269 resultados para Agonist
Resumo:
Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)
Resumo:
Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)
Resumo:
JUSTIFICATIVA E OBJETIVOS: Verificar o efeito sedativo da clonidina, um a2-agonista, e do midazolam, um benzodiazepínico, quando utilizados na medicação pré-anestésica, empregando-se avaliação clínica e eletroencefalográfica bispectral. MÉTODO: Após aprovação institucional e consentimento escrito fornecido, 45 pacientes de 18 a 65 anos, estado físico ASA I, foram aleatoriamente distribuídos nos grupos placebo (P), clonidina (C) ou midazolam (M), em que receberam, respectivamente placebo, 150 µg de clonidina ou 15 mg de midazolam por via oral, 60 minutos antes da indução da anestesia (n = 15 por grupo). A monitorização constituiu-se de eletrocardiograma (D II), pressão arterial não invasiva, freqüência cardíaca, saturação de pulso de oxigênio, freqüência respiratória, temperatura axilar e da sala de cirurgia e eletroencefalograma bispectral para determinação do índice bispectral (BIS). Esses atributos e a escala de sedações (1 - ansioso, 2 - calmo, 3 - sonolento, 4 - dormindo com reflexo, 5 - dormindo sem reflexo) foram obtidos aos 0 (M0), 15 (M15), 30 (M30), 40 (M40), 50 (M50) e 60 (M60) minutos após a medicação. RESULTADOS: Nos grupos não houve alteração significante dos parâmetros respiratórios, hemodinâmicos e de temperatura. Houve diferença significante entre os grupos na ES (M60: M=C>P) e no BIS (M50 e M60: M=C>P). CONCLUSÕES: Nas condições utilizadas, a clonidina e o midazolam determinaram níveis de sedação adequados e semelhantes na medicação pré-anestésica de pacientes estado físico ASA I, quando avaliados pela escala de sedação e pelo índice bispectral, sem determinarem alterações hemodinâmicas e respiratórias.
Resumo:
We investigated whether or not surgical denervation of the rat vas deferens changes the alpha(1)-adrenoceptor subtypes involved in the contractions to noradrenaline. Denervated vas deferens was approximate to22 times more sensitive to noradrenaline (pD(2)=7.35 +/- 0.04) than control vas (pD(2)= 6.01 +/- 0.03). This difference in noradrenaline potency was eliminated when cocaine (6 muM) was added to control vas (pD(2)=7.22 +/- 0.04). The noradrenaline-induced contractions of control and denervated vas deferens were insensitive to the alpha(1B)/alpha(1D)-adrenoceptor alkylating agent chloroethylclonidine (100 muM, 45 min). The concentration-response curves to noradrenaline in control and denervated vas deferens were competitively antagonised by prazosin (pA(2)approximate to9.6), WB-4101 (pA(2)approximate to9.5), 5-methyl urapidil (pA(2)approximate to8.4), phentolamine (pA(2)approximate to8.7), yohimbine (pA(2)approximate to6.9), BMY 7378 (pA(2)approximate to6.9) and indoramin (pA(2)approximate to8.7). After the treatment of control and denervated vas deferens with phenoxybenzamine, the partial agonist oxymetazoline antagonised competitively the concentration-response curves to noradrenaline showing pA(2) values approximate to7.4 in both groups. We conclude that noradrenaline-induced contractions in control and denervated rat vas deferens are mediated by alpha(1A)-adrenoceptors and that surgical denervation of the rat vas deferens is not able to change the alpha(1)-adrenoceptor subtypes involved in the contractions to noradrenaline.
Resumo:
We investigated the effects of hydrocortisone during the prenatal period and its repercussion on puberty installation and adrenergic response of seminal vesicle in adult rats. The efficacy of the hydrocortisone treatment in reducing adrenal wet weight immediately after delivery in both the treated mothers and respective pups at birth may indicate impairment of the hypothalamus-pituitary-adrenal axis. This parameter was unchanged in the adult phase of these descendants, suggesting recuperation of this axis. In addition, the treatment with hydrocortisone delayed the age of puberty installation, probably by absence of both physiologic production and liberation of luteinizing hormone and testosterone. Despite the significant reduction in testosterone level as well as of wet weights of both vas deferens and testis in the adult phase, no difference was observed in the sensitivity of the seminal vesicle to the studied sympathetic agonist. However, the observed reduction in contractile response of the seminal vesicle may be a consequence of contractile-system damage in this organ. It is possible that this alteration may cause a reduction in the amount of vesicular secretion so important in the process of ejaculation. In conclusion, these results suggest that administration of hydrocortisone in late prenatal life did not influence the hypothalamus-pituitary-adrenal axis in adult life, although it altered the hypothalamus-pituitary-gonadal axis, and reduced testosterone production starting at puberty, as a consequence of an incomplete masculinization of the hypothalamus plus a reduction in the contractile response of the seminal vesicle. (c) 2005 Elsevier B.V. All rights reserved.
Resumo:
The aim of this study was to verify, by means of functional methods, whether the circadian rhythm changes adrenergic response patterns in the epididymal half of the vas deferens isolated from control rats as well as from rats submitted to acute stress. The experiments were performed at 9:00 a.m., 3:00 p.m., 9:00 p.m., and 3:00 a.m. The results showed a light-dark dependent variation of the adrenergic response pattern on organs isolated from control as well as from stressed rats. In the control group, only the phenylephrine sensitivity was changed throughout the circadian rhythm. Under the stress condition, both norepinephrine and phenylephrine response patterns were changed, mainly during darkness. The maximal contractile response to both alpha- and beta-agonist and alpha(1)-agonist was increased in the dark phase, corresponding to high plasmatic concentrations of endogenous melatonin. The vas deferens isolated from stressed rats during the light phase simultaneously incubated with exogenous melatonin showed the same pattern of response obtained in the dark phase, thus indicating a peripheric action of melatonin on this organ. Therefore, the circadian rhythms are important to the adrenergic response pattern in rat vas deferens from both control and stressed rats. In conclusion, we suggest a melatonin modulation on alpha(1)-postsynaptic adrenergic response in the rat vas deferens. (c) 2005 Elsevier B.V. All rights reserved.
Resumo:
The objective of this study was to evaluate protocols for synchronizing ovulation in beef cattle. In Experiment 1, Nelore cows (Bos indicus) at random stages of the estrous cycle were assigned to 1 of the following treatments: Group GP controls (nonlactating, n=7) received GnRH agonist (Day 0) and PGF2 alpha (Day 7); while Groups GPG (nonlactating, n=8) and GPG-L (lactating, n=9) cows were given GnRH (Day 0), PGF2a (Day 7) and GnRH again (Day 8, 30 h after PGF2 alpha). A new follicular wave was observed 1.79+/-0.34 d after GnRH in 19/24 cows. After PGF2a, ovulation occurred in 19/24 cows (6/7 GP, 6/8 GPG, 7/9 GPG-L). Most cows (83.3%) exhibited a dominant follicle just before PGF2a, and 17/19 ovulatory follicles were from a new follicular wave. There was a more precise synchrony of ovulation (within 12 h) in cows that received a second dose of GnRH (GPG and GPG-L) than controls (GP, ovulation within 48 h; P<0.01). In Experiment 2, lactating Nelore cows with a visible corpus luteum (CL) by ultrasonography were allocated to 2 treatments: Group GPE (n=10) received GnRH agonist (Day 0), PGF2a (Day 7) and estradiol benzoate (EB; Day 8, 24 h after PGF2 alpha); while Group EPE (n=11), received EB (Day 0), PGF2a (Day 9) and EB (Day 10, 24 h after PGF2a). Emergence of a new follicular wave was observed 1.6+/-0.31 d after GnRH (Group GPE). After EB injection (Day 8) ovulation was observed at 45.38+/-2.03 h in 7/10 cows within 12 h. In Group EPE the emergence of a new follicular wave was observed later (4.36+/-0.31 d) than in Group GEP (1.6+/-0.31 d; P<0.001). After the second EB injection (Day 10) ovulation was observed at 44.16+/-2.21 h within 12 (7/11 cows) or 18 h (8/11 cows). All 3 treatments were effective in synchronizing ovulation in beef cows. However, GPE and, particularly EPE treatments offer a promising alternative to the GPG protocol in timed artificial insemination of beef cattle, due to the low cost of EB compared with GnRH agonists. (C) 2000 by Elsevier B.V.
Resumo:
Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)
Two new bradykinin-related peptides from the venom of the social wasp Protopolybia exigua (Saussure)
Resumo:
Two bradykinin-related peptides (Protopolybiakinin-I and Protopolybiakinin-II) were isolated from the venom of the social wasp Protopolybia exigua by RP-HPLC, and sequenced by Edman degradation method. Peptide sequences of Protopolybiakinin-I and Protopolybiakinin-II were DKNKKPIRVGGRRPPGFTR-OH and DKNKKPIWMAGFPGFTPIR-OH, respectively. Synthetic peptides with identical sequences to the bradykinin-related peptides and their biological functions were characterized. Protopolybiakinin-I caused less potent constriction of the isolated rat ileum muscles than bradykinin (BK). In addition, it caused degranulation of mast cells which was seven times more potent than BK. This peptide causes algesic effects due to the direct activation of B-2-receptors. Protopolybiakinin-II is not an agonist of rat ileum muscle and had no algesic effects. However, Protopolybiakinin-II was found to be 10 times more potent as a mast cell degranulator than BK. The amino acid sequence of Protopolybiakinin-I is the longest among the known wasp kinins. (c) 2006 Elsevier B.V. All rights reserved.
Resumo:
Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)
Resumo:
The aim of the present study was to evaluate the potency and maximal responses (E-max) to the adenosine receptor agonists N-6-cyclopentyladenosine (CPA), N-ethylcarboxamidoadenosine (NECA) and N-6-(3-iodobenzyl)-5'-N-methylcarbaxamidoadenosine (IB-MECA) in right atria from trained rats. We also investigated the interaction between the training bradycardia and the sensitivity of the chronotropic response mediated by adenosine receptor stimulation.2. Animals were submitted to run training for 60 min, 5 days a week, over a period of 8 weeks. Mean blood pressure and heart rate were measured in conscious animals. Right atria were isolated and concentration-response curves to CPA, NECA and IB-MECA were obtained.3. A reduction in heart rate was found in trained rats, indicating that the training programme was successful in inducing physical conditioning. The three adenosine receptor agonists induced a concentration-dependent negative chronotropic response. The rank order of potency and E-max for the three adenosine receptor agonists was CPA>NECA>IB-MECA.4. Dynamic exercise for 8 weeks did not alter the E a, for CPA, NECA and IB-MECA. Similarly, the potencies of CPA and NECA were not affected by run training, whereas the potency of IB-MECA was reduced (6.10+/-0.09 vs 5.66+/-0.10 for sedentary and trained groups, respectively).5. In conclusion, run training for 8 weeks induced a desensitization of the chronotropic response to IB-MECA without changing the potency of CPA and NECA. These findings exclude the participation of adenosine receptors in the training bradycardia.
Resumo:
This study aimed to investigate the in vivo and in vitro reactivity of airway smooth muscle in rats depleted of sensory neuropeptides by treatment with capsaicin at neonatal stage. Wistar rats were neonatally injected with either capsaicin (50 mg/kg, s.c., 2nd day of life) or its vehicle (10% ethanol and 10% Tween 80, in 0.9% w/v NaCl solution) and used at adult ages (60-70 days later). Analysis of the lungs showed a higher number of infiltrating neutrophils, eosinophils and mononuclear cells into the peribronchiolar regions of capsaicin-pretreated rats compared to vehicle group. This was associated with a higher contraction index of bronchiolar wall in the capsaicin group. The in vitro tracheal reactivity in response to methacholine (full muscarinic agonist) and pilocarpine (partial muscarinic agonist) was also significantly higher in capsaicin-pretreated rats compared to vehicle group. In conclusion, the neuropeptide depletion by capsaicin neonatal treatment lead to marked contraction of the rat airways at adult age, suggesting a protective role for C fibers in the lungs. (C) 2003 Elsevier B.V. Ireland Ltd. All rights reserved.
Resumo:
Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)
Resumo:
Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)
Resumo:
Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)