BIOMAT Database Logo BIOMAT Database Logo

Guanine nucleotide-induced positive cooperativity in muscarinic-cholinergic antagonist binding. 1986

J L Boyer, and M Martínez-Cárcamo, and J A Monroy-Sánchez, and C Posadas, and J A García-Sáinz

The effect of guanine nucleotides on the binding of [3H] Quinuclidinyl benzilate to heart muscarinic receptors was studied. It was observed that GTP and Gpp (NH)p increased antagonist binding. Scatchard transformation of the data resulted in curvilinear plots (downward concavity) consistent with positive cooperativity. Graphic analysis for cooperativity indicated that guanine nucleotides: a) increased slightly but consistently the affinity for the antagonist (independent of receptor occupancy) and b) induce positive cooperativity in the binding of [3H]QNB (dependent of receptor occupancy).

UI MeSH Term Description Entries
D007700 Kinetics The rate dynamics in chemical or physical systems.
D008297 Male Males
D009206 Myocardium The muscle tissue of the HEART. It is composed of striated, involuntary muscle cells (MYOCYTES, CARDIAC) connected to form the contractile pump to generate blood flow. Muscle, Cardiac,Muscle, Heart,Cardiac Muscle,Myocardia,Cardiac Muscles,Heart Muscle,Heart Muscles,Muscles, Cardiac,Muscles, Heart
D011813 Quinuclidinyl Benzilate A high-affinity muscarinic antagonist commonly used as a tool in animal and tissue studies. Benzilate, Quinuclidinyl
D011919 Rats, Inbred Strains Genetically identical individuals developed from brother and sister matings which have been carried out for twenty or more generations or by parent x offspring matings carried out with certain restrictions. This also includes animals with a long history of closed colony breeding. August Rats,Inbred Rat Strains,Inbred Strain of Rat,Inbred Strain of Rats,Inbred Strains of Rats,Rat, Inbred Strain,August Rat,Inbred Rat Strain,Inbred Strain Rat,Inbred Strain Rats,Inbred Strains Rat,Inbred Strains Rats,Rat Inbred Strain,Rat Inbred Strains,Rat Strain, Inbred,Rat Strains, Inbred,Rat, August,Rat, Inbred Strains,Rats Inbred Strain,Rats Inbred Strains,Rats, August,Rats, Inbred Strain,Strain Rat, Inbred,Strain Rats, Inbred,Strain, Inbred Rat,Strains, Inbred Rat
D011950 Receptors, Cholinergic Cell surface proteins that bind acetylcholine with high affinity and trigger intracellular changes influencing the behavior of cells. Cholinergic receptors are divided into two major classes, muscarinic and nicotinic, based originally on their affinity for nicotine and muscarine. Each group is further subdivided based on pharmacology, location, mode of action, and/or molecular biology. ACh Receptor,Acetylcholine Receptor,Acetylcholine Receptors,Cholinergic Receptor,Cholinergic Receptors,Cholinoceptive Sites,Cholinoceptor,Cholinoceptors,Receptors, Acetylcholine,ACh Receptors,Receptors, ACh,Receptor, ACh,Receptor, Acetylcholine,Receptor, Cholinergic,Sites, Cholinoceptive
D011976 Receptors, Muscarinic One of the two major classes of cholinergic receptors. Muscarinic receptors were originally defined by their preference for MUSCARINE over NICOTINE. There are several subtypes (usually M1, M2, M3....) that are characterized by their cellular actions, pharmacology, and molecular biology. Muscarinic Acetylcholine Receptors,Muscarinic Receptors,Muscarinic Acetylcholine Receptor,Muscarinic Receptor,Acetylcholine Receptor, Muscarinic,Acetylcholine Receptors, Muscarinic,Receptor, Muscarinic,Receptor, Muscarinic Acetylcholine,Receptors, Muscarinic Acetylcholine
D006160 Guanosine Triphosphate Guanosine 5'-(tetrahydrogen triphosphate). A guanine nucleotide containing three phosphate groups esterified to the sugar moiety. GTP,Triphosphate, Guanosine
D006165 Guanylyl Imidodiphosphate A non-hydrolyzable analog of GTP, in which the oxygen atom bridging the beta to the gamma phosphate is replaced by a nitrogen atom. It binds tightly to G-protein in the presence of Mg2+. The nucleotide is a potent stimulator of ADENYLYL CYCLASES. GMP-PNP,GMP-P(NH)P,Gpp(NH)p,Guanosine 5'-(Beta,Gamma-Imido)Triphosphate,Guanyl-5'-Imidodiphosphate,P(NH)PPG,Guanyl 5' Imidodiphosphate,Imidodiphosphate, Guanylyl
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia

Related Publications

J L Boyer, and M Martínez-Cárcamo, and J A Monroy-Sánchez, and C Posadas, and J A García-Sáinz
Reciprocal modulation of agonist and antagonist binding to muscarinic cholinergic receptor by guanine nucleotide.
March 1982, Proceedings of the National Academy of Sciences of the United States of America,
J L Boyer, and M Martínez-Cárcamo, and J A Monroy-Sánchez, and C Posadas, and J A García-Sáinz
Guanine nucleotide modulation of muscarinic cholinergic receptor binding in postmortem human brain--a preliminary study in Alzheimer's disease.
November 1987, Neuroscience letters,
J L Boyer, and M Martínez-Cárcamo, and J A Monroy-Sánchez, and C Posadas, and J A García-Sáinz
Agonist and guanine nucleotide modulation of muscarinic cholinergic receptors in cultured heart cells.
October 1980, The Journal of biological chemistry,
J L Boyer, and M Martínez-Cárcamo, and J A Monroy-Sánchez, and C Posadas, and J A García-Sáinz
Two distinct, divalent cation-sensitive, antagonist binding states of heart muscarinic receptors: differential modulation by guanine nucleotide.
January 1990, General pharmacology,
J L Boyer, and M Martínez-Cárcamo, and J A Monroy-Sánchez, and C Posadas, and J A García-Sáinz
Differential modification of the interaction of cardiac muscarinic cholinergic and beta-adrenergic receptors with a guanine nucleotide binding component(s).
May 1982, Molecular pharmacology,
J L Boyer, and M Martínez-Cárcamo, and J A Monroy-Sánchez, and C Posadas, and J A García-Sáinz
Agonist-antagonist interactions with rat atrial muscarinic cholinergic receptor sites: differential regulation by guanine nucleotides.
September 1979, European journal of pharmacology,
J L Boyer, and M Martínez-Cárcamo, and J A Monroy-Sánchez, and C Posadas, and J A García-Sáinz
Cooperativity and oligomeric status of cardiac muscarinic cholinergic receptors.
April 2002, Biochemistry,
J L Boyer, and M Martínez-Cárcamo, and J A Monroy-Sánchez, and C Posadas, and J A García-Sáinz
Guanine nucleotide-sensitive, high affinity binding of carbachol to muscarinic cholinergic receptors of 1321N1 astrocytoma cells is insensitive to pertussis toxin.
January 1985, Molecular pharmacology,
J L Boyer, and M Martínez-Cárcamo, and J A Monroy-Sánchez, and C Posadas, and J A García-Sáinz
Tissue-dependent association of muscarinic acetylcholine receptors with guanine nucleotide-binding regulatory proteins.
September 1991, Molecular pharmacology,
J L Boyer, and M Martínez-Cárcamo, and J A Monroy-Sánchez, and C Posadas, and J A García-Sáinz
Positive cooperativity in the binding of alcuronium and N-methylscopolamine to muscarinic acetylcholine receptors.
November 1990, Molecular pharmacology,
Copied contents to your clipboard!