Rigid analogs of acetylcholine can be m1-selective agonists: implications for a rational treatment strategy in Alzheimer's disease

Abraham Fisher; David Gurwitz; Dov Barak; Rachel Haring; Ishai Karton; Rachel Brandeis; Zipora Pittel; Daniele Marciano; Haim Meshulam; Zvi Vogel; Eliahu Heldman

doi:10.1016/S0960-894X(00)80541-7

Rigid analogs of acetylcholine can be m1-selective agonists: implications for a rational treatment strategy in Alzheimer's disease

Abraham Fisher, David Gurwitz, Dov Barak, Rachel Haring, Ishai Karton, Rachel Brandeis, Zipora Pittel, Daniele Marciano, Haim Meshulam, Zvi Vogel, Eliahu Heldman

Research output: Contribution to journal › Article › peer-review

10 Scopus citations

Abstract

Rigid analogs of acetylcholine offer an opportunity for selective actions at muscarinic receptor subtypes, since restricted conformational mobility alters the capacity of ligands to adapt to subtle differences in receptor structure. AF102B, a highly rigid analog of acetylcholine, is a centrally active M1 agonist and is evaluated in light of some currently available therapeutic strategies in Alzheimer's disease.

Original language	English
Pages (from-to)	839-844
Number of pages	6
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	2
Issue number	8
DOIs	https://doi.org/10.1016/S0960-894X(00)80541-7
State	Published - 1 Jan 1992
Externally published	Yes

ASJC Scopus subject areas

Biochemistry
Molecular Medicine
Molecular Biology
Pharmaceutical Science
Drug Discovery
Clinical Biochemistry
Organic Chemistry

Access to Document

10.1016/S0960-894X(00)80541-7

Cite this

Fisher, A., Gurwitz, D., Barak, D., Haring, R., Karton, I., Brandeis, R., Pittel, Z., Marciano, D., Meshulam, H., Vogel, Z., & Heldman, E. (1992). Rigid analogs of acetylcholine can be m1-selective agonists: implications for a rational treatment strategy in Alzheimer's disease. Bioorganic and Medicinal Chemistry Letters, 2(8), 839-844. https://doi.org/10.1016/S0960-894X(00)80541-7

@article{f1cc4024cf9c4f01b0589e65c69d9e00,

title = "Rigid analogs of acetylcholine can be m1-selective agonists: implications for a rational treatment strategy in Alzheimer's disease",

abstract = "Rigid analogs of acetylcholine offer an opportunity for selective actions at muscarinic receptor subtypes, since restricted conformational mobility alters the capacity of ligands to adapt to subtle differences in receptor structure. AF102B, a highly rigid analog of acetylcholine, is a centrally active M1 agonist and is evaluated in light of some currently available therapeutic strategies in Alzheimer's disease.",

author = "Abraham Fisher and David Gurwitz and Dov Barak and Rachel Haring and Ishai Karton and Rachel Brandeis and Zipora Pittel and Daniele Marciano and Haim Meshulam and Zvi Vogel and Eliahu Heldman",

year = "1992",

month = jan,

day = "1",

doi = "10.1016/S0960-894X(00)80541-7",

language = "English",

volume = "2",

pages = "839--844",

journal = "Bioorganic and Medicinal Chemistry Letters",

issn = "0960-894X",

publisher = "Elsevier Ltd.",

number = "8",

}

Fisher, A, Gurwitz, D, Barak, D, Haring, R, Karton, I, Brandeis, R, Pittel, Z, Marciano, D, Meshulam, H, Vogel, Z & Heldman, E 1992, 'Rigid analogs of acetylcholine can be m1-selective agonists: implications for a rational treatment strategy in Alzheimer's disease', Bioorganic and Medicinal Chemistry Letters, vol. 2, no. 8, pp. 839-844. https://doi.org/10.1016/S0960-894X(00)80541-7

TY - JOUR

T1 - Rigid analogs of acetylcholine can be m1-selective agonists

T2 - implications for a rational treatment strategy in Alzheimer's disease

AU - Fisher, Abraham

AU - Gurwitz, David

AU - Barak, Dov

AU - Haring, Rachel

AU - Karton, Ishai

AU - Brandeis, Rachel

AU - Pittel, Zipora

AU - Marciano, Daniele

AU - Meshulam, Haim

AU - Vogel, Zvi

AU - Heldman, Eliahu

PY - 1992/1/1

Y1 - 1992/1/1

N2 - Rigid analogs of acetylcholine offer an opportunity for selective actions at muscarinic receptor subtypes, since restricted conformational mobility alters the capacity of ligands to adapt to subtle differences in receptor structure. AF102B, a highly rigid analog of acetylcholine, is a centrally active M1 agonist and is evaluated in light of some currently available therapeutic strategies in Alzheimer's disease.

AB - Rigid analogs of acetylcholine offer an opportunity for selective actions at muscarinic receptor subtypes, since restricted conformational mobility alters the capacity of ligands to adapt to subtle differences in receptor structure. AF102B, a highly rigid analog of acetylcholine, is a centrally active M1 agonist and is evaluated in light of some currently available therapeutic strategies in Alzheimer's disease.

UR - http://www.scopus.com/inward/record.url?scp=0026657437&partnerID=8YFLogxK

U2 - 10.1016/S0960-894X(00)80541-7

DO - 10.1016/S0960-894X(00)80541-7

M3 - Article

AN - SCOPUS:0026657437

SN - 0960-894X

VL - 2

SP - 839

EP - 844

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 8

ER -

Rigid analogs of acetylcholine can be m1-selective agonists: implications for a rational treatment strategy in Alzheimer's disease

Abstract

ASJC Scopus subject areas

Access to Document

Other files and links

Fingerprint

Cite this