Erowid References Database
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Peroutka SJ, Moskowitz MA, Reinhard JF, Snyder SH.
“Neurotransmitter Receptor Binding in Bovine Cerebral Microvessels”.
Science. 1980;208(4444):610-2.
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Abstract
Receptor binding for neurotransmitters and drugs was studied in bovine cerebral microvessels (CM). Receptor binding was studied in CM and membrane fractions (MF) obtained from calf cortical gray matter homogenates. Drug competition was determined at alpha-adrenergic sites against 3H aminoclonidine and 3H WB-4101, at beta-adrenergic sites against 3H dihydroalprenol, and histamine 1 sites against 3H mepyramine. Binding of 0.6 nM 3H aminoclonidine and 0.9 nM 3H WB-4101 in the CM was about 50% that of MF. 0.8 nM 3H Dihydroalprenolol binding in the CM and 2.0 nM 3H mepyramine labeling of histamine 1 receptors were 30% and 65%, respectively, of MF preparations. Only very low levels for 3H-5HT, 3H spiroperidol (both 2 nM) and 3.7 nM D-3H LSD binding to 5-HT receptors, for 1.4 nM D-3H Ala-Leu-enkephalin and 1.9 nM 3H naloxone binding to opiate receptors, to 0.7 nM 3H flunitrazopam binding to benzodiapine receptors and for 0.2 nM 3H quinuclidinyl benzilate binding to muscarinic cholinergic receptors was obtained for CM. In drug competition binding studies (-) epinephrine was more potent than the (+) isomer at alpha-adrenergic sites of CM and MF. WB-4101 and prazosin were equipotent at CM and MF alpha-adrenergic sites. Isoproterenol was more potent than norepinephrine and epinephrine at beta-adrenergic sites. (-) Epinephrine was more potent than (+) epinephrine. D-Chlorpheniramine was more potent than L-chlorpheniramine and mepyramine more potent than histamine at histamine- 1 sites.
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