2010年6月
Functional and pharmacological characterization of a beta-adrenergic-like octopamine receptor from the silkworm Bombyx mori
INSECT BIOCHEMISTRY AND MOLECULAR BIOLOGY
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- 巻
- 40
- 号
- 6
- 開始ページ
- 476
- 終了ページ
- 486
- 記述言語
- 英語
- 掲載種別
- DOI
- 10.1016/j.ibmb.2010.04.007
- 出版者・発行元
- PERGAMON-ELSEVIER SCIENCE LTD
A cDNA encoding a seven-transmembrane receptor was cloned from the nervous tissues of silkworm (Bombyx mori) larvae. Sequence analysis indicated that the gene is an ortholog of CG6989, which encodes a Drosophila beta-adrenergic-like octopamine (OA) receptor (DmOct beta 2R). As very little information is available regarding this class of receptors, we generated a cell line that stably expressed the gene in HEK-293 cells and we then performed functional and pharmacological studies of this receptor. [(3)H]OA-binding assays using membrane preparations of this cell line showed that the receptor possesses a higher affinity for OA than for tyramine (TA) or dopamine (DA). The cell line elicited a bell-shaped, OA concentration-dependent increase in intracellular cAMP levels, with a maximum at 100 nM. (R)-OA was more potent than (S)-OA. TA and DA had weak or marginal effects on cAMP production. The OA receptor agonist demethylchlordimeform elicited a similar biphasic response, although the maximum response was attained at a concentration as low as 1 nM. The rank order of potency of other agonists was as follows: naphazoline > tolazoline, clonidine. Among the antagonists tested, only chlorpromazine significantly attenuated the OA-induced increase in cAMP levels. No increase in intracellular Ca(2+) levels was observed with OA at concentrations up to 100 mu M. These findings indicate that the cloned receptor is a beta-adrenergic-like OA receptor with unique functional and pharmacological properties. (C) 2010 Elsevier Ltd. All rights reserved.
- リンク情報
- ID情報
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- DOI : 10.1016/j.ibmb.2010.04.007
- ISSN : 0965-1748
- Web of Science ID : WOS:000279368700006