Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0344307 (analgesia)
 28,200 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

The minimum region in salmon calcitonin (sCT) which induces antigenicity and gastrointestinal disturbances has been identified by examining the cross-reactivity of several sCT fragments and CT analogs with antisera from sCT-treated patients, and by examining inhibition of gastrointestinal motility of these sCT fragments and CT analogs in conscious dogs. Sixteen residues at the N-terminus of sCT comprised the minimum fragment capable of inducing both activities. Human CT (hCT) showed no antigenicity and a four-order weaker inhibition of gastrointestinal motility than sCT. Based on these data, we synthesized the human and salmon chimeric CT, ACT-15, in which the 16 N-terminal residues were those of hCT and the 16 C-terminal residues were those of sCT. ACT-15 had no cross-reactivity with the antisera and had almost the same weak gastrointestinal inhibition effect as hCT in dog and rat models. Nevertheless, it retained a hypocalcemic activity and an analgesic activity comparable to sCT. These results suggest that the amino acid residues in the N-terminal half of CT are responsible for the formation of antibodies and the induction of gastrointestinal disturbances, but may not influence calcium metabolism or analgesia. Clinical studies of ACT-15 will be needed to confirm this hypothesis.
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PMID:A chimeric analog of human and salmon calcitonin eliminates antigenicity and reduces gastrointestinal disturbances. 128 Feb 7

The analgesic action of calcitonin (0.25 MRC units.kg-1) injected into lateral cerebral ventricle was investigated in rats. The pain threshold was evaluated by the tail-flick test. The influences of icv naloxone 5 micrograms/rat, a blocker of opiate receptor, on the analgesic action of calcitonin were observed. The results showed that icv calcitonin produced a significant analgesic action, which was reversed by naloxone. While the pain threshold was raised by calcitonin, the contents of central monoamines (5-HT, NE, DA) in brain (diencephalon, brain stem) were examined by fluorophotometry, which were increased remarkably. It is suggested that calcitonin-induced analgesia is related to the opiate receptors and the contents of 5-HT, NE, and DA in CNS.
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PMID:[Central analgesic action of calcitonin and its relationship with central monoamine transmitters]. 135 Aug 81

We compared the analgesia induced by intraperitoneally (i.p.) and intracerebroventricularly (i.c.v.) administered salmon-calcitonin (S-CT), using the hot-plate test and the writhing test. The influence of the route of administration on the analgesia induced by morphine was also studied. After i.p. administration the analgesic effect was observed only in the writhing test. When S-CT was administered i.c.v., analgesia was observed in both tests, although it was greater in the writhing test than in the hot-plate test. I.c.v. injected S-CT increased the analgesia of i.p. injected morphine. Our results provide new information about the analgesic effect of S-CT and suggest that central mechanisms are involved.
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PMID:Analgesic effect of salmon-calcitonin administered by two routes. Effect on morphine analgesia. 145 45

Based on the important relationship of calcitonin and serotonin with narcotic drugs at the level of the central nervous system and with the modulating mechanisms of pain sensation, we have studied whether central baseline levels of these modulators possess a predictive value for the assessment of the intensity and duration of narcotic spinal analgesia. Therefore, intradural levels of calcitonin an serotonin were measured in 18 patients who underwent and infraumbilical laparotomy with intradural anesthesia with bupivacaine associated with 0.5 mg of morphine. There was no statistically significant correlation between the levels of calcitonin and serotonin with the age, weight, height, sex, values of analogic visual scale 2, 4, 6, 12 and 24 hours after lumbar punction, and duration of the analgesia. Even though a correlation exists in experimental models, our results indicate that baseline values of modulators calcitonin and serotonin lack of predictive value for the assessment of the degree and duration of narcotic spinal analgesia.
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PMID:[Lack of predictive power of cerebrospinal fluid calcitonin and serotonin concentrations for the intensity of postoperative pain and the duration of analgesia after subarachnoid morphine administration]. 159 86

To determine whether or not the CNS inhibitory activity of eel calcitonin (eCT) on adenylyl cyclase is the endocellular mechanism underlying the antinociceptive effect of the peptide, as shown for morphine analgesia, we administered Bordetella pertussis toxin (PTX) by intracerebroventricular (ICV) injection (0.5 microgram/rat) to block the receptor-mediated inhibition of adenylyl cyclase. In PTX-treated rats there was no change in eCT (2.5 micrograms/rat, ICV)-induced antinociceptive activity (hot-plate test) nor in eCT (100 ng/rat, ICV) inhibition of gastric acid secretion (Shay test) whereas morphine (5 micrograms/rat, ICV) analgesia was significantly reduced. In vitro studies showed no reduction of eCT binding in the CNS of rats treated with PTX in vivo. Moreover, PTX treatment did not change the inhibitory effect of eCT on adenylyl cyclase in isolated membranes from rat striatum in contrast with opiates (DAME and morphine) whose effects were lost. As PTX is known to inactivate the guanidine binding inhibitory protein Gi, these data suggest that a G protein, distinct from the Gi protein involved in the coupling of opiate receptors into a functional response, could be responsible for regulating the intracellular pathways resulting in eCT-induced antinociceptive effect and inhibition of gastric acid secretion.
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PMID:Treatment with pertussis toxin does not prevent central effects of eel calcitonin. 165 2

In osteoporosis, calcitonin exerts an analgesic effect that is unrelated to its effect on bone. Although the precise mechanism has yet to be clarified, there is some evidence that the analgesic effect of calcitonin may be mediated through the endogenous opioid system. The intranasal administration of calcitonin seems to be more effective in producing analgesia than parenteral administration.
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PMID:Use of calcitonin in the treatment of bone pain associated with osteoporosis. 193 18

Intracerebroventricular injection of pertussis toxin (PTX, 1 microgram/rat) six days before the hot plate test abolished analgesia induced by central morphine. The toxin did not affect analgesia evoked by central neurotensin or ASU 1-7 eel calcitonin. PTX pretreatment also attenuated footshock-induced analgesia (FSIA) delivered to all four paws. When the shock was restricted to the front paws, PTX consistently lowered postshock tail flick latencies, but did not reduce analgesia resulting from shock delivered to the hind paws. It thus appears that PTX-sensitive G-proteins are an essential transduction step needed to initiate the molecular events underlying opiate analgesia evoked by either morphine or shock. In contrast, the signal transduction mechanism subsequent to the stimulation of neurotensin or calcitonin receptors, and to the nonopiate FSIA, appears not to involve PTX-sensitive G-proteins.
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PMID:Pertussis toxin pretreatment affects opiate/nonopiate and stress-induced analgesia differently. 206 92

Peptides with hormonal or neuronal activity are derived by enzymatic processing from pro-hormones, which by themselves are biologically inert. Processing and other enzymatic conversions may occur step-wise, leading to the formation of a cascade of biologically active (or inactive) peptides. The neurokin in substance P is known to be metabolically transformed both by amino- and endopeptidases. More N-terminal substance (1-7) has been found than C-terminal (2-11 to 5-11) fragments in various CNS areas. The substance P (1-7) fragment also shows biological activity e.g., providing analgesia, lowering blood pressure, inhibiting aggressive behavior and (in contrast to substance P) inhibiting grooming behavior. An endopeptidase generating substance P (1-7) and to a lesser extent, substance (1-8), has been isolated and characterized from human cerebrospinal fluid (CSF) and bovine spinal cord, as a metalloenzyme with essential SH-groups. Substance P co-exists with calcitonin gene related peptide (CGRP) in a large population of non-myelinated primary afferent ('pain') fibers. Intrathecal injection of substance P causes behavioral and physiological responses which are potentiated and prolonged by CGRP. It was found that CGRP competes with substance P for the endopeptidase. It is suggested that the main action of CGRP in the spinal cord is to inhibit substance P degradation.
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PMID:Modulation of endopeptidase activity by calcitonin gene related peptide: a mechanism affecting substance P action? 245 90

In this study we have examined the results of salmon calcitonin treatment on migraine pain. The mechanism by which calcitonin induces analgesia is still not understood. We observed the effect of a 5-day treatment with salmon calcitonin (IM 100 IU/day) on circulating levels of beta-endorphin, ACTH, and cortisol in 20 patients with migraine during the headache-free period. All 3 hormones were increased after the calcitonin administration and the maximum increase was obtained in beta-endorphin levels. There were significant statistical correlations between beta-endorphin, ACTH, and cortisol levels determined before and after calcitonin treatment.
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PMID:Treatment of migraine with salmon calcitonin: effects on plasma beta-endorphin, ACTH and cortisol levels. 256 Apr 8

The effects of epidural analgesia on plasma calcitonin gene-related peptide (CGRP) values during and after hysterectomy were investigated in 14 healthy patients. In seven patients who received general anaesthesia alone for pelvic surgery, there were no significant changes in plasma CGRP concentrations. In the remaining patients, who received extensive epidural blockade in addition to general anaesthesia, there were again no significant changes in plasma CGRP values. This was in spite of profound sympathetic blockade, as shown by marked hypotension and a significant decline in plasma catecholamines. The epidural group of patients showed the expected attenuation of the glucose, cortisol and growth hormone responses to surgery. The results show that circulating CGRP is unlikely to be involved in the modulation of peripheral vascular tone during pelvic surgery under either general or epidural anaesthesia.
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PMID:Effects of epidural analgesia on plasma calcitonin gene-related peptide. 258 98


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