PubMed · 6196797
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B Pernow. 1983. Substance P.. https://pubmed.ncbi.nlm.nih.gov/6196797/
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Several 6-alkyl analogues of nicotine were examined in radioligand binding and in vivo functional assays. Although (-)6-ethylnicotine (3) binds with high affinity at nACh receptors (Ki=5.6 nM) and produces nicotine-like actions, its n-propyl homologue (-)4 (Ki=22 nM) failed to produce such effects. In fact, (-)4 antagonized the antinociceptive effects of (-)nicotine in the tail-flick assay in mice, but not the spontaneous activity or discriminative stimulus effects of (-)nicotine. Compound (-)4 appears to selectively antagonize only one of the three effects examined and is an interesting cholinergic agent for subsequent investigation.
The antihyperalgesia effect of BmK AS, a novel sodium channel-specific polypeptide modulator from Chinese scorpion venom in rats was investigated in this study. PWLs (paw withdrawal latency) were increased to 150+/-28, 203+/-34 and 250+/-17% of the control by administration of BmK AS (10 microl) at the concentration of 0.001, 0.01 and 0.1 mg/ml in carrageenan-induced inflamed rats, respectively. Meanwhile, PWLs were enhanced to about 126+/-4, 132+/-4 and 140+/-6% of the control at the same applied concentration of BmK AS in normal rats. The results suggest that BmK AS can induce peripheral antihyperalgesia and antinociception, which probably by modulating the sodium channel on nociceptive afferent pathway.
We investigated the antinociceptive effect of 1-(4-fluorophenyl)-3-methyl-5-[4-(methylsulfinyl)phenyl]pyrazole (FR143166) in the tail-pinch test in mice. The p.o. and i.t. injection of FR143166 exerted dose-dependent antinociceptive actions with ED(50) values of 24 mg/kg and 15 micro g/mouse, respectively. However, i.c.v. injection of FR143166 at a maximum dose of 128 micro g/mouse did not show any antinociceptive effect. The antinociceptive effect of FR143166 injected i.t. was abolished by co-administration of the nonselective serotonin (5-hydroxytryptamine, 5-HT) receptor antagonist, methysergide, but not by the adrenoceptor antagonists, phentolamine and propranolol. Moreover, the effect of FR143166 was also reversed by the 5-HT(2A) receptor antagonist, ketanserin, and the 5-HT(3) receptor antagonist, MDL-72222 (3-tropanyl-3,5-dichlorobenzoate). The effect of FR143166 was attenuated by p-chlorophenylalanine, but not by 6-hydroxydopamine plus nomifensine pretreatment. These results suggest that the descending serotonergic system, especially spinal 5-HT(2A) and 5-HT(3) receptors, is involved in the antinociceptive activity of spinally administered FR143166 on noxious mechanical stimuli.