Muscarinic Effects of Various Isoarecaidine Esters in Sympathetic Ganglia

Porsius, A. J.; Wilffert, Bob; Lambrecht, Günter; Moser, Ulrich; Mutschler, E.

doi:10.1111/j.1474-8673.1981.tb00503.x

Cited by 7 publications

(5 citation statements)

References 8 publications

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“…The pressor effect produced by paraoxon was abolished by antimuscarinic agents: dexetimide (0.2 mg/kg) blocks the pressor response to stimulants of ganglionic muscarinic receptors (Porsius et al, 1981). Our results show that N-methylatropine (0.5 mg/kg) also blocks the pressor response to QS-4-Me, which indicates that ganglion muscannic receptors are blocked by this antimuscarinic drug.…”

Section: Diionsupporting

confidence: 54%

“…However, only higher doses of paraoxon were able to produce pressor effects in the pithed rat with low initial blood pressure, as was demonstrated previously by Varagic (1955) and McEwen (1968) using physostigmine. The pressor effect produced by paraoxon was abolished by antimuscarinic agents: dexetimide (0.2 mg/kg) blocks the pressor response to stimulants of ganglionic muscarinic receptors (Porsius et al, 1981). Our results show that N-methylatropine (0.5 mg/kg) also blocks the pressor response to QS-4-Me, which indicates that ganglion muscannic receptors are blocked by this antimuscarinic drug.…”

Section: Diionsupporting

confidence: 51%

“…The following were used: dexetimide HC1 (= dbenzethimide HCI) (Janssen Pharmaceutics); mecamylamine HCl (Sigma); N-methylatropinium nitrate (Merck); paraoxon (Sigma); pentobarbitone sodium (Abbott); phentolamine HCl (Ciba Geigy); prazosin HC1 (Pfizer); reserpine (Ciba Geigy); vasopressin (Sandoz); and 1,1-dimethyl-4carboxypiperdine methylester iodide (abbreviation: QS-4-Me) which was synthesized and donated by Lambrecht & Mutschler (1973). This quarternary isocareidine ester induces pressor effects by stimula-tion of muscarinic receptors in sympathetic ganglia (Porsius, Wilffert, Lambrecht, Moser & Mutschler, 1981).…”

Section: Drugsmentioning

confidence: 99%

“…QS-4-Me) which was synthesized and donated by Lambrecht & Mutschler (1973). This quarternary isocareidine ester induces pressor effects by stimulation of muscarinic receptors in sympathetic ganglia (Porsius, Wilffert, Lambrecht, Moser & Mutschler, 1981).…”

Section: Introductionmentioning

confidence: 99%

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The Pressor Effects of Paraoxon in the Pithed Rat

Neef

Porsius

1982

British J Pharmacology

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1In pithed rats paraoxon 825 JAg/kg induced a short-lasting pressor effect. Lower doses of the drug were ineffective. 2 The pressor effect was prevented by N-methylatropine, dexetimide and x-receptor blocking agents but not by mecamylamine. 3 When blood pressure of pithed rats was elevated either by the continuous infusion of vasopressin or by electrical stimulation of the pithing rod, both 275 and 825 gAg/kg paraoxon induced further pressor effects. The effectiveness of various receptor blocking agents was similar to that observed in pithed rats without vasopressin. 4 It is concluded that the pressor effect of paraoxon is mediated by ganglionic muscarinic receptors. Stimulation of these receptors by accumulated acetylcholine results in an increase in postganglionic sympathetic activity and causes pressor effects. 5The peripheral action of paraoxon is compared with its action in intact anaesthetized animals.

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Section: Diionsupporting

confidence: 54%

Section: Diionsupporting

confidence: 51%

Section: Drugsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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The Pressor Effects of Paraoxon in the Pithed Rat

Neef

Porsius

1982

British J Pharmacology

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“…It has been concluded that the pressor effects brought about by quaternary compounds can be attributed to the stimulation of nicotinic and muscarinic receptors in the sympathetic ganglia of both pithed and anesthetized rats [17] . Moreover, Polinsky and coworkers found that the increased plasma epinephrine levels following arecoline treatment in normal subjects and patients with multiple system atrophy might result from nicotinic adrenal stimulation [18] .…”

mentioning

confidence: 99%

Arecoline inhibits catecholamine release from perfused rat adrenal gland1

Lim

Kim

2006

Acta Pharmacologica Sinica

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Aim: To study the effect of arecoline, an alkaloid isolated from Areca catechu, on the secretion of catecholamines (CA) evoked by cholinergic agonists and the membrane depolarizer from isolated perfused rat adrenal gland. Methods: Adrenal glands were isolated from male Sprague‐Dawley rats. The adrenal glands were perfused with Krebs bicarbonate solution by means of a peristaltic pump. The CA content of the perfusate was measured directly using the fluorometric method. Results: Arecoline (0.1–1.0 mmol/L) perfused into an adrenal vein for 60 min produced dose‐ and time‐dependent inhibition in CA secretory responses evoked by acetylcholine (ACh) (5.32 mmol/L), 1.1‐dimethyl‐4‐phenyl piperazinium iodide (DMPP) (100 μmol/L for 2 min) and 3‐(m‐choloro‐phenyl‐carbamoyl‐oxy)‐2‐butynyl trimethyl ammonium chloride (McN‐A‐343) (100 μmol/L for 2 min). However, lower doses of arecoline did not affect CA secretion of high K+ (56 mmol/L); higher doses greatly reduced CA secretion of high K+. Arecoline also failed to affect basal catecholamine output. Furthermore, in adrenal glands loaded with arecoline (0.3 mmol/L), CA secretory response evoked by Bay‐K‐8644 (10 μmol/L), an activator of L‐type Ca2+ channels, was markedly inhibited, whereas CA secretion by cyclopiazonic acid (10 μmol/L), an inhibitor of cytoplasmic Ca2+‐ATPase, was not affected. Nicotine (30 μmol/L), which was perfused into the adrenal gland for 60 min, however, initially enhanced ACh‐evoked CA secretory responses. As time elapsed, these responses became more inhibited, whereas the initially enhanced high K+‐evoked CA release diminished. CA secretion evoked by DMPP and McN‐A‐343 was significantly depressed in the presence of nicotine. Conclusion: Arecoline dose‐dependently inhibits CA secretion from isolated perfused rat adrenal gland evoked by activation of cholinergic receptors. At lower doses arecoline does not inhibit CA secretion through membrane depolarization, but at larger doses it does. This inhibitory effect of arecoline may be mediated by blocking the calcium influx into the rat adrenal medullary chromaffin cells without the inhibition of Ca2+ release from the cytoplasmic calcium store. There seems to be a difference in the mode of action of nicotine and arecoline in rat adrenomedullary CA secretion.

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Struktur‐ und Konformations‐Wirkungs‐Beziehungen heterocyclischer Acetylcholinanaloga, 18. Mitt.¹⁾ Synthese und muskarinartige Wirkung von Estern des Sulfoarecaidins und Sulfoisoarecaidins

Moser

Lambrecht

Mustschler

et al. 1983

Archiv der Pharmazie

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Es wurden Ester des Sulfoarecaidins und Sulfoisoarecaidins 5 und 6 synthetisiert und an der Longitudinalmuskulatur des Meerschweinchen-Ileum auf muskarinartige Wirkung untersucht. Die Stiirke der Muskarinwirkung der Ester 5 und 6 ist von der Liinge der Esterseitenketts abhangig. Struetrue-and ConformptiOa-Activity Relation&ipa of Heterocyclic Acetylcholine Aodogues, XVIIk Synthesis and Mascnrine-Type Activity of Snlfoawddiae and Sdoisoarecaidine EstersThe esters 5 and 6 of sulfoarecaidine and sulfoisoarecaidine were prepared and tested for muscarine-type activity. Results indicate that the muscarinic potency of 5 and 6 strongly depends on the length of the ester side chain. lm Rahmen von Untersuchungenl-n iiber Struktur-Wirkungs-Beziehungen heterocyclischer Acetylcholinanaloga hatten wir festgestellt, daf3 die Stiirke der Muskarinwirkung der Arecaidinester lac bnv. 2sowie der Isoarecaidinester 3a-c bzw. 4pc von drei strukturellen Parametern abhiingt: 1. Vorn Vorhandensein der Ringdoppelbindung, 2. von der Art der Substitution am Ringstickstoff und 3. von der Lange der Esterseitenkette. FOOR FOOR 1 2 3 R: a = CH3; b = GH,; c = n-C3H, Wir konnten zeigen, daS f i r die Abnahme an rnuskarinartiger Potenz bei den Estern 1-4 nach Hydrierung der Ringdoppelbindung die hierdurch veranderte Ringgeornetrie verantwortlich istS3"). 0365-6233183108084k570 S MSWO 0 Verlag Chemie h b H , Weinheim 1983

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Muscarinic Effects of Various Isoarecaidine Esters in Sympathetic Ganglia

Cited by 7 publications

References 8 publications

The Pressor Effects of Paraoxon in the Pithed Rat

The Pressor Effects of Paraoxon in the Pithed Rat

Arecoline inhibits catecholamine release from perfused rat adrenal gland1

Struktur‐ und Konformations‐Wirkungs‐Beziehungen heterocyclischer Acetylcholinanaloga, 18. Mitt.¹⁾ Synthese und muskarinartige Wirkung von Estern des Sulfoarecaidins und Sulfoisoarecaidins

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Muscarinic Effects of Various Isoarecaidine Esters in Sympathetic Ganglia

Cited by 7 publications

References 8 publications

The Pressor Effects of Paraoxon in the Pithed Rat

The Pressor Effects of Paraoxon in the Pithed Rat

Arecoline inhibits catecholamine release from perfused rat adrenal gland1

Struktur‐ und Konformations‐Wirkungs‐Beziehungen heterocyclischer Acetylcholinanaloga, 18. Mitt.1) Synthese und muskarinartige Wirkung von Estern des Sulfoarecaidins und Sulfoisoarecaidins

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Struktur‐ und Konformations‐Wirkungs‐Beziehungen heterocyclischer Acetylcholinanaloga, 18. Mitt.¹⁾ Synthese und muskarinartige Wirkung von Estern des Sulfoarecaidins und Sulfoisoarecaidins