

In vitro vasomotor responses of saphenous veins of 15 patients undergoing peripheral vascular bypass procedures were studied. Vessels were harvested by standard techniques, sectioned into 4 mm rings, and suspended in organ baths under isometric tension. Stimulation with cumulative doses of norepinephrine revealed a -logED50 of 6.85 +/- 0.12 M and maximal tension of 8.64 +/- 1.77 g. Patient characteristics suggesting high maximal response (by univariate analysis) included male sex (male 11.69 +/- 2.49 g versus female 5.08 +/- 1.69 g; p = 0.058). Intact and denuded rings were additionally tested for endothelium-dependent relaxation following submaximal norepinephrine precontraction. The vessels relaxed in response to acetylcholine (maximal relaxation 31.1 +/- 10.7% at 1 x 10(-6) M), calcium ionophore A23187 (85.3 +/- 11.8% at 1 x 10(-5) M), and sodium nitroprusside (150.8 +/- 15.2% at 1 x 10(-5) M), but only acetylcholine relaxation was completely endothelium-dependent. Calcium ionophore A23187 relaxation was partially dependent on the endothelium while sodium nitroprusside relaxation was entirely endothelium-independent. Negligible relaxation was observed in response to adenosine diphosphate (ADP) (12.1 +/- 12.8% at 1 x 10(-5) M) while histamine and serotonin caused additional contraction only. We concluded that, in patients undergoing vascular surgical procedures, the saphenous vein (1) demonstrates variable contractile function which appears to be greater in males following spinal anesthesia, and (2) exhibits moderate endothelium-dependent relaxation in response to acetylcholine and calcium ionophore A23187 but not to ADP, histamine, or serotonin.

Acetylcholine↗
PubMed1996

Relaxation: mapping an uncharted world.

Nine hundred and forty practitioners of massage, abbreviated progressive muscle relaxation (PMR), yoga stretching, breathing, imagery meditation, and various combination treatments described their technique experiences on an 82-item wordlist. Factor analysis yielded 10 interpretable relaxation categories: Joyful Affects and Appraisals (Joyful), Distant, Calm, Aware, Prayerful, Accepted, Untroubled, Limp, Silent, and Mystery The relaxation response and cognitive/somatic specificity models predict Calm and Limp, which account for only 5.5% of the variance of relaxation experience. Unlike much of previous relaxation research, we found important technique differences. PMR and massage are associated with Distant and Limp; yoga stretching, breathing, and meditation with Aware; meditation with Prayerful and all techniques except PMR with Joyful. Results are consistent with cognitive-behavioral relaxation theory and have implications for relaxation theory, treatment, training, assessment, and research. We close with a revised model of relaxation that posits three global dimensions; tension-relief, passive disengagement, and passive engagement.

Adult↗
PubMed1982

Neural and humoral factors influence gastric receptive relaxation in dogs.

To clarify the neural and humoral factors which control gastric receptive relaxation, the effects of various types of vagotomy or splanchnicotomy on receptive relaxation of the canine innervated corpus pouch were investigated. The influence of gastrin, histamine H1-receptor antagonist, and anti-histamine releasing agents on receptive relaxation were also examined. Selective proximal vagotomy or splanchnicotomy resulted in a slight disturbance in receptive relaxation. Truncal vagotomy produced a marked disturbance in receptive relaxation. Administration of tetragastrin potently inhibited receptive relaxation, however, recovery occurred by injecting a histamine H1-receptor antagonist. Increased serum gastrin induced by perfusion of the antrum with liver extract solution disturbed receptive relaxation and this response was inhibited by pretreatment with transamine, an inhibitor of histamine release from histamine secreting cells. These results indicate that receptive relaxation in the canine stomach is controlled not only by vagal and splanchnic nerves, but also by gastrin and histamine.

Animals↗
PubMed1997

Isoflurane inhibits endothelium-mediated nitric oxide relaxing pathways in the isolated perfused rabbit lung.

PURPOSE: The role of volatile anaesthetics on nitric oxide (NO)-dependent relaxation is unclear in the pulmonary circulation. We examined the effects of isoflurane on NO-dependent relaxation in isolated perfused rabbit lungs. METHODS: Eighteen rabbit lungs were perfused in a constant-flow recirculation manner. In study 1 (n = 12), acetylcholine (ACh, 4 x 10(-10)-10(-8) M) or nitroglycerine (NTG, 6 x 10(-10)-10(-8) M) was cumulatively injected into the pulmonary artery in the absence or presence of isoflurane (1, 2 MAC). In study 2 (n = 6), ACh was injected as in study 1 in the presence or absence of N omega-nitro-L-arginine methyl ester (L-NAME, 100 microM), an NO synthesis blocker. In all experiments, indomethacin was administered to prevent formation of vasoactive prostanoid metabolites, and the pulmonary vessels were preconstricted with prostaglandin F2 alpha (PGF2 alpha) infused before ACh or NTG injection. The ACh- or NTG-induced relaxation was expressed as % decrease in PGF2 alpha preconstriction. RESULTS: Isoflurane at 2 MAC attenuated the dose-dependent relaxation to ACh at doses of 4 x 10(-9) M and 4 x 10(-8) M from 27.8 +/- 4.3% and 38.8 +/- 5.3% to 17.0 +/- 3.5% and 25.5 +/- 4.9%, respectively (P < 0.05). Isoflurane did not change the dose-dependent relaxation to NTG and L-NAME abolished the ACh-induced relaxation. CONCLUSION: Isoflurane inhibited NO-dependent relaxation in the pulmonary circulation at a site distal to the endothelial cell receptor-mediated responses but proximal to guanylate cyclase activation of vascular smooth muscle. Acetylcholine-induced relaxation in isolated perfused rabbit lungs was regulated primarily by NO.

Acetylcholine↗
PubMed1997

Evidence for muscarinic M4 receptors mediating nonadrenergic noncholinergic relaxations in rabbit anococcygeus muscle.

The aim of the present study was to characterize the muscarinic receptor subtype mediating nonadrenergic noncholinergic (NANC) relaxations in the rabbit anococcygeus muscle (RAM) by the use of muscarinic receptor agonists and a battery of key muscarinic antagonists. In addition, experiments were carried out to identify the NANC neurotransmitter(s) involved in the inhibitory NANC neurotransmission. In preparations with histamine-raised tone, the nonselective muscarinic agonists (pD2 values) (+)-muscarine (5.23), cis-dioxolane (5.16), oxotremorine M (4.95) and carbachol (4.06) produced concentration-dependent relaxations corresponding to 72.6-85.0% of the histamine-induced precontraction. In contrast, the subtype-preferring (M1/M4 over M2 and M3 receptors) agonists 4-(3-chlorophenylcarbamoyloxy)-2-butynyltrimethylammonium chloride (McN-A-343), (S)-4-(dimethylamino)-1-methyl-2-butynyl-N-(3-chlorophenyl)carbamate methobromide [(S)-BN 228], (R)- and (S)-N-methyl-N-(1-methyl-4-pyrrolidino-2-butynyl)acetamide [(R)- and (S)-BM 5] showed no or rather low [(S)-BN 228] muscarinic activity. The low potencies, together with the ineffectiveness of some agonists, indicated a low effective receptor reserve associated with the relaxant response. No contractile responses to (+)-muscarine were observed neither in unstimulated nor in precontracted preparations suggesting that the existence of an excitatory postjunctional muscarinic receptor may be excluded. The nicotinic antagonist hexamethonium had no influence on relaxant responses to (+)-muscarine, but abolished relaxations elicited by (-)-nicotine. This demonstrates that the RAM contains also nicotinic acetylcholine receptors (AchRs) mediating inhibitory NANC responses. Relaxations induced by the stimulation of muscarinic and nicotinic AchRs as well as by electrical field stimulation (EFS) were completely abolished by tetrodotoxin and were also sensitive to the nitric oxide (NO) synthase inhibitor N(G)-nitro-L-arginine (L-NOARG), indicating that NO plays an important role as an inhibitory NANC transmitter in RAM. All muscarinic antagonists investigated did not influence the histamine-induced precontraction, but shifted the concentration-response curve of (+)-muscarine to the right in a parallel fashion. Schild analysis yielded regression lines of unit slope, indicating competitive antagonism. The following rank order of antagonist potencies (pA2 values) was found: 11-([4-[4-(diethylamino)-butyl]-1-piperidinyl]-acetyl-5,11-dihydro-6H-py rido (2,3-b) (1,4)-benzodiazepine-6-one hydrochloride (AQ-RA 741; 8.08) = himbacine (8.03) > or = tripitramine (7.69) > or = p-fluorohexahydro-sila-difenidol (p-F-HHSiD; 7.48) > or = methoctramine (7.30) > or = pirenzepine (7.18) > or = guanylpirenzepine (6.24). A comparison of the pA2 values determined in the RAM with published data from binding studies at muscarinic M1-M4 and m5 receptors suggests that the functional muscarinic receptor mediating NANC relaxation in the RAM is of the M4 subtype. Taken together, the results obtained in the present study provide convincing evidence that relaxant responses elicited by muscarinic stimuli in RAM are nitrergic in nature and mediated by muscarinic M4 receptors located somadendritically on NANC neurons. Thus, the isolated RAM may serve as a functional muscarinic M4 receptor model.

Animals↗
PubMed1998

Relaxant effect of the calcitonin gene-related peptide (CGRP) on the nonpregnant and pregnant rat uterus. Comparison with vascular tissue.

To explore the role of calcitonin gene-related peptide (CGRP) in rat pregnancy, we determined the density of myometrial CGRP-encoded nerve fibre terminals and examined, in an organ bath, the relaxant effect of the peptide on uterine strips near parturition. Comparisons were made with the uterus and aorta of nonpregnant rats. In the myometrium, CGRP immunoreactive nerve fibers were abundant in nonpregnant rats and scarce at the parturient stage. In the aorta there was no variation in the density of CGRP fibres with gestation. In nonpregnant rats only, CGRP relaxed spontaneous and tetrodotoxin (TTX)-sensitive electrically-evoked uterine contractions (EC50 40 nM, Emax 80%). The effect was antagonized by CGRP[8-37] (pKB 6.47) but was not affected by either blockers of nitricoxid synthase or ATP-sensitive potassium channels. CGRP was also able to relax contractions evoked by direct depolarization of the cells (TTX-insensitive contractions) (EC50, 2 nM, Emax 70%). In aorta contracted with arginine vasopressin, CGRP-induced relaxation was the same in nonpregnant and parturient animals. It was antagonized by CGRP [8-371 (pKB 6.90) and was abolished in presence of the nitric oxide synthase inhibitor Nomega-nitro-L-arginine methyl ester (L-NAME). Amylin neither relaxed the uterus nor the aorta. In pregnant rats, the relaxant effect of CGRP on the uterus was limited on day 21 and was totally absent on day 22 of gestation. We conclude that the primary relaxant effect of CGRP on the uterus occurs at the level of myometrial smooth muscle cells. In the myometrium, gestation decreases CGRP innervation and impairs the relaxant responses to CGRP. Such changes are not observed in vascular tissues like aorta.

Animals↗
PubMed1997

Incomplete upper esophageal sphincter relaxation: association with achalasia but not other esophageal motility disorders.

Incomplete upper esophageal sphincter (UES) relaxation is not well understood. We compared clinical and manometric characteristics of patients with normal and abnormal UES relaxation. Consecutive patients (n = 208) underwent manometric evaluation of the lower esophageal sphincter (LES), esophageal body, and UES/pharynx. The patients were divided into those with abnormal UES relaxation (residual pressure > 6.7 mmHg) (n = 21) and normal relaxation (n = 187). Clinical and manometric profiles were compared. Sex, age, and presenting complaint did not correlate with UES relaxation. Normal esophageal peristaltic sequences were more frequently present in the normal UES group (73.6%) compared with the abnormal (55.8%) (p < 0.01). The UES relaxation was shorter in the group with abnormal relaxation (410.0 ms vs. 510.2 ms, p < 0.001). All other manometric parameters were not different between the two groups. When individual manometric diagnoses were analyzed, only achalasia was noted to be more common in the abnormal UES group (23.8% vs. 9.1%, p < 0.05), and a trend was noted toward diffuse esophageal spasm being more common (14.3% vs. 9.6%, not significant). We conclude that incomplete UES relaxation is a rare manometric finding, associated with achalasia and not specifically associated with any other motility disturbance. This finding may represent a secondary response to the poor esophageal emptying seen in achalasia.

Deglutition Disorders↗