Abstract
Five human pancreatic carcinoma cell lines were screened for the presence of muscarinic cholinergic receptors (mAChRs), using [<sup>3</sup>H]7V-meth-ylscopolamine ([<sup>3</sup>H]NMS). T3M4 and COLO-357 cells exhibited specific, high-affinity binding to mAChRs. A small amount of [<sup>3</sup>H]NMS also bound in PANC-I and ASPC-I cells, but not in MIA PaCa-2 cells. Atropine, pirenzepine (PZ), and ll-[[2-[(diethylamino) methyl]-1-piperidinyl] acetyl]-5, ll-dihydro-6H-pyrido-[2, 3-b][l, 4] benzodiazepine-6-one (AF-DX 116) inhibited [3H]NMS binding and carbachol-mediated [3H]inositol monophosphate formation in both T3M4 and COLO-357 cells. The order of inhibition was: Atropine > PZ > AF-DX 116. Carbachol did not alter [3H]inositol monophosphate formation in the other cell lines. These findings suggest that the mAChRs expressed in some human pancreatic cancer cells exhibit the pharmacologic characteristics of a muscarinic receptor subtype with an intermediate affinity for PZ and a lower affinity for AF-DX 116 and are functionally coupled to activation of phospholipid hydrolysis.
| Original language | English (US) |
|---|---|
| Pages (from-to) | 1-2 |
| Number of pages | 2 |
| Journal | Pancreas |
| Volume | 4 |
| Issue number | 3 |
| State | Published - 1989 |
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Keywords
- Muscarinic receptors
- Pancreatic carcinomas
- Phospholipid hydrolysis
ASJC Scopus subject areas
- Endocrinology
- Endocrinology, Diabetes and Metabolism
- Hepatology
- Internal Medicine
Cite this
Identification and characterization of muscarinic receptors in cultured human pancreatic carcinoma cells. / Ackerman, Martha S.; Roeske, William R; Heck, Richard J.; Korc, Murray.
In: Pancreas, Vol. 4, No. 3, 1989, p. 1-2.Research output: Contribution to journal › Article
}
TY - JOUR
T1 - Identification and characterization of muscarinic receptors in cultured human pancreatic carcinoma cells
AU - Ackerman, Martha S.
AU - Roeske, William R
AU - Heck, Richard J.
AU - Korc, Murray
PY - 1989
Y1 - 1989
N2 - Five human pancreatic carcinoma cell lines were screened for the presence of muscarinic cholinergic receptors (mAChRs), using [3H]7V-meth-ylscopolamine ([3H]NMS). T3M4 and COLO-357 cells exhibited specific, high-affinity binding to mAChRs. A small amount of [3H]NMS also bound in PANC-I and ASPC-I cells, but not in MIA PaCa-2 cells. Atropine, pirenzepine (PZ), and ll-[[2-[(diethylamino) methyl]-1-piperidinyl] acetyl]-5, ll-dihydro-6H-pyrido-[2, 3-b][l, 4] benzodiazepine-6-one (AF-DX 116) inhibited [3H]NMS binding and carbachol-mediated [3H]inositol monophosphate formation in both T3M4 and COLO-357 cells. The order of inhibition was: Atropine > PZ > AF-DX 116. Carbachol did not alter [3H]inositol monophosphate formation in the other cell lines. These findings suggest that the mAChRs expressed in some human pancreatic cancer cells exhibit the pharmacologic characteristics of a muscarinic receptor subtype with an intermediate affinity for PZ and a lower affinity for AF-DX 116 and are functionally coupled to activation of phospholipid hydrolysis.
AB - Five human pancreatic carcinoma cell lines were screened for the presence of muscarinic cholinergic receptors (mAChRs), using [3H]7V-meth-ylscopolamine ([3H]NMS). T3M4 and COLO-357 cells exhibited specific, high-affinity binding to mAChRs. A small amount of [3H]NMS also bound in PANC-I and ASPC-I cells, but not in MIA PaCa-2 cells. Atropine, pirenzepine (PZ), and ll-[[2-[(diethylamino) methyl]-1-piperidinyl] acetyl]-5, ll-dihydro-6H-pyrido-[2, 3-b][l, 4] benzodiazepine-6-one (AF-DX 116) inhibited [3H]NMS binding and carbachol-mediated [3H]inositol monophosphate formation in both T3M4 and COLO-357 cells. The order of inhibition was: Atropine > PZ > AF-DX 116. Carbachol did not alter [3H]inositol monophosphate formation in the other cell lines. These findings suggest that the mAChRs expressed in some human pancreatic cancer cells exhibit the pharmacologic characteristics of a muscarinic receptor subtype with an intermediate affinity for PZ and a lower affinity for AF-DX 116 and are functionally coupled to activation of phospholipid hydrolysis.
KW - Muscarinic receptors
KW - Pancreatic carcinomas
KW - Phospholipid hydrolysis
UR - http://www.scopus.com/inward/record.url?scp=84934741466&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=84934741466&partnerID=8YFLogxK
M3 - Article
C2 - 2734280
AN - SCOPUS:84934741466
VL - 4
SP - 1
EP - 2
JO - Pancreas
JF - Pancreas
SN - 0885-3177
IS - 3
ER -