Abstract：
:The effects of phencyclidine [1-(1-phenylcyclohexyl)-piperidine; PCP] on cardiac action potential duration (APD) were compared to those of some of its derivatives, in strips of isolated frog ventricular muscle perfused with normal Ringer solution. We studied compounds with PCP-like behavioral actions (N-ethyl-1-phenyl-cyclohexylamine: PCE; and m-amino-PCP) as well as behaviorally inactive analogs (m-nitro-PCP; the quaternary derivative PCP-methyl iodide; and various fragments of the PCP molecule). Exposure to PCP, 3 microM to 1 mM, produced reversible, dose- and pH-dependent prolongations, of the APD to over 100% above control. The observed effects of the drugs are compatible with a mechanism of blockade of potassium conductance. An intracellular site for this action is suggested by: (i) the inactivity of the quaternary analog; (ii) the marked increase in the potency of the compounds when the external pH is changed in the region of their respective pKa values to increase the concentration of the unionized species; and (iii) the pronounced acceleration of the termination of the PCP effect by washout with a series of buffer solutions with decreasing pH values. The rank order of potency of the compounds in lengthening APD (PCE greater than m-amino PCP greater than PCP much much greater than m-nitro-PCP) is the same as reported from other pharmacological studies of specific PCP actions, and matches the rank of behavioral activity of the drugs.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
D'Amico GA,Kline RP,Maayani S,Weinstein H,Kupersmith Jdoi
10.1016/0014-2999(83)90578-2subject
Has Abstractpub_date
1983-04-08 00:00:00pages
283-90issue
4eissn
0014-2999issn
1879-0712pii
0014-2999(83)90578-2journal_volume
88pub_type
杂志文章abstract：:Using 3H-ligands and radioactive microspheres we studied the binding characteristics and the effects on the distribution of carotid arterial blood flow of n-(3-acetylaminophenyl)piperazine hydrochloride (BEA 1654). The compound had a Ki value of 32 nM (5-HT: 8 nM) on 5-HT1 but no or very weak affinity for 5-HT2, alpha...
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journal_title：European journal of pharmacology
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journal_title：European journal of pharmacology
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journal_title：European journal of pharmacology
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abstract：:The action of a new effective antiarrhythmic agent, encainide, was studied with respect to the mechanical performance of isolated cat papillary muscle. Encainide (0.1-10 micrograms/ml) did not alter the performance of cardiac muscle during either the contraction or relaxation phase. By contrast, lidocaine (1-5 microgr...
journal_title：European journal of pharmacology
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doi：10.1016/0014-2999(81)90511-2
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