Narkosepotenzierende und analgetische Wirkung von 1,4-Dipyrrolidino-2-butin

Lenke, D

doi:10.1007/bf00246774

Cited by 26 publications

(6 citation statements)

References 4 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…The antinociceptive effect of morphine (5 mg kg-' i.p.) in the lesioned rats did not differ from that in the sham operated rats ( (34) and animals (12,13,14,15,16,17,18,19,20). A large difference exists between the analgesia induced in animals by both BIMU 1 and BIMU 8 and that induced by direct muscarinic agonists and cholinesterase inhibitors.…”

Section: 4andx8*mentioning

confidence: 66%

“…It has long been known that ACh (11). selective Ml agonists such as McN-A-343 and AF-102B (12), unselective muscarinic agonists such as tremorine (13), oxotremorine (14,15), arecoline (16), pilocarpine (17) and cholinesterase inhibitors such as physostigmine (18,19) and diisopropyl phosphorofluoridate (20) induce antinociception in laboratory animals by the activation of the cholinergic system. Moreover, the amplification of cholinergic neurotransmission induced by antagonism of muscarinic autoreceptors (2 1, 22, 23) or, alternatively, by interaction with heteroreceptors (24) located on presynaptic cholinergic terminals, produces a central antinociceptive effect.…”

mentioning

confidence: 99%

See 1 more Smart Citation

Central cholinergic antinociception induced by 5HT4 agonists: BIMU 1 and BIMU 8

Ghelardini¹,

Galeotti²,

Casamenti³

et al. 1996

Life Sciences

View full text Add to dashboard Cite

show abstract

Section: 4andx8*mentioning

confidence: 66%

mentioning

confidence: 99%

Central cholinergic antinociception induced by 5HT4 agonists: BIMU 1 and BIMU 8

Ghelardini¹,

Galeotti²,

Casamenti³

et al. 1996

Life Sciences

View full text Add to dashboard Cite

show abstract

“…Furthermore, in the rat cerebral cortex, caffeine reduced the inhibition of ACh release produced by morphine (Jhamandas et al 1978;Phillis et al 1980). It has long been known that ACh (Pedigo et al 1975), selective M 1 agonists such as McN-A-343 and AF-102B , unselective muscarinic agonists such as tremorine (Lenke 1958), oxotremorine (George et al 1962;Bartolini et al 1987), arecoline (Herz 1962), pilocarpine (Hendershot and Forsaith 1959) and cholinesterase inhibitors such as physostigmine (Harris et al 1969;Ireson 1970) and diisopropyl phosphorofluoridate (Lentz et al 1969) induce antinociception in laboratory animals by the activation of the cholinergic system. Moreover, the amplification of cholinergic neurotransmission induced by antagonism of muscarinic autoreceptors Gualtieri et al 1989;Ghelardini et al 1990) or, alternatively, by interaction with heteroreceptors ) located on presynaptic cholinergic terminals, produces a central antinociceptive effect.…”

Section: Introductionmentioning

confidence: 99%

Caffeine induces central cholinergic analgesia

Ghelardini¹,

Galeotti²,

Bartolini³

1997

Naunyn-Schmiedeberg's Arch Pharmacol

View full text Add to dashboard Cite

The antinociceptive effect of caffeine was examined by using the hot-plate, abdominal constriction tests in mice and the tail flick and paw-pressure tests in rats. Caffeine (1-5 mg kg -1 s.c. in mice; 2.5-5 mg kg -1 i.p. in rats) produced significant antinociception in both species which was prevented by atropine (5 mg kg -1 i.p.), pirenzepine (0.1 µg per mouse i.c.v.), hemicholinium-3 (1 µg/ mouse i.c.v.) and N 6 -cyclopentyladenosine (5 µg/mouse i.c.v.), but not by naloxone (1 mg kg -1 i.p.), CGP 35348 (100 mg kg -1 i.p.), α-methyl p-tyrosine (100 mg kg -1 i.p.) and reserpine (2 mg kg -1 i.p.). Intracerebroventricular injection of caffeine in mice at doses (2.5-5 µg per mouse) which were largely ineffective by parenteral routes, induces an antinociception whose intensity equalled that obtainable s.c. or i.p. In the antinociceptive dose-range, caffeine did not produce any behavioural impairment as revealed by the rotarod and Irwing tests. On the basis of the above data, it can be postulated that caffeine exerts an antinociceptive effect mediated by central amplification of cholinergic transmission.

show abstract

“…It has long been known that the direct and indirect activation of the cholinergic system produces analgesia in both animals (1,2,9,(16)(17)(18)21,23,24) and humans (20). Because sumatriptan is endowed with cholinergic antinociceptive properties and 8-OH-DPAT enhances ACh release, the goals of the present study were to explore whether other 5-HT 1A agonists, such as gepirone and 8-OH-DPAT, were able to increase the pain threshold in mice and then investigate whether a cholinergic mechanism underlies 5-HT 1A antinociception.…”

mentioning

confidence: 99%

5-HT1A Agonists Induce Central Cholinergic Antinociception

Galeotti

Ghelardini

Bartolini

1997

Pharmacology Biochemistry and Behavior

View full text Add to dashboard Cite

GALEOTTI, N., C. GHELARDINI AND A. BARTOLINI. 5-HT 1A agonists induce central cholinergic antinociception. PHARMACOL BIOCHEM BEHAV 57 (4) 835-841, 1997.-The antinociceptive effects of the 5-HT 1A agonists buspirone [3 mg/kg intraperitoneally (IP)], gepirone (3-6 mg/kg IP), and 8-OH-DPAT [3-5 mg/kg IP; 1-3 g per mouse intracerebroventricularly (ICV)] were examined in mice by using the hot-plate (thermal stimulus) and abdominal constriction (chemical stimulus) tests. Buspirone, gepirone, and 8-OH-DPAT produced significant antinociception, which was prevented by atropine (5 mg/kg IP), the ACh depletor hemicholinium-3 (1 g per mouse ICV), and the 5-HT 1A antagonist NAN 190 (0.5 g per mouse ICV), but not by naloxone (1 mg/kg IP), the GABA B antagonist CGP 35348 (100 mg/kg IP), and pertussis toxin (0.25 g per mouse ICV). NAN 190, which totally antagonized buspirone, gepirone, and 8-OH-DPAT antinociception, did not modify the analgesic effect of morphine (5 mg/kg subcutaneously). In the antinociceptive dose range, none of the 5HT 1A agonists impaired mouse performance evaluated by rota-rod and hole board tests. On the basis of these data, it can be postulated that buspirone, gepirone, and 8-OH-DPAT exert an antinociceptive effect mediated by a central amplification of cholinergic transmission. © 1997 Elsevier Science Inc. 8-OH-DPATBuspirone Gepirone 5-HT 1A receptors ACh Cholinergic neurotransmission Antinociception Analgesia THE nonbenzodiazepine anxiolytic drugs buspirone, gepirone, and 8-OH-DPAT are agonists of the serotoninergic 5-HT 1A receptors in the central nervous system. Serotonin 5-HT 1A sites are localized predominantly on the axon terminals of serotoninergic neurons. They function as autoreceptors (14), and their stimulation leads to the disinhibition of the cholinergic system that is tonically inhibited by tryptaminergic control (11). Bianchi et al. (4) demonstrated that the full 5-HT 1A agonist 8-OH-DPAT was able to increase ACh release from the cerebral cortex of freely moving guinea pigs. Recent studies have shown that buspirone, given systemically, produces antinociception in several pain tests in rats (12). Giordano and Rogers (13) reported that buspirone-induced analgesia may be a nonopioid, adrenally mediated co-and/or epi-phenomenon to core hypothermia evoked by 5-HT 1A receptor agonism. Recently, it was reported that sumatriptan, another 5-HT 1A agonist, was able to induce antinociception in mice and rats through a cholinergic mechanism (3).It has long been known that the direct and indirect activation of the cholinergic system produces analgesia in both animals (1,2,9,16-18,21,23,24) and humans (20). Because sumatriptan is endowed with cholinergic antinociceptive properties and 8-OH-DPAT enhances ACh release, the goals of the present study were to explore whether other 5-HT 1A agonists, such as gepirone and 8-OH-DPAT, were able to increase the pain threshold in mice and then investigate whether a cholinergic mechanism underlies 5-HT 1A antinociception. Moreover, we examined whether such antinoci...

show abstract

Narkosepotenzierende und analgetische Wirkung von 1,4-Dipyrrolidino-2-butin

Cited by 26 publications

References 4 publications

Central cholinergic antinociception induced by 5HT4 agonists: BIMU 1 and BIMU 8

Central cholinergic antinociception induced by 5HT4 agonists: BIMU 1 and BIMU 8

Caffeine induces central cholinergic analgesia

5-HT1A Agonists Induce Central Cholinergic Antinociception

Contact Info

Product

Resources

About