[3H]Pirenzepine Identifies Putative M1 Muscarinic Receptors in Human Stellate Ganglia
Authors
Affiliations
The specific binding of [3H]pirenzepine ( [3H]PZ) and [3H](-) quinuclidinyl benzilate ( [3H](-)QNB) was investigated in homogenates of human stellate ganglia. [3H]PZ saturation isotherms yielded a Kd of 14 nM and Bmax of 16.7 fmol/mg protein, while [3H](-)QNB binding curves yielded a Kd of 59 pM and Bmax of 33.0 fmol/mg protein. This represents the greatest proportion of high affinity [3H]PZ labeling, relative to [3H](-)QNB, seen in any peripheral tissue examined thus far.
Valuskova P, Farar V, Forczek S, Krizova I, Myslivecek J Front Pharmacol. 2018; 9:124.
PMID: 29515448 PMC: 5826229. DOI: 10.3389/fphar.2018.00124.
The Concise Guide to PHARMACOLOGY 2013/14: G protein-coupled receptors.
Alexander S, Benson H, Faccenda E, Pawson A, Sharman J, Spedding M Br J Pharmacol. 2014; 170(8):1459-581.
PMID: 24517644 PMC: 3892287. DOI: 10.1111/bph.12445.
Berrie C, Birdsall N, Hulme E, Keen M, Stockton J Br J Pharmacol. 1985; 85(3):697-703.
PMID: 4027484 PMC: 1916521. DOI: 10.1111/j.1476-5381.1985.tb10566.x.
Carmine A, Brogden R Drugs. 1985; 30(2):85-126.
PMID: 3928324 DOI: 10.2165/00003495-198530020-00001.
Birdsall N, Hulme E, Keen M Br J Pharmacol. 1986; 87(2):307-16.
PMID: 3754173 PMC: 1916543. DOI: 10.1111/j.1476-5381.1986.tb10819.x.