Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts:   Target Concepts:
Query: UMLS:C0020672 (hypothermia)
 17,327 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

The pharmacological properties of the 5-hydroxytryptamine (HT)(1A) receptor agonist (R)-3,4-dihydro-N-isopropyl-3-(N-isopropyl-N-propylamino)-2H-1-benzopyran-5-carboxamide (NAE-086) were examined with in vitro and in vivo techniques. Receptor binding studies demonstrated that NAE-086 was a high-affinity and selective 5-HT(1A) receptor ligand with a K(i) value of 4.5 nM in membranes from rat hippocampus. Of 32 other receptors examined NAE-086 had a modest affinity only for the 5-HT(7) receptor (K(i) = 240 nM). NAE-086 inhibited VIP-stimulated adenylyl cyclase activity in GH(4)ZD10 cells with 79% of the efficacy of 5-HT. This inhibition was blocked by the 5-HT(1A) receptor (and beta-adrenoceptor) antagonist (-)alprenolol. A minor metabolite of NAE-086 in rats, (R)-3,4-dihydro-3-(N-isopropyl-N-propylamino)-2H-1-benzopyran-5-carboxamide had a similar receptor profile but had 17 times higher affinity for the 5-HT(1A) receptor (K(i) = 0.26 nM). In vivo, NAE-086 induced all the typical effects of a 5-HT(1A) receptor agonist in rats: it decreased 5-HT synthesis (5-HTP accumulation) and 5-HT turnover (measured as the ratio of 5-hydroxyindoleacetic acid/5-HT), increased corticosterone secretion, induced the 5-HT(1A) syndrome (flat body posture and forepaw treading), inhibited the cage-leaving response, and caused hypothermia. All the responses mediated by postsynaptic 5-HT(1A) receptors were attenuated after single or repeated treatment of the rats with NAE-086. Simultaneously with the development of the tolerance to 5-HT(1A) receptor-mediated responses, 5-HT(2A) receptor-mediated responses were enhanced, as judged from the increased number of spontaneous and/or agonist [1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane]-induced wet-dog shake responses. The significance of this behavioral effect in relation to clinical observations is discussed.
 ...
PMID:The pharmacological profile of (R)-3,4-dihydro-N-isopropyl-3-(N-isopropyl-N-propylamino)-2H-1-benzopyran-5-carboxamide, a selective 5-hydroxytryptamine(1A) receptor agonist. 1171 72

To systematically evaluate the efficacy and safety of Ganmao Qingre Granules in treatment of children with wind-cold syndrome. The study systematically retrieved CNKI, WanFang, VIP, CBM, PubMed, EMbase and Cochrane Library for children cases with wind-cold syndrome treated with RCT. The literature inclusion criteria provided by Cochrane was used to evaluate the litera-ture quality, and Meta-analysis was conducted by RevMan 5.3 software. A total of 6 literatures were included, with a total sample size of 492 cases, including 246 cases in the experimental group and 246 cases in the control group. According to the results of Meta-analysis, the experimental group recorded the hypothermia time(MD=-0.38, 95%CI[-0.53,-0.23], P<0.01), the total clinical effective rate(RR=1.25, 95%CI[1.15, 1.36], P<0.01), the cough relief time(MD=-2.75, 95%CI[-3.05,-2.46], P<0.01), the decrease nasal congestion relief time(MD=-1.45, 95%CI[-1.69,-1.22], P<0.01), traditional Chinese medicine syndrome score(MD=-8.35, 95%CI[-9.35,-7.36], P<0.01), all of them were superior to those of the control group(Aminophenol Huangnamin Granules), with statistically significant differences. Only 2 literatures mentioned no obvious adverse reaction, and the other 4 literatures did not mention any adverse reactions. Based on the results of this study, it was indicated that Ganmao Qingre Granules were effective in the treatment of children with wind-cold syndrome, but with unclear adverse reactions. Due to the insufficient quantity and low quality of included literatures, the efficacy and safety need to be further confirmed by more high-quality clinical studies.
 ...
PMID:[Meta-analysis of Ganmao Qingre Granules in treatment of children with wind-cold syndrome]. 3272 42