Characterization and distribution of alpha 2-adrenergic receptors in the human intestinal mucosa.
Open accessAbstract
The subtype and the expression of the alpha 2-adrenergic receptor were investigated in the normal mucosa from human intestine by means of radioligand binding, RNase mapping, and measurement of adenylate cyclase activity. The study of the binding of the alpha 2-adrenergic antagonist, [3H]RX821002, to epithelial cell membranes indicated the existence of a single class of noninteracting sites displaying a high affinity for the radioligand (Kd = 1.1 +/- 0.5 nM). The rank order of potency of antagonists to inhibit [3H]RX821002 binding (RX821002 > yohimbine = rauwolscine > phentolamine approximately idazoxan >> chlorpromazine > prazosin) suggested that the receptor is of the alpha 2A subtype. A conclusion which is confirmed by the fact that only alpha 2C10 transcripts were found in the human intestine mucosa. Competition curves with (-)-norepinephrine demonstrated that 60% of the receptor population exhibited high affinity for agonists. This high-affinity state was abolished by the addition of GTP plus Na+ or by prior treatment of the membranes with pertussis toxin indicating it corresponded to G protein-coupled receptors. [32P]ADP-ribosylation and immunoblotting experiments identified two pertussis toxin-sensitive G proteins corresponding to Gi2 and Gi3. The study of the distribution of the receptor indicated that (a) the proximal colon is the intestine segment exhibiting the highest receptor density and (b) the receptor is predominantly expressed in crypts and is preferentially located in the basolateral membrane of the polarized cell. The distribution of the receptor along the crypt-surface axis of the colon mucosa can be correlated with a higher level of alpha 2C10-specific mRNA and a higher efficiency of UK14304 to inhibit adenylate cyclase in crypt cells.
The claims and statistics of this paper haven’t been checked yet.
Run the check — free, no account needed. It reads the open-access text and checks the sources it cites.
Integrity signals
Registry
Cites
Statistics
Claims the paper makes
The claims and statistics of this paper haven’t been checked yet.
Run the check — free, no account needed. It reads the open-access text and checks the sources it cites.
Claims other papers make about this one
Each is checked against this paper’s own text: does it say what the citing paper says it does?
Autoinducer 3 can stimulate norepinephrine receptors on the surface of eukaryotic cells, and α-2 receptors are present on the brush border of human enterocytes.
“For example, autoinducer 3 can stimulate nor epinephrine receptors on the surface of eukaryotic cells, and α-2 receptors are present on the brush border of human enterocytes.51”
From Principles and clinical implications of the brain-gut-enteric microbiota axis (2009) · cites this paper as [51]
Self-check
Percentages, sums and reported differences re-computed from the paper’s own numbers.
The self-check needs the paper’s full text.
Cites
Bradford, M. M. (1976) · Analytical Biochemistry · doi:10.1016/0003-2697(76)90527-3 · Cited by 255,302 · see citing works
Single-Step Method of RNA Isolation by Acid Guanidinium Thiocyanate–Phenol–Chloroform Extraction
Chomczynski, P., & Sacchi, N. (1987) · Analytical Biochemistry · doi:10.1006/abio.1987.9999 · Cited by 65,240 · see citing works
Single-step method of RNA isolation by acid guanidinium thiocyanate-phenol-chloroform extraction
Chomczyński, P., & Sacchi, N. (1987) · Analytical Biochemistry · doi:10.1016/0003-2697(87)90021-2 · Cited by 47,092 · see citing works
Yung-Chi, C., & Prusoff, W. H. (1973) · Biochemical Pharmacology · doi:10.1016/0006-2952(73)90196-2 · Cited by 12,922 · see citing works
Garen, A., & Levinthal, C. (1960) · Biochimica et Biophysica Acta · doi:10.1016/0006-3002(60)91282-8 · Cited by 1,401 · see citing works
Purification of the human intestinal brush border membrane
Schmitz, J., Preiser, H., Maestracci, D., Ghosh, B. K., Cerda, J. J., & Crane, R. K. (1973) · Biochimica et Biophysica Acta (BBA) - Biomembranes · doi:10.1016/0005-2736(73)90434-3 · Cited by 790 · see citing works
Kobilka, B. K., Matsui, H., Kobilka, T. S., Yang‐Feng, T. L., Francke, U., Caron, M. G., Lefkowitz, R. J., & Regan, J. W. (1987) · Science · doi:10.1126/science.2823383 · Cited by 786 · see citing works
Cloning and expression of a human kidney cDNA for an alpha 2-adrenergic receptor subtype.
Regan, J. W., Kobilka, T. S., Yang-Feng, T. L., Caron, M. G., Lefkowitz, R. J., & Kobilka, B. K. (1988) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.85.17.6301 · Cited by 434 · see citing works
Sub types of α2-adrenoceptors: Pharmacological and molecular biological evidence converg
Bylund, D. B. (1988) · Trends in Pharmacological Sciences · doi:10.1016/0165-6147(88)90254-4 · Cited by 378 · see citing works
Simonds, W. F., Goldsmith, P. K., Codina, J., Unson, C. G., & Am, S. (1989) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.86.20.7809 · Cited by 376 · see citing works
Lomasney, J. W., Lorenz, W., Allen, L. F., King, K., Regan, J. W., Yang‐Feng, T. L., Caron, M. G., & Lefkowitz, R. J. (1990) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.87.13.5094 · Cited by 283 · see citing works
Rio, M. C., Bellocq, J., Gairard, B., et al. (1987) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.84.24.9243 · Cited by 279 · see citing works
Gershon, M. D., & Erde, S. M. (1981) · Gastroenterology · doi:10.1016/0016-5085(81)90275-4 · Cited by 221 · see citing works
Biodata handling with microcomputers
Barrett, A. (1984) · International Journal of Bio-Medical Computing · doi:10.1016/0020-7101(84)90045-x · Cited by 213 · see citing works
[45] ADP-ribosylation of membrane components by pertussis and cholera toxin
Ribeiro-Neto, F., Mattera, R., Hildebrandt, J. D., et al. (1985) · Methods in enzymology on CD-ROM/Methods in enzymology · doi:10.1016/0076-6879(85)09115-7 · Cited by 206 · see citing works
Ion transport in rabbit ileal mucosa. 3. Effects of catecholamines
Field, M., & McColl, I. (1973) · American Journal of Physiology-Legacy Content · doi:10.1152/ajplegacy.1973.225.4.852 · Cited by 203 · see citing works
Treatment of Diabetic Diarrhea with Clonidine
Fedorak, R. N., FIELD, M., & CHANG, E. B. (1985) · Annals of Internal Medicine · doi:10.7326/0003-4819-102-2-197 · Cited by 199 · see citing works
Laburthe, M., Chenut, B., Rouyer‐Fessard, C., et al. (1986) · Endocrinology · doi:10.1210/endo-118-5-1910 · Cited by 138 · see citing works
Intestinal ion transport: effect of norepinephrine, pilocarpine, and atropine
Hubel, K. (1976) · American Journal of Physiology-Legacy Content · doi:10.1152/ajplegacy.1976.231.1.252 · Cited by 108 · see citing works
alpha 2-Adrenergic receptor regulation of ion transport in rabbit ileum
Chang, E. B., Field, M., & Miller, R. J. (1982) · American Journal of Physiology-Gastrointestinal and Liver Physiology · doi:10.1152/ajpgi.1982.242.3.g237 · Cited by 106 · see citing works
Tutton, P. J. M., & Barkla, D. H. (1987) · PubMed · Cited by 97 · see citing works
Kurose, H., Regan, J. W., Caron, M. G., et al. (1991) · Biochemistry · doi:10.1021/bi00227a024 · Cited by 90 · see citing works
A single column method for the assay of adenylate cyclase
Alvarez, R., & Daniels, D. V. (1990) · Analytical Biochemistry · doi:10.1016/0003-2697(90)90423-7 · Cited by 82 · see citing works
Chang, E. B., Field, M., & Miller, R. J. (1983) · American Journal of Physiology-Gastrointestinal and Liver Physiology · doi:10.1152/ajpgi.1983.244.1.g76 · Cited by 79 · see citing works
Homburger, V., Brabet, P., Audigier, Y., et al. (1987) · Molecular Pharmacology · doi:10.1016/s0026-895x(25)10438-0 · Cited by 75 · see citing works
Purified epithelial Na+ channel complex contains the pertussis toxin-sensitive G alpha i-3 protein.
Ausiello, D. A., Stow, J. L., Cantiello, H. F., et al. (1992) · Journal of Biological Chemistry · doi:10.1016/s0021-9258(18)42897-9 · Cited by 73 · see citing works
Clonidine and Lidamidine to Inhibit Watery Diarrhea in a Patient with Lung Cancer
McArthur, K. E., ANDERSON, D. S., DURBIN, T. E., et al. (1982) · Annals of Internal Medicine · doi:10.7326/0003-4819-96-3-323 · Cited by 73 · see citing works
Milligan, G., Carr, C., Gould, G. W., et al. (1991) · Journal of Biological Chemistry · doi:10.1016/s0021-9258(18)38138-9 · Cited by 68 · see citing works
Alpha-2 receptors in the gastrointestinal system: A new therapeutic approach
DiJoseph, J. F., Taylor, J., & Mir, G. (1984) · Life Sciences · doi:10.1016/0024-3205(84)90067-5 · Cited by 68 · see citing works
Chang, E. B., Fedorak, R. N., & Field, M. (1986) · PubMed · Cited by 63 · see citing works
Radioautographic localization of epidermal growth factor receptors in human fetal gut
Ménard, D., & Pothier, P. (1991) · Gastroenterology · doi:10.1016/0016-5085(91)90520-u · Cited by 61 · see citing works
G-proteins mediate intestinal chloride channel activation
Tilly, B. C., Kansen, M., van Gageldonk, P. G. M., et al. (1991) · Journal of Biological Chemistry · doi:10.1016/s0021-9258(18)52205-5 · Cited by 54 · see citing works
Paris, H. J., Voisin, T., Rémaury, A., et al. (1990) · Journal of Pharmacology and Experimental Therapeutics · doi:10.1016/s0022-3565(25)12655-4 · Cited by 45 · see citing works
Self-citationNakaki, T., Nakadate, T., Yamamoto, S., et al. (1983) · Molecular Pharmacology · doi:10.1016/s0026-895x(25)14228-4 · Cited by 45 · see citing works
On the innervation of the ileal mucosa in the rat‐a synapse
Newson, B., Ahlman, H. K., Dahlström, A., Gupta, T. K. D., & Nyhus, L. M. (1979) · Acta Physiologica Scandinavica · doi:10.1111/j.1748-1716.1979.tb06357.x · Cited by 44 · see citing works
Cyclic nucleotide metabolism in rat colonic epithelial cells with different proliferative activities
Craven, P. A., & DeRubertis, F. R. (1981) · Biochimica et Biophysica Acta (BBA) - General Subjects · doi:10.1016/0304-4165(81)90183-5 · Cited by 42 · see citing works
Seuwen, K., Magnaldo, I., Kobilka, B. K., et al. (1990) · Cell Regulation · doi:10.1091/mbc.1.6.445 · Cited by 41 · see citing works
Bouscarel, B. E., Cortinovis, C., Carpéné, C., et al. (1985) · European Journal of Pharmacology · doi:10.1016/0014-2999(85)90062-7 · Cited by 36 · see citing works
Endogenous norepinephrine release induced by tyramine modulates intestinal ion transport
Tapper, E. J., Bloom, A. S., & Lewand, D. L. (1981) · American Journal of Physiology-Gastrointestinal and Liver Physiology · doi:10.1152/ajpgi.1981.241.3.g264 · Cited by 36 · see citing works
Devedjian, J.-C., Fargues, M., Denis, C., et al. (1991) · Journal of Biological Chemistry · doi:10.1016/s0021-9258(18)98692-8 · Cited by 35 · see citing works
Self-citationLaburthe, M., Amiranoff, B., & Boissard, C. (1982) · Biochimica et Biophysica Acta (BBA) - Molecular Cell Research · doi:10.1016/0167-4889(82)90029-5 · Cited by 33 · see citing works
Sénard, J., Langin, D., Estañ, L., et al. (1990) · European Journal of Pharmacology · doi:10.1016/0014-2999(90)94096-g · Cited by 31 · see citing works
van den Berghe, N., Nieuwkoop, N. J., Vaandrager, A. B., et al. (1991) · Biochemical Journal · doi:10.1042/bj2780565 · Cited by 25 · see citing works
The binding of [3H]prazosin and [3H]clonidine to rat jejunal epithelial cell membranes
Cotterell, D. J., Munday, K. A., & Poat, J. A. (1984) · Biochemical Pharmacology · doi:10.1016/0006-2952(84)90458-1 · Cited by 23 · see citing works
Paris, H. J., Taouis, M., & Galitzky, J. (1987) · Molecular Pharmacology · doi:10.1016/s0026-895x(25)13050-2 · Cited by 20 · see citing works
Adrenergic versus VIPergic control of cyclic AMP in human colonic crypts
Boige, N., Munck, À., & Laburthe, M. (1984) · Peptides · doi:10.1016/0196-9781(84)90238-9 · Cited by 18 · see citing works
Antisecretory activity of the alpha2-adrenoceptor agonist, xylazine in rat jejunal epithelium
Cox, H. M., & Cuthbert, A. W. (1989) · Naunyn-Schmiedeberg s Archives of Pharmacology · doi:10.1007/bf00168660 · Cited by 18 · see citing works
Couvineau, A., Darmoul, D., Blais, A., et al. (1992) · American Journal of Physiology-Cell Physiology · doi:10.1152/ajpcell.1992.262.6.c1478 · Cited by 15 · see citing works
Self-citationα2-Adrenergic agonists: A newer class of antidiarrheal drug
Dharmsathaphorn, K. (1986) · Gastroenterology · doi:10.1016/0016-5085(86)90650-5 · Cited by 14 · see citing works
α2-adronoceptor in HT29 human colon adenocarcinoma cell-line: study of [3H](−)-adrenaline binding
Sénard, J., Mauriège, P., Daviaud, D., et al. (1989) · European Journal of Pharmacology · doi:10.1016/0014-2999(89)90285-9 · Cited by 9 · see citing works
Self-citation
Flagged first, then by citations
Research works printed but not linked: 2
- Pamucku, R., and E. B. Chang. 1990. Alpha2-adrenergic agonists as anti- diarrhoeal agents: a review of physiological and cellular mechanisms. In Text- book of Secretory Diarrhoea. Volume 28. E. Lebenthal and M. Duffey, editors. Raven Press, New York. 383-393.
- Simonds, W. F., P. K. Goldsmith, J. Codina, C. G. Unson, and A. M. Spiegel. 1989. Gi2 mediates a2-adrenergic inhibition ofadenylate cyclase in plate- let membranes: in situ identification with Ga C-terminal antibodies. Proc. Nail. Acad. Sci. USA. 86:7809-7813.
Cited by
Sorted by citations
Principles and clinical implications of the brain-gut-enteric microbiota axis
Rhee, S. H., Pothoulakis, C., & Mayer, E. A. (2009) · Nature Reviews Gastroenterology & Hepatology · doi:10.1038/nrgastro.2009.35 · Cited by 1,342 · see citing works
“For example, autoinducer 3 can stimulate norepinephrine receptors on the surface of eukaryotic cells, and α-2 receptors are present on the brush border of human enterocytes”
Inter-kingdom signalling: Communication between bacteria and their hosts
Hughes, D. T., & Sperandio, V. (2008) · Nature Reviews Microbiology · doi:10.1038/nrmicro1836 · Cited by 761 · see citing works
Li, M., Kim, Y.-M., Koh, J. H., Park, J., Kwon, H. M., Park, J.-H., Jin, J., Park, Y., Kim, D., & Kim, W.-U. (2024) · Journal of Clinical Investigation · doi:10.1172/jci167835 · Cited by 25 · see citing works
- Authors
- Valet, P., Senard, J. M., Devedjian, J. C., Planat, V, Salomon, R., Voisin, T., Drean, G., Couvineau, A., Daviaud, D., & Denis, C.
- Affiliations
- Inserm (FR)
- Venue
- Journal of Clinical Investigation
- Published
- 1993-05-01
- Volume
- 91
- Issue
- 5
- Pages
- 2049-2057
- ISSN
- 0021-9738 (ISSN-L)
- PMC
- PMC288203
- OpenAlex
- W2070409051
- Cited by
- 58
- References
- 50
- Citations by year
- 2024: 3 · 2023: 1 · 2022: 2 · 2021: 4 · 2020: 1 · 2019: 1 · 2018: 3 · 2016: 2 · 2015: 1
- FWCI
- 0.52
- Type
- journal article
- Language
- en
- Open access
- bronze
- doi.org
- Locations
- Journal of Clinical Investigation (publishedVersion)
- PubMed Central (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Receptor Mechanisms and Signaling
- Health Sciences › Medicine › Gastroenterology › Gastrointestinal motility and disorders
- Life Sciences › Neuroscience › Cellular and Molecular Neuroscience › Neuropeptides and Animal Physiology
- Keywords
- alpha2-adrenoceptors, human intestinal mucosa, colon, crypt, receptor distribution, G protein-coupled receptors, Gi2, Gi3, adenylate cyclase, RX821002, pertussis toxin, basolateral membrane, epithelial cells
- MeSH terms
- Adenylyl Cyclase Inhibitors, Brimonidine Tartrate, Adenosine Diphosphate Ribose, Adrenergic alpha-Agonists, Adrenergic alpha-Antagonists, Binding, Competitive, Cell Membrane, Colon, Dioxanes, Duodenum, Epinephrine, Epithelium, Humans, Intestinal Mucosa, Kinetics, Microvilli, NAD, Organ Specificity, Virulence Factors, Bordetella, Quinoxalines, Receptors, Adrenergic, alpha, RNA, Messenger, Idazoxan, Pertussis Toxin, Adenylate Cyclase Toxin
About these checks
Registry, retraction, Cites and statistics results are computed, not judged, with one exception: a printed reference that no index lists is read once by a model before it counts as a citation error. Claims are extracted by a model and kept only when their quote appears verbatim in the text; each cited source is then checked, with a model’s help, for whether it says what the claim relies on. Those verdicts can be wrong — read the claim’s quote and the cited source before relying on one.
Statistics and arithmetic are recomputed, not judged.
Confidence bands are shown only for fields calibrated on our annotated test set. None is calibrated yet, so no band is shown.
What counts as a claim ›How we measure confidence ›How we check this ›
Are you an author, or do you see a problem with this page? Request a review
