DOI: 10.1111/j.1476-5381.1974.tb09658.x. THE PROPERTIES OF MUSCARINIC RECEPTORS IN MAMMALIAN CEREBRAL CORTEX

THE PROPERTIES OF MUSCARINIC RECEPTORS IN MAMMALIAN CEREBRAL CORTEX

10.1111/j.1476-5381.1974.tb09658.x

Crossref journal-article

Wiley

British Journal of Pharmacology (311)

Abstract

The reaction of tritiated propylbenzilylcholine mustard ([3H]‐PrBCM; N‐2′‐chloroethyl‐N‐[2″,3″‐3H2]‐propyl‐2‐aminoethylbenzilate) with homogenates of mammalian brain has been studied. The uptake can be divided into an atropine‐sensitive component of fixed capacity (380 pmol/g protein in the rat) and an atropine‐insensitive part. The atropine‐sensitive portion is identified as muscarinic receptor by its insensitivity to nicotinic antagonists and anticholinesterases and its sensitivity to a range of muscarinic antagonists. The uptake of [3H]‐PrBCM is also inhibited by muscarinic agonists and there is reasonable quantitative agreement between the affinities of agonists estimated in this way and in intact tissues by physiological responses. The fraction of [3H]‐PrBCM uptake inhibited by muscarinic antagonists and agonists is the same. The amount of receptor found in six mammalian species was inversely related to the size of the brain, but the rates of alkylation and the sensitivity to atropine were not dissimilar.

Bibliography

BURGEN, A. S. V., HILEY, C. R., & YOUNG, J. M. (1974). THE PROPERTIES OF MUSCARINIC RECEPTORS IN MAMMALIAN CEREBRAL CORTEX. British Journal of Pharmacology, 51(2), 279â285. Portico.

Authors 3

A.S.V. BURGEN (first)
C.R. HILEY (additional)
J.M. YOUNG (additional)

References 10 Referenced 101

10.1111/j.1476-5381.1974.tb09602.x
10.1146/annurev.pa.09.040169.001233
{'key': 'e_1_2_1_4_1', 'first-page': '33', 'article-title': 'Binding of atropine and muscarone to rat brain fractions and its relation to the actylcholine receptor', 'volume': '9', 'author': 'Farrow J.T.', 'year': '1973', 'journal-title': 'Mol. Pharmac.'} / Mol. Pharmac. / Binding of atropine and muscarone to rat brain fractions and its relation to the actylcholine receptor by Farrow J.T. (1973)
10.1111/j.1749-6632.1967.tb53817.x
10.1016/S0021-9258(19)52451-6
{'key': 'e_1_2_1_7_1', 'first-page': '62', 'article-title': 'Measurement of drug receptor dissociation constants of muscarinic agonists on intestinal smooth muscle', 'volume': '180', 'author': 'Parker R.B.', 'year': '1972', 'journal-title': 'J. Pharmac. exp. Ther.'} / J. Pharmac. exp. Ther. / Measurement of drug receptor dissociation constants of muscarinic agonists on intestinal smooth muscle by Parker R.B. (1972)
10.1098/rspb.1965.0058
{'key': 'e_1_2_1_9_1', 'first-page': '394', 'article-title': 'A new kind of drug antagonism: evidence that agonists cause a molecular change in acetylcholine receptors', 'volume': '5', 'author': 'Rang H.P.', 'year': '1969', 'journal-title': 'Mol. Pharmac.'} / Mol. Pharmac. / A new kind of drug antagonism: evidence that agonists cause a molecular change in acetylcholine receptors by Rang H.P. (1969)
10.1152/ajplegacy.1952.168.3.747 / Am. J. Physiol. / Activity of acetylcholine system in cerebral cortex of various unanesthetized mammals by Tower D.B. (1952)
10.1111/j.2042-7158.1972.tb08925.x

Dates

Type	When
Created	13 years, 1 month ago (July 20, 2012, 10:27 a.m.)
Deposited	1 year, 10 months ago (Nov. 4, 2023, 5:37 a.m.)
Indexed	1 year, 10 months ago (Nov. 4, 2023, 8:14 p.m.)
Issued	51 years, 3 months ago (June 1, 1974)
Published	51 years, 3 months ago (June 1, 1974)
Published Online	13 years, 1 month ago (July 19, 2012)
Published Print	51 years, 3 months ago (June 1, 1974)

Funders 0

None

BibTeX

@article{BURGEN_1974, title={THE PROPERTIES OF MUSCARINIC RECEPTORS IN MAMMALIAN CEREBRAL CORTEX}, volume={51}, ISSN={1476-5381}, url={http://dx.doi.org/10.1111/j.1476-5381.1974.tb09658.x}, DOI={10.1111/j.1476-5381.1974.tb09658.x}, number={2}, journal={British Journal of Pharmacology}, publisher={Wiley}, author={BURGEN, A.S.V. and HILEY, C.R. and YOUNG, J.M.}, year={1974}, month=jun, pages={279–285} }

JSON

{
  "indexed": {
    "date-parts": [
      [
        2023,
        11,
        5
      ]
    ],
    "date-time": "2023-11-05T00:14:28Z",
    "timestamp": 1699143268659
  },
  "reference-count": 10,
  "publisher": "Wiley",
  "issue": "2",
  "license": [
    {
      "start": {
        "date-parts": [
          [
            2012,
            7,
            19
          ]
        ],
        "date-time": "2012-07-19T00:00:00Z",
        "timestamp": 1342656000000
      },
      "content-version": "vor",
      "delay-in-days": 13928,
      "URL": "http://onlinelibrary.wiley.com/termsAndConditions#vor"
    }
  ],
  "content-domain": {
    "domain": [
      "bpspubs.onlinelibrary.wiley.com"
    ],
    "crossmark-restriction": true
  },
  "published-print": {
    "date-parts": [
      [
        1974,
        6
      ]
    ]
  },
  "abstract": "<jats:p><jats:list list-type=\"explicit-label\">\n<jats:list-item><jats:p>The reaction of tritiated propylbenzilylcholine mustard ([<jats:sup>3</jats:sup>H]\u2010PrBCM; <jats:italic>N</jats:italic>\u20102\u2032\u2010chloroethyl\u2010<jats:italic>N</jats:italic>\u2010[2\u2033,3\u2033\u2010<jats:sup>3</jats:sup>H<jats:sub>2</jats:sub>]\u2010propyl\u20102\u2010aminoethylbenzilate) with homogenates of mammalian brain has been studied.</jats:p></jats:list-item>\n<jats:list-item><jats:p>The uptake can be divided into an atropine\u2010sensitive component of fixed capacity (380 pmol/g protein in the rat) and an atropine\u2010insensitive part.</jats:p></jats:list-item>\n<jats:list-item><jats:p>The atropine\u2010sensitive portion is identified as muscarinic receptor by its insensitivity to nicotinic antagonists and anticholinesterases and its sensitivity to a range of muscarinic antagonists.</jats:p></jats:list-item>\n<jats:list-item><jats:p>The uptake of [<jats:sup>3</jats:sup>H]\u2010PrBCM is also inhibited by muscarinic agonists and there is reasonable quantitative agreement between the affinities of agonists estimated in this way and in intact tissues by physiological responses.</jats:p></jats:list-item>\n<jats:list-item><jats:p>The fraction of [<jats:sup>3</jats:sup>H]\u2010PrBCM uptake inhibited by muscarinic antagonists and agonists is the same.</jats:p></jats:list-item>\n<jats:list-item><jats:p>The amount of receptor found in six mammalian species was inversely related to the size of the brain, but the rates of alkylation and the sensitivity to atropine were not dissimilar.</jats:p></jats:list-item>\n</jats:list></jats:p>",
  "DOI": "10.1111/j.1476-5381.1974.tb09658.x",
  "type": "journal-article",
  "created": {
    "date-parts": [
      [
        2012,
        7,
        20
      ]
    ],
    "date-time": "2012-07-20T14:27:23Z",
    "timestamp": 1342794443000
  },
  "page": "279-285",
  "update-policy": "http://dx.doi.org/10.1002/crossmark_policy",
  "source": "Crossref",
  "is-referenced-by-count": 101,
  "title": "THE PROPERTIES OF MUSCARINIC RECEPTORS IN MAMMALIAN CEREBRAL CORTEX",
  "prefix": "10.1111",
  "volume": "51",
  "author": [
    {
      "given": "A.S.V.",
      "family": "BURGEN",
      "sequence": "first",
      "affiliation": []
    },
    {
      "given": "C.R.",
      "family": "HILEY",
      "sequence": "additional",
      "affiliation": []
    },
    {
      "given": "J.M.",
      "family": "YOUNG",
      "sequence": "additional",
      "affiliation": []
    }
  ],
  "member": "311",
  "published-online": {
    "date-parts": [
      [
        2012,
        7,
        19
      ]
    ]
  },
  "reference": [
    {
      "key": "e_1_2_1_2_1",
      "doi-asserted-by": "publisher",
      "DOI": "10.1111/j.1476-5381.1974.tb09602.x"
    },
    {
      "key": "e_1_2_1_3_1",
      "doi-asserted-by": "publisher",
      "DOI": "10.1146/annurev.pa.09.040169.001233"
    },
    {
      "key": "e_1_2_1_4_1",
      "first-page": "33",
      "article-title": "Binding of atropine and muscarone to rat brain fractions and its relation to the actylcholine receptor",
      "volume": "9",
      "author": "Farrow J.T.",
      "year": "1973",
      "journal-title": "Mol. Pharmac."
    },
    {
      "key": "e_1_2_1_5_1",
      "doi-asserted-by": "publisher",
      "DOI": "10.1111/j.1749-6632.1967.tb53817.x"
    },
    {
      "key": "e_1_2_1_6_1",
      "doi-asserted-by": "publisher",
      "DOI": "10.1016/S0021-9258(19)52451-6"
    },
    {
      "key": "e_1_2_1_7_1",
      "first-page": "62",
      "article-title": "Measurement of drug receptor dissociation constants of muscarinic agonists on intestinal smooth muscle",
      "volume": "180",
      "author": "Parker R.B.",
      "year": "1972",
      "journal-title": "J. Pharmac. exp. Ther."
    },
    {
      "key": "e_1_2_1_8_1",
      "doi-asserted-by": "publisher",
      "DOI": "10.1098/rspb.1965.0058"
    },
    {
      "key": "e_1_2_1_9_1",
      "first-page": "394",
      "article-title": "A new kind of drug antagonism: evidence that agonists cause a molecular change in acetylcholine receptors",
      "volume": "5",
      "author": "Rang H.P.",
      "year": "1969",
      "journal-title": "Mol. Pharmac."
    },
    {
      "key": "e_1_2_1_10_1",
      "doi-asserted-by": "crossref",
      "first-page": "747",
      "DOI": "10.1152/ajplegacy.1952.168.3.747",
      "article-title": "Activity of acetylcholine system in cerebral cortex of various unanesthetized mammals",
      "volume": "168",
      "author": "Tower D.B.",
      "year": "1952",
      "journal-title": "Am. J. Physiol."
    },
    {
      "key": "e_1_2_1_11_1",
      "doi-asserted-by": "publisher",
      "DOI": "10.1111/j.2042-7158.1972.tb08925.x"
    }
  ],
  "container-title": "British Journal of Pharmacology",
  "original-title": [],
  "language": "en",
  "link": [
    {
      "URL": "https://api.wiley.com/onlinelibrary/tdm/v1/articles/10.1111%2Fj.1476-5381.1974.tb09658.x",
      "content-type": "unspecified",
      "content-version": "vor",
      "intended-application": "text-mining"
    },
    {
      "URL": "https://bpspubs.onlinelibrary.wiley.com/doi/pdf/10.1111/j.1476-5381.1974.tb09658.x",
      "content-type": "unspecified",
      "content-version": "vor",
      "intended-application": "similarity-checking"
    }
  ],
  "deposited": {
    "date-parts": [
      [
        2023,
        11,
        4
      ]
    ],
    "date-time": "2023-11-04T09:37:11Z",
    "timestamp": 1699090631000
  },
  "score": 1,
  "resource": {
    "primary": {
      "URL": "https://bpspubs.onlinelibrary.wiley.com/doi/10.1111/j.1476-5381.1974.tb09658.x"
    }
  },
  "subtitle": [],
  "short-title": [],
  "issued": {
    "date-parts": [
      [
        1974,
        6
      ]
    ]
  },
  "references-count": 10,
  "journal-issue": {
    "issue": "2",
    "published-print": {
      "date-parts": [
        [
          1974,
          6
        ]
      ]
    }
  },
  "alternative-id": [
    "10.1111/j.1476-5381.1974.tb09658.x"
  ],
  "URL": "http://dx.doi.org/10.1111/j.1476-5381.1974.tb09658.x",
  "relation": {},
  "ISSN": [
    "0007-1188",
    "1476-5381"
  ],
  "subject": [],
  "container-title-short": "British J Pharmacology",
  "published": {
    "date-parts": [
      [
        1974,
        6
      ]
    ]
  },
  "assertion": [
    {
      "value": "2012-07-19",
      "order": 2,
      "name": "published",
      "label": "Published",
      "group": {
        "name": "publication_history",
        "label": "Publication History"
      }
    }
  ]
}