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Abstract

Alpha-2 adrenoceptor in rat jejunum epithelial cells: characterization with [3H]RX821002 and distribution along the villus-crypt axis.

H Paris, T Voisin, A Remaury, C Rouyer-Fessard, D Daviaud, D Langin and M Laburthe
Journal of Pharmacology and Experimental Therapeutics September 1990, 254 (3) 888-893;
H Paris
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T Voisin
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A Remaury
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C Rouyer-Fessard
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D Daviaud
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D Langin
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M Laburthe
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Abstract

Alpha-2 adrenergic receptivity of rat jejunum epithelial cells was studied using the new antagonist radioligand, [3H]RX821002 [( 3H]-2-(2-methoxy-1,4-benzodioxan-2-yl)-2-imidazoline). All the parameters of [3H]RX821002 binding were consistent with the labeling of an alpha-2 adrenoceptor. The use of this probe was moreover extremely convenient, because contrarily to [3H]yohimbine and [3H]rauwolscine, [3H]RX821002 displayed in this tissue a very high affinity (Kd = 0.54 +/- 0.12 nM) and a low level of nonspecific binding (5% at 1 nM [3H]RX821002). Competition studies with various antagonists and agonists showed that the labeled sites were alpha-2-selective and stereospecific. Oxymetazoline was much more potent than chlorpromazine or prazosin suggesting that the receptor is of the alpha-2-subtype. Yohimbine and rauwolscine were equipotent, which is also in agreement with the pharmacological definition of this subtype. These two compounds displayed, however, a rather weak affinity (Ki approximately 40 nM), which is somewhat different with what one should expect for a true alpha-2A adrenoceptor. Altogether the competition data indicated that the alpha-2 adrenoceptor from rat jejunal epithelium is neither an alpha-2A, nor an alpha-2B, nor an alpha-2c adrenoceptor and may belong to a fourth subtype.(ABSTRACT TRUNCATED AT 250 WORDS)

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Journal of Pharmacology and Experimental Therapeutics
Vol. 254, Issue 3
1 Sep 1990
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Abstract

Alpha-2 adrenoceptor in rat jejunum epithelial cells: characterization with [3H]RX821002 and distribution along the villus-crypt axis.

H Paris, T Voisin, A Remaury, C Rouyer-Fessard, D Daviaud, D Langin and M Laburthe
Journal of Pharmacology and Experimental Therapeutics September 1, 1990, 254 (3) 888-893;

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Abstract

Alpha-2 adrenoceptor in rat jejunum epithelial cells: characterization with [3H]RX821002 and distribution along the villus-crypt axis.

H Paris, T Voisin, A Remaury, C Rouyer-Fessard, D Daviaud, D Langin and M Laburthe
Journal of Pharmacology and Experimental Therapeutics September 1, 1990, 254 (3) 888-893;
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