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| Predicate | Object |
|---|---|
| rdf:type | |
| lifeskim:mentions | |
| pubmed:issue |
4
|
| pubmed:dateCreated |
1992-4-23
|
| pubmed:abstractText |
Radioligand-binding experiments were performed with crude membrane homogenates (CMH) from human skin in order to investigate the epidermal beta-adrenergic receptor (beta AR) density. CMH were prepared from leftovers of split-thickness skin grafts by sequential homogenization and centrifugation procedures to yield essentially epidermal fragments. Saturation experiments with the non-selective beta-adrenoceptor antagonist (-)-[125I]-iodocyanopindolol (ICYP) as radioligand showed saturable specific binding isotherms. Scatchard transformation of the data demonstrated high-affinity binding of ICYP to a single class of beta AR (Bmax = 80 +/- 10 fmol/mg protein; KD = 8 pM +/- 0.9; n = 8). beta AR antagonists displaced ICYP in a monophasic displacement pattern. The IC50 values were (nmol/1) propranolol (non-selective) 24.8; ICI 118,551 (beta 2 selective) 14.7; CGP-12177 (non-selective) 28.9; bisoprolol (beta 1 selective) 1500; CGP-20712A (beta 1 selective) 8990. beta AR agonists displaced ICYP with a potency ranking isoprenaline greater than adrenaline greater than noradrenaline. We conclude that epidermal crude membrane homogenates prepared from human split-thickness skin contain a high population of beta 2-adrenergic receptors. These receptors may be studied to further investigate the nature of human epidermal beta-adrenergic mechanisms.
|
| pubmed:language |
eng
|
| pubmed:journal | |
| pubmed:citationSubset |
IM
|
| pubmed:chemical | |
| pubmed:status |
MEDLINE
|
| pubmed:month |
Apr
|
| pubmed:issn |
0022-202X
|
| pubmed:author | |
| pubmed:issnType |
Print
|
| pubmed:volume |
98
|
| pubmed:owner |
NLM
|
| pubmed:authorsComplete |
Y
|
| pubmed:pagination |
475-80
|
| pubmed:dateRevised |
2004-11-17
|
| pubmed:meshHeading |
pubmed-meshheading:1312566-Adult,
pubmed-meshheading:1312566-Aged,
pubmed-meshheading:1312566-Female,
pubmed-meshheading:1312566-Humans,
pubmed-meshheading:1312566-Keratinocytes,
pubmed-meshheading:1312566-Male,
pubmed-meshheading:1312566-Membranes,
pubmed-meshheading:1312566-Microscopy, Electron,
pubmed-meshheading:1312566-Middle Aged,
pubmed-meshheading:1312566-Protein Binding,
pubmed-meshheading:1312566-Receptors, Adrenergic, beta,
pubmed-meshheading:1312566-Skin
|
| pubmed:year |
1992
|
| pubmed:articleTitle |
Binding of beta-adrenergic receptors in human skin.
|
| pubmed:affiliation |
Department of Dermatology, University of Hamburg, Germany.
|
| pubmed:publicationType |
Journal Article
|