Erowid References Database
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Williams M, Martin GE.
“Selectivity of cyproheptadine as assessed by radioligand binding”.
J. Pharm.Pharmacol.. 1982;34:58-59.
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Abstract
Cyproheptadine is:widely used experimentally as an anti-5-hydroxytrytaminergic, antihistaminic and antiacetylcholine drug, these intrinsic properties being well established (Stone et al 1961). More recently, studies on cyproheptadine inhibition of insulin secretion (Donatsch et al 1980) have led to the suggestion that the drug interacts with calcium channels and in so doing produced its in vivo pharmacological effects. Examination of cyproheptadine in radioligand receptor-binding assays shoed that it was some five orders of magnitude more active in displacing appropriate radioligands from central histamine, 5-HT-2 and muscarinic cholinergic receptor sites than in inhibiting depolarization dependent calcium fluxes (Donatsch et al 1980). Radioligand binding to central receptors was measured using membranes prepared from rat brain by described methods as follows (with final radioligand concentration and tissue proparation) muscarinic cholinergic ([3H]quinuclidinyl benzylate ([3H]QNB); 60 pM; rat cortical S1 fraction; Yamamura & Snyder 1974); alpha-adrenoceptor ([3H]WB 4101; 0.2 nM, rat forebrain; Greenberg et al 1976); beta-adrenoreceptor ([3H]-dihydroalprenolol ([3H]DHA); 1.0 nM; rat cortical P2 fraction; Bylund & Snyder 1976); dopamine ([3H]-apomorphine; 0.2 nM; rat caudate; Seeman et al 1976) neuroleptic ([3H]spiroperidol; 0.1 nM; rat caudate; Burt et al 1976); 5HT-1 ([3H]5-HT; 4 nM; rat forebrain, Bennett & Snyder 1976); 5HT-2 ([3H]mianserin; rat forebrain; 0.75 nM; Peroutka & Snyder 1981); 5-HT-1 and 2 ([3H]lysergic acid diethylamide (LSD); 2 nM; rat forebrain; Bennett & Snyder 1976); GABA ([3H]GABA; 10 nM; whole brain crude synaptic membranes; Enna & Snyder 1977); anxiolytic ([3H]diazpam; 1.5 nM; rat cortical P2 fraction; Squires & Braestrap 1977); adenosine A-1; ([3H]2-chloroadenosine (2-CADO; 1.0 nM; whole brain crude synaptic membranes; Williams & Risley 1980). Examination of cyproheptadine in eleven receptor binding assays (Table 1) confirmed the
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