Cardiovascular effects of peptide kinin B2 receptor antagonists in rats

2002 ◽  
Vol 80 (4) ◽  
pp. 310-322 ◽  
Author(s):  
F Carini ◽  
M Guelfi ◽  
A Lecci ◽  
M Tramontana ◽  
S Meini ◽  
...  

Bradykinin (BK) is a vasoactive peptide reputed to play an important role in cardiovascular homeostasis. In this study, we describe the cardiovascular changes (mean blood pressure (BP) and heart rate (HR)) induced by the i.v. administration (left jugular vein) of two selective kinin B2 receptor antagonist, namely icatibant (0.1–1 µmol/kg as a bolus) and MEN11270 (0.1–1 µmol/kg as a bolus or 1 µmol/kg infused in 15 or 60 min), in urethane-anaesthetized or conscious rats with an indwelling catheter implanted in the right carotid artery for BP measurements. In conscious rats, icatibant at 0.1 or 0.3 µmol/kg did not change BP but at 0.1 µmol/kg increased HR at 30 min from administration. MEN11270 at 0.1 or 0.3 µmol/kg induced a dose-related increase in BP and a concomitant bradycardia (significant at 0.3 µmol/kg) lasting for 5 or 30 min, respectively. Icatibant at 1 µmol/kg induced a slight (P < 0.05) increase in BP that resolved in 5 min and a biphasic tachycardia (peaks at 30 and 90 min from administration). MEN11270 at 1 µmol/kg induced a triphasic change in HR (tachycardia in the first 5 min, bradycardia at 30 min, and tachycardia at 90 and 120 min) and a biphasic change in BP (hypotension at 15 min and hypertension at 30 min). The i.v. infusion of MEN11270 (1 µmol/kg in 15 or 60 min) produced hypertension, whereas HR was increased only following the 15-min infusion. In urethane-anaesthetized rats, both icatibant and MEN11270 (0.1 µmol/kg as a bolus) increased BP and the onset for this effect was correlated with the time course of the antagonism of BK-induced hypotension, where the effect of MEN11270 was more rapid than that of icatibant. These results indicate that kinin B2 receptor antagonists can induce acute cardiovascular effects, and the reason for the different haemodynamic profile between icatibant and MEN11270 could be putatively attributed to kinetic characteristics.Key words: icatibant, MEN11270, bradykinin, blood pressure, heart rate.

1980 ◽  
Vol 59 (s6) ◽  
pp. 295s-297s ◽  
Author(s):  
G. Haeusler ◽  
R. Osterwalder

1. Substance P, injected into a lateral brain ventricle of urethane-anaesthetized rats, caused dose-dependent increases in blood pressure and heart rate. 2. By contrast, exposure of the obex region of the medulla oblongata to pieces of filter paper soaked in substance P-containing solution resulted in falls of blood pressure and heart rate in both rats and cats. 3. A more precise application of substance P to the first synapse of the baroreceptor reflex by micro-injection into defined areas of the nucleus of the solitary tract also led to an activation of the baroreceptor reflex. 4. Capsaicin, which is known to release substance P from primary afferents, mimicked the sympatho-inhibitory and cardiovascular effects of substance P when applied locally to the nucleus of the solitary tract. 5. The results are compatible with a transmitter or neuromodulatory role for substance P at the first synapse of the baroreceptor reflex.


2013 ◽  
Vol 68 (5-6) ◽  
pp. 181-190 ◽  
Author(s):  
Paulo J. C. Anjos ◽  
Aline O. Lima ◽  
Patrícia S. Cunha ◽  
Damião P. De Sousa ◽  
Alexandre S. C. Onofre ◽  
...  

Linalool is a monoterpene alcohol and constituent of several Brazilian aromatic medicinal plants, popularly used against hypertension. Cardiovascular effects induced by linalool were evaluated. In normotensive rats, (±)-linalool [1, 5, 10, and 20 mg/kg body weight (BW); intravenous (i.v.)]-induced hypotension was associated with tachycardia, which was attenuated by atropine (2 mg/kg BW) and NG-nitro-L-arginine methyl ester (20 mg/kg BW), but was not modified after indomethacin (5 mg/kg BW) administration. In hypertensive rats, linalool [200 mg/kg BW; oral (v.o.)] reduced blood pressure without changing the heart rate. In intact rings of rat mesenteric artery precontracted with 10 μM phenylephrine, linalool (from 6.4 · 10 - 6 to 6.4 · 10 - 3 M) induced relaxations in a concentration-dependent manner [Emax = (115 ± 13)%] that were not changed after atropine administration [Emax = (105 ± 2)%], and were not different from those obtained in endothelium-denuded rings precontracted with phenylephrine [Emax = (108 ± 7)%] or 80 mM KCl [Emax = (113 ± 7)%] or tetraethylammonium incubation [Emax = (105 ± 12)%]. Linalool (1.9 · 10- 3 M) antagonized the contractions induced by CaCl2 (3 · 10 - 6 - 10 - 2 M) (maximal inhibition, 81%). Furthermore, linalool inhibited the contractions induced by 10 μM phenylephrine or 20 mM caffeine. In conclusion, these results demonstrate that linalool reduces blood pressure probably due to a direct effect on the vascular smooth muscle leading to vasodilation.


1980 ◽  
Vol 59 (s6) ◽  
pp. 235s-237s ◽  
Author(s):  
R. W. Rockhold ◽  
J. T. Crofton ◽  
L. Share

1. The cardiovascular effects of an enkephalin analogue were examined in spontaneously hypertensive and normotensive Wistar-Kyoto rats. (D-Ala2)-methionine enkephalin caused a biphasic increase in blood pressure and an increase in heart rate after intracerebroventricular injection. 2. The initial pressor response to (D-Ala2)-methionine enkephalin was greater in hypertensive than in normotensive rats. No difference was noted between groups during the secondary pressor response. Heart rate increases paralleled the secondary increase in blood pressure. 3. Naloxone pretreatment abolished the secondary increase in blood pressure and the tachycardia, but did not blunt the initial pressor response in female Wistar-Kyoto rats. 4. Plasma levels of arginine vasopressin were depressed during the plateau phase of the pressor response in hypertensive rats given intracerebroventricular (d-Ala2)-methionine enkephalin. 5. The results suggest that the cardiovascular effects of central enkephalin are not due to vasopressin, but may involve activation of the sympathetic nervous system.


PEDIATRICS ◽  
1989 ◽  
Vol 83 (2) ◽  
pp. 240-243
Author(s):  
Myung K. Park ◽  
Da-Hae Lee

Indirect BP measurement was obtained in the right upper arm in 219 healthy newborn infants with the Dinamap monitor and was compared with values obtained from the calf to establish normative BP values and to help establish a diagnosis of hypertension and coarctation of the aorta in the newborn. There were 174 Mexican-Americans (79.5%), 33 whites (15.0%), and 12 blacks (5.5%). The width of the BP cuff was selected to be 0.4 to 0.5 times the circumference of the extremities. Three supine position readings of BPs and heart rate were obtained from each site and were averaged for statistical analyses. Mean arm BP values (±SD) of the neonate less than 36 hours of age were 62.6±6.9/38.9± 5.7 mm Hg (48.0±6.2 mm Hg). Neonates older than 36 hours had slightly but significantly (P&lt;.05) greater values (4 to 6 mm Hg) than did infants younger than 36 hours of age. Active neonates had values 6 to 10 mm Hg greater than quiet neonates (P&lt;.05). BP values in the calf obtained with the same-sized cuff were almost identical with those obtained from the arm. Differences in consecutively obtained arm and calf BPs (arm values minus calf values) were 1.1±7.7 mm Hg systolic, -0.01 ± 6.2 mm Hg diastolic, and 0.9 ±6.9 mm Hg mean pressures. Mean heart rate (±SD) of neonates less than 36 hours of age was 129.4± 13.2 beats per minute and that of neonates older than 36 hours of age was 139.4± 14.1 beats per minute. These results show the following: (1) arm BPs and calf BPs using the same-sized cuff are almost identical with mean values of approximately 65/ 41 mm Hg (50 mm Hg) in neonates one to three days of age, (2) arm BP of 75/49 mm Hg (59 mm Hg) or greater is in the hypertensive range, and (3) calf BPs that are less than arm BPs by mean + 1 SD (6 to 9 mm Hg) necessitate a thorough investigation for coarctation of the aorta.


2021 ◽  
pp. 1-7
Author(s):  
Tércio A.R. Barros ◽  
Wagner L. do Prado ◽  
Thiago R.S. Tenório ◽  
Raphael M. Ritti-Dias ◽  
Antônio H. Germano-Soares ◽  
...  

This study compared the effects of self-selected exercise intensity (SEI) versus predetermined exercise intensity (PEI) on blood pressure (BP) and arterial stiffness in adolescents with obesity. A total of 37 adolescents, 14.7 (1.6) years old, body mass index ≥95th percentile were randomly allocated into SEI (n = 18; 12 boys) or PEI (n = 19; 13 boys). Both groups exercised for 35 minutes on a treadmill, 3 times per week, for 12 weeks. The SEI could set the speed at the beginning of the sessions and make changes every 5 minutes. The PEI adolescents were trained at an intensity set at 60% to 70% of heart rate reserve. Brachial and central BP, pulse pressure, augmentation index, and carotid–femoral pulse wave were determined at baseline and after 12 weeks. Both groups reduced brachial systolic BP (SEI, Δ = −9 mm Hg; PEI, Δ = −4 mm Hg; P < .01), central systolic BP (SEI, Δ = −4 mm Hg; PEI, Δ = −4 mm Hg; P = .01), and central pulse pressure (SEI, Δ = −4 mm Hg; PEI, Δ = −3 mm Hg; P = .02) without differences between groups. No changes in the augmentation index and carotid–femoral pulse wave were observed in either group. The SEI induced similar changes in various cardiovascular outcomes compared with PEI in adolescents with obesity.


1993 ◽  
Vol 75 (2) ◽  
pp. 663-667 ◽  
Author(s):  
M. Saito ◽  
A. Tsukanaka ◽  
D. Yanagihara ◽  
T. Mano

The aim of this study was to clarify the relationship between sympathetic outflow to skeletal muscle and oxygen uptake during dynamic exercise. Muscle sympathetic nerve activity (MSNA) was recorded from the right median nerve microneurographically in eight healthy volunteers during leg cycling at four different intensities in a seated position for a 16-min bout. Work loads selected were 20, 40, 60, and 75% of maximal oxygen uptake (VO2max). Heart rate and blood pressure were measured during each exercise test. MSNA burst frequency was suppressed by 28% during cycling at 20% VO2max (23 vs. 33 bursts/min for control). Thereafter, it increased in a linear fashion with increasing work rate, with a significantly higher burst frequency during 60% VO2max than the control value. Both heart rate and mean blood pressure rose significantly during 20% VO2max from the control value and increased linearly with increased exercise intensity. During light exercise, MSNA was suppressed by arterial and cardiopulmonary baroreceptors as a result of the hemodynamic changes associated with leg muscle pumping. The baroreflex inhibition may overcome the muscle metaboreflex excitation to induce MSNA suppression during light exercise. These results suggest that during light exercise MSNA is inhibited, perhaps due to loading of the cardiopulmonary and arterial baroreflexes, and that during heavier exercise the increase in MSNA occurs as muscle metaboreflexes are activated.


Author(s):  
G.F. Stegmann

In humans the combined administration of epidural anaesthesia and inhalation anaesthesia may result in cardiovascular instability associated with decreases in heart rate and blood pressure. Anaesthesia was induced with a combination of midazolam / ketamine in 18 female pigs with a mean body weight of 24.9±5.9 kg scheduled for surgical removal of the liver. After tracheal intubation, anaesthesia was maintained on a circle rebreathing circuit with isoflurane. Epidural anaesthesia was administered with ropivacaine (AL-group, n=8) at 0.2 mℓ / kg of a 7.5 mg / mℓ solution to the anaesthetised animals. The A-group (n = 10) received isoflurane anaesthesia only. The vaporiser was set at 2.5 % for the A-group and 1.5 % for the AL-group. Heart rate, invasive systolic, diastolic, and mean arterial blood pressure were monitored. Comparisons were made between treatments and within treatments comparing variables during surgical preparation and abdominal surgery. Differences between treatments were not statistically significant (P > 0.05) during surgical preparation or during abdominal surgery. For within treatment groups, the differences between surgical preparation and abdominal surgery were statistically significant (P < 0.05) for heart rate in the A-group, but not statistically significant (P > 0.05) for the other variables. It is concluded that abdominal surgery may be associated with statistically significant changes in heart rate in isoflurane-anaesthetised pigs and that the combined administration of epidural ropivacaine may prevent statistically significant changes in HR during abdominal surgery.


2016 ◽  
Vol 29 (3) ◽  
pp. 543-552
Author(s):  
João Douglas Alves ◽  
Jorge Luiz de Brito Gomes ◽  
Caio Victor Coutinho de Oliveira ◽  
José Victor de Miranda Henriques Alves ◽  
Fabiana Ranielle de Siqueira Nogueira ◽  
...  

Abstract Introduction: Tai-Chi-Chuan and Yoga have becoming popular practices. However is unclear the cardiovascular effects, and if they present similar behavior to aerobic and resistance sessions. Objective: To evaluate the cardiovascular responses during the session and post-exercise hypotension (PEH) of Tai Chi Chuan (TS) and Yoga (YS) in comparison to aerobic (AS) and resistance (SR) exercises. Methods: Fourteen young women (22.3 ± 2 years) apparently healthy performed four sessions (AS, RS, TS and YS). The heart rate (HR), systolic (SBP) and diastolic blood pressure (DBP) were recorded at resting, during (every 10 minutes) and until 50 minutes of recovery. Results: AS, RS, TS e YS showed significant increase in HR compared to resting.AS at 10, 30 e 50 minutes in relation to RS, TS e YS. The RS in relation to TS and YS at 10, 30 and 50 minutes. No significant difference between TS and YS. SBP was significantly increased in AS, RS, TS e YS at 10, 30 e 50 minutes during the session, in relation to rest. AS was significantly higher at 30 e 50 minutes than RS and higher than TS and YS at 10, 30 e 50 minutes. No significant difference in DBP. For PEH, AS, RS and TS significantly reduced at 10, 30 and 50 minutes. YS reduced at 50 minutes. No significant diastolic PEH. Conclusion: TS and YS showed as safe alternatives of exercising in the normotensive young adult woman, despite having lower values, they promote similar hemodynamic behavior to AS and RS.


1992 ◽  
Vol 72 (3) ◽  
pp. 1039-1043 ◽  
Author(s):  
V. K. Somers ◽  
K. C. Leo ◽  
R. Shields ◽  
M. Clary ◽  
A. L. Mark

Recent evidence indicates that muscle ischemia and activation of the muscle chemoreflex are the principal stimuli to sympathetic nerve activity (SNA) during isometric exercise. We postulated that physical training would decrease muscle chemoreflex stimulation during isometric exercise and thereby attenuate the SNA response to exercise. We investigated the effects of 6 wk of unilateral handgrip endurance training on the responses to isometric handgrip (IHG: 33% of maximal voluntary contraction maintained for 2 min). In eight normal subjects the right arm underwent exercise training and the left arm sham training. We measured muscle SNA (peroneal nerve), heart rate, and blood pressure during IHG before vs. after endurance training (right arm) and sham training (left arm). Maximum work to fatigue (an index of training efficacy) was increased by 1,146% in the endurance-trained arm and by only 40% in the sham-trained arm. During isometric exercise of the right arm, SNA increased by 111 +/- 27% (SE) before training and by only 38 +/- 9% after training (P less than 0.05). Endurance training did not significantly affect the heart rate and blood pressure responses to IHG. We also measured the SNA response to 2 min of forearm ischemia after IHG in five subjects. Endurance training also attenuated the SNA response to postexercise forearm ischemia (P = 0.057). Sham training did not significantly affect the SNA responses to IHG or forearm ischemia. We conclude that endurance training decreases muscle chemoreflex stimulation during isometric exercise and thereby attenuates the sympathetic nerve response to IHG.


2011 ◽  
Vol 51 (5) ◽  
pp. 282
Author(s):  
Tjhin Wiguna ◽  
Sasanto Wibisono ◽  
Sudigdo Sastroasmoro ◽  
Fransiscus D. Suyatna

Objective To identify the cardiovascular effects of long-acting methylphenidate administered for twelve weeks in Indonesian children with ADHD.Methods This was an 18-week, time series study on children with ADHD who were given 20 mg of long-acting methylphenidate for twelve weeks. During the study period we made ten serial observations of the subjects, including before, during and 6 weeks following drug administration. We included drug naive children with ADHD between the ages of 7 – 10 years. Children with mental retardation and chronic physical or mental disorders were excluded. Blood pressure was measured by sphygmomanometer with a child’s cuff at the brachial artery. We also collected data on heart rate, side effects, complaints and other medications used during the study. Repeated analysis was performed on the data with a P level of 0.05.Results Twenty-one subjects were recruited for this study. Mean blood pressure fluctuated insignificantly during the research period, for both mean systolic and mean diastolic blood pressures (P=0.115 and P=0.059). Mean heart rate also fluctuated insignificantly (P=0.091). All fluctuations were within the normal ranges. During the study, there were complaints of dizziness, nausea, and gastrointestinal upset, but they were reportedly mild and disappeared before the second week of observation.Conclusion Administration of 20 mg long-acting methylphenidate for twelve weeks in children with ADHD altered mean blood pressures and heart rates, but within the normal range for children of their age. However, cardiovascular risk observation is still needed when administering methylphenidate to children with ADHD, especially for those using the medication long-term.[Paediatr Indones. 2011;51:282-7].


Sign in / Sign up

Export Citation Format

Share Document