Tissue distribution of mRNAs encoding muscarinic acetylcholine receptor subtypes

Maeda, Akito; Kubo, Tai; Mishina, Masayoshi; Numa, Shosaku

doi:10.1016/0014-5793(88)80947-5

Cited by 220 publications

(78 citation statements)

References 27 publications

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“…These subtypes were termed m1 to m5 (Bonner et al, 1987;Buckley et al, in press). The antagonist binding properties of the individual cloned m1, m2 and m3 receptors and their pattems of expression in various tissues correspond closely to those of the pharmacologically defined M 1 , M 2 and M 3 receptors (Peralta et al, 1987;Akiba et al, 1988;Maeda et al, 1988;Buckley et al, in press). …”

Section: Introductionsupporting

confidence: 55%

Muscarinic receptor subtypes in rat pancreatic islets: binding and functional studies

Verspohl

Tacke

Mutschler

et al. 1990

European Journal of Pharmacology

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Cholinergie agents arepotent modulators of insulin release that aet via musearinie reeeptors. We now investigated the musearlnie receptor subtype present in rat panereatic islets in binding and funetional studies. Binding of 5 nM [ 3 H]N-methylscopolamine ([ 3 H]NMS) was half maximal at 30 min. At 60 min, the maximal total bindingwas 1.29% and the non-specifie binding (presence of 100 ,uM atropine) was 0.18% of the total radioaetivity per 10 f.'g islet protein. The high-affinity Kds were 8.5, 56, 1300 and 1300 nM, respectively. The high affinity Kd of the muscarinie receptor agonist, arecaidine propargyl ester (APE), was 8.1 nM. The EC 50 for the biologieal effects of APE on insulin and glucagon secretion was 3.2 and 2.3 nM. The rank order for the high-affinity biological effects of antagonists (inhibition of APE-mediated insulin/ glucagon release) was almost the same as for binding. The data indicate that rat pancreatie islets contain neither an MI subtype (high-affinity for pirenzepine) nor an M 2 subtype (high-affinity for methoctramine) receptor. However, the data evidence an M 3 receptor subtype, since SiHC in the absence of the M 1 receptor subtype shows a relatively high affinity to the receptors in rat panereatie islets.

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Section: Introductionsupporting

confidence: 55%

Muscarinic receptor subtypes in rat pancreatic islets: binding and functional studies

Verspohl

Tacke

Mutschler

et al. 1990

European Journal of Pharmacology

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“…For example, several subtypes of muscarinic, serotonergic, and adrenergic receptors have now been cloned [19][20][21][22][23][24][25][26]. These receptor subtypes are expressed in distinct regions of the brain, and in the case of muscarinic receptors, different receptor gene products are expressed in presynaptic versus postsynaptic locations [27][28][29]. Recently, a cDNA sequence for a rat brain D2 receptor was reported showing significant sequence homology with receptors that mediate signal transduction by coupling with G-proteins [30].…”

Section: Introductionmentioning

confidence: 99%

The distribution of a dopamine D2 receptor mRNA in rat brain

1989

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Based on the recently reported sequence ofa dopamine D2 receptor cloned from rat brain, we prepared a series ofcDNA probes to determine the distribution of mRNA encoding this receptor. Within the forebrain, D2 receptor mRNA is abundant in the caudate-putamen, accumbens nucleus and olfactory tubercle. Moderate to low levels of mRNA are observed in the medial habenular nucleus, diagonal band, lateral septal nucleus, claustrum, dorsal endopiriform nucleus, and entorhinal cortex. In the mesencephalon, D2 receptor mRNA is abundant within the substantia nigra, pars compacta, and the ventral tegmental area. Comparison of the distributions of the mRNA and ligand binding indicates that both presynaptic and postsynaptic D2 receptors of the nigrostriatal, mesolimbic and mesocortical pathways are derived from the same mRNA. Dopamine receptor; Neurotransmitter receptor; mRNA

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“…The antagonist binding properties of individual mAChR subtypes expressed in Xenopus oocytes [2,3,12] show that mAChR I, mAChR II and mAChR III correspond most closely to the pharmacologically defined M1 (I), M2 cardiac (II) and M2 glandular (III) subtypes [13][14][15], respectively. This, together with the differential tissue distribution of the mRNAs encoding the individual mAChR species [2,[16][17][18][19], indicates that the mAChR heterogeneity in tissues with respect to antagonist binding is attributable to the presence of distinct mAChR gene products by themselves or in various combinations.…”

Section: Introductionmentioning

confidence: 99%

Location of a region of the muscarinic acetylcholine receptor involved in selective effector coupling

et al. 1988

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Chimaeric muscarinic acetylcholine receptors (mAChR) in which corresponding portions of mAChR I and mAChR II are replaced with each other have been produced in Jfenopus oocytes by expression of cDNA constructs encoding them.Functional analysis of the chimaeric mAChRs indicates that a region mostly comprising the putative cytoplasmic portion between the proposed transmembrane segments V and VI is involved in selective coupling of mAChR I and mAChR II with different effector systems. In contrast, the exchange of this region between mAChR I and mAChR II does not significantly affect the antagonist binding properties of the two mAChR subtypes.

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Tissue distribution of mRNAs encoding muscarinic acetylcholine receptor subtypes

Cited by 220 publications

References 27 publications

Muscarinic receptor subtypes in rat pancreatic islets: binding and functional studies

Muscarinic receptor subtypes in rat pancreatic islets: binding and functional studies

The distribution of a dopamine D2 receptor mRNA in rat brain

Location of a region of the muscarinic acetylcholine receptor involved in selective effector coupling

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