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Abstract

Binding of a radiolabeled triazolopyridazine to a subtype of benzodiazepine receptor in the rat cerebellum.

D L Niehoff, R D Mashal, W D Horst, R A O'Brien, J M Palacios and M J Kuhar
Journal of Pharmacology and Experimental Therapeutics June 1982, 221 (3) 670-675;
D L Niehoff
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R D Mashal
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W D Horst
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R A O'Brien
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J M Palacios
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M J Kuhar
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Abstract

The triazolopyridazine (TPZ) drugs, typified by CL218,872 (CL), have a relatively higher affinity for a subpopulation of benzodiazepine (BZ) receptors. The binding of radiolabeled CL to membranes from rat cerebellum, a region enriched in the TPZ-preferring ("Type 1") BZ receptor, was characterized and compared with that of [3H]flunitrazepam ([3H]FLU) in the same preparation. [3H]CL had clonazepam displaceable binding which was saturable. The Kd was approximately 21 nM and the Bmax was approximately 600 fmol/mg of protein. [3H]CL binding was similar to that for [3H]FLU in that exogenous gamma-aminobutyric acid (GABA) enhanced the binding; however, [3H]CL binding differed from that for [3H]FLU in that anions, cartazolate and pentobarbital did not enhance [3H]CL binding. These data suggest that [3H]CL binds to the Type 1 BZ receptor in a manner different from that of a BZ drug such as FLU. Inasmuch as GABA enhances [3H]CL binding, but anions, cartazolate and pentobarbital do not, [3H]CL may bind to the Type 1 BZ receptor in such a way that it interacts with the GABA site, but perhaps not directly with the ionophore or the postulated pyrazolopyridine-barbiturate site. Thus, TPZ drugs may affect the GABA receptor complex in a different or perhaps less extensive way than the BZs. This, in addition to the regional localization of the Type 1 receptor, may be an important part of the mechanism of action of the TPZs.

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Journal of Pharmacology and Experimental Therapeutics
Vol. 221, Issue 3
1 Jun 1982
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Abstract

Binding of a radiolabeled triazolopyridazine to a subtype of benzodiazepine receptor in the rat cerebellum.

D L Niehoff, R D Mashal, W D Horst, R A O'Brien, J M Palacios and M J Kuhar
Journal of Pharmacology and Experimental Therapeutics June 1, 1982, 221 (3) 670-675;

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Abstract

Binding of a radiolabeled triazolopyridazine to a subtype of benzodiazepine receptor in the rat cerebellum.

D L Niehoff, R D Mashal, W D Horst, R A O'Brien, J M Palacios and M J Kuhar
Journal of Pharmacology and Experimental Therapeutics June 1, 1982, 221 (3) 670-675;
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