Heterogeneity of muscarinic receptors in the guinea pig esophageal muscularis mucosae and ileal longitudinal muscle

Kamikawa, Yuichiro; Uchida, Kohsuke; Shimo, Yasuo

doi:10.1016/0016-5085(85)90141-6

Cited by 36 publications

(20 citation statements)

References 22 publications

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“…In typical M2-receptors on smooth muscle (Hammer et al, 1980;Barlow et al, 1981) and on nerves (Brown et al, 1980b;Halim et al, 1982;Kilbinger, 1984;Mitchelson, 1984) the pA2 value for pirenzepine was between 6 and 7 and McN A-343 was ineffective or a partial agonist. In a recently reported study oflongitudinal strips ofmuscularis mucosa from guinea-pig oesophagus, Kamikawa et al (1985) found pA2 values of 9.4 for atropine and 7.4 for pirenzepine from Schild-plots with slopes near 1. In guinea-pig ileum, pA2 values were significantly lower than in muscularis mucosa, 8.8 for atropine and 6.9 for pirenzepine, but Schild-plots had slopes of about 1.5.…”

Section: Resultsmentioning

confidence: 92%

Receptors for neurotransmitters in opossum oesophagus muscularis mucosa

Daniel

Jury

Robotham

1986

British J Pharmacology

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Section: Resultsmentioning

confidence: 92%

Receptors for neurotransmitters in opossum oesophagus muscularis mucosa

Daniel

Jury

Robotham

1986

British J Pharmacology

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“…Non-vascular tissues were prepared as follows: guinea-pig (Dunkin-Hartley, 300 g, male) urinary bladder (Eglen & Whiting, 1987), proximal ileum (Clague et al, 1985), oesophageal muscularis mucosae (Kamikawa et al, 1985), zig-zag tracheal strips (Emmerson & McKay, 1979), uterus (Edinburgh Staff, 1968), rat (Sprague-Dawley, 250g, male) paced (2Hz, threshold voltage +10%, 1ms duration) left atria (Blinks, 1966), vas deferens (Edinburgh Staff, 1968), anococcygeus muscle (Gillespie, 1972) and fundic strip (Coleman, 1987).…”

Section: Isolated Tissuesmentioning

confidence: 99%

The pharmacological properties of the peptide, endothelin

Eglen¹,

Michel²,

Sharif³

et al. 1989

British J Pharmacology

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1 The effect of endothelin (ET-1) has been studied on isolated vascular and non-vascular preparations, using both functional and competition radioligand binding techniques. The effects of endothelin on blood pressure were studied in both anaesthetised, chemically denervated normotensive and spontaneously hypertensive rats (SHR). 2 Endothelin elicited contractile responses in the rat thoracic aorta, perfused mesenteric bed, rabbit mesenteric artery and portal vein. The maximal responses in the rat aorta were enhanced by removal of the endothelium, and were reduced in the presence of either a cyclo-oxygenase inhibitor (indomethacin) or a thromboxane receptor antagonist (SQ 29,548). In terms of potency, the most sensitive preparation was the rat endothelium-denuded aorta and rat perfused mesenteric bed (-log EC50 values = 8.2 + 0.07 and 8.2 + 0.12, mean + s.e.mean, n = 4, respectively). In the perfused mesenteric bed of the rat the maximum response to endothelin (219 + 12 mmHg, n = 4) was greater than that to either phenylephrine (maximal response = 67 + 9 mmHg; n = 4) or KCl (maximal response = 110 + 6 mmHg, n = 4).3 Endothelin elicited contractile responses of the guinea-pig isolated ileum, oesophageal muscularis mucosae and uterus. Responses were also observed in the rat fundic strip and paced left atria. The guinea-pig urinary bladder, trachea, rat vas deferens and anococcygeus exhibited little or no response to endothelin at the concentrations studied (1 x 10 -2-3.2 x 10 -8M). Of the above preparations, the ileum and oesophageal muscularis mucosae were the most sensitive to endothelin (-log EC50 = 8.5 + 0.11 and 8.4 + 0.06, n = 6, respectively), exhibiting potencies similar to those observed in the endothelium-denuded aorta of the rat. 4 In competition-radioligand binding studies, endothelin did not displace either [3H]-PN 210-100 or [125I]< -)-co-conotoxin GVIA from binding sites in membranes from rat cerebral cortex and, skeletal muscle or from guinea-pig cerebral cortex and hippocampus, respectively. This indicates a lack of direct interaction of endothelin at the dihydropyridine binding site and the N-type calcium channel, respectively. However, in functional studies, contractile responses to endothelin (1 x 10-8M) in the endothelium-denuded aorta of the rat were potently reversed by nifedipine, verapamil, and prenylamine (-log IC50 values = 8.0 + 0.13, 7.2 + 0.09 and 6.6 + 0.08, n = 4-8,

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“…The responsiveness of this tissue to tions of the mucosa (King et al, 1922). Our recent catecholamines, acetylcholine, 5-hydroxytryptamine, studies have concentrated on the autonomic innervatachykinins and opioid peptides is different from those tion and receptor system in the guinea-pig oesoof the external muscle of the guinea-pig ileum (Kamikawa et al, 1982;1985b;Kamikawa & Shimo, 1983a,b, 'Correspondence. 1984.…”

Section: Introductionmentioning

confidence: 99%

Pharmacological characterization of the histamine receptor in the isolated muscularis mucosae of the guinea‐pig oesophagus

Fujinuma

Kamikawa

Shimo

1985

British J Pharmacology

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1 To characterize the histamine receptors in the muscularis mucosae, the isotonic responsiveness of the isolated muscularis mucosae of the guinea-pig oesophagus to histamine receptor agonists and antagonists was examined in vitro. 2 Histamine (0.1-100 M) produced a concentration-dependent contraction of the muscularis mucosae (EC50 = 1.6 ± 0.2 LM). The contractions were rapid in onset, sustained, reversible by washing and the preparation did not show tachyphylaxis. 3 2-Methylhistamine (2-MH), 2-pyridylethylamine (PEA) and 4-methylhistamine (4-MH) produced similar sustained contractions of the muscularis mucosae. The order of sensitivity was histamine > 2-MH > PEA> 4-MH. Impromidine (10-300 LM) and dimaprit (10-300 gM) caused no response in this tissue. 4 The contractile responses to histamine, 2-MH, and PEA were competitively antagonized by diphenhydramine, and the pA2 values were almost the same (approximately 8.1). Cimetidine (I 00 gM)could not modify the contractile response to these agonists. 5 The contractile response to histamine was slightly inhibited by tetrodotoxin (0.3 JM), atropine (1 LM), indomethacin (0.1-3 jAM) or aspirin (30-300 jM), and the EC50 value was increased about [2][3][4][5][6] times by these drugs. 6 When the preparation was incubated in Tyrode solution containing various calcium concentrations (0, 0.45, 0.9 and 1.8 mM), the concentration-response curve to histamine was shifted to the right and downward; the effect was inversely dependent on the calcium concentration, and in a calcium-free medium the response to histamine was abolished. Verapamil (1-10 M) partially inhibited the contractile response to histamine. 7 The present results indicate that the contraction of the guinea-pig oesophageal muscularis mucosae to histamine is mediated mainly by a direct action on the smooth muscle and partly by indirect actions via the stimulation of either endogenous prostaglandin biosynthesis or intramural cholinergic nerves. The histamine receptors responsible for contractions of this tissue are probably mainly of the H,-subtype with H2-receptors having a negligible role.

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Heterogeneity of muscarinic receptors in the guinea pig esophageal muscularis mucosae and ileal longitudinal muscle

Cited by 36 publications

References 22 publications

Receptors for neurotransmitters in opossum oesophagus muscularis mucosa

Receptors for neurotransmitters in opossum oesophagus muscularis mucosa

The pharmacological properties of the peptide, endothelin

Pharmacological characterization of the histamine receptor in the isolated muscularis mucosae of the guinea‐pig oesophagus

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