PMID- 9772088
OWN - NLM
STAT- MEDLINE
DCOM- 19981022
LR  - 20191210
IS  - 0300-483X (Print)
IS  - 0300-483X (Linking)
VI  - 129
IP  - 2-3
DP  - 1998 Aug 21
TI  - Phencyclidine block of Ca2+ ATPase in rat heart sarcoplasmic reticulum.
PG  - 95-102
AB  - Phencyclidine hydrochloride (PCP) also known as Angel Dust is a very potent 
      psychotomimetic drug of abuse. Besides its central nervous system (CNS) effects 
      PCP produces a number of adverse effects in a variety of tissues including the 
      cardiovascular system. Since PCP is known to alter the cellular calcium 
      homeostasis the present studies were initiated to determine the changes in 
      cardiac Ca2+ ATPase activity in rats treated with PCP. For in vitro studies the 
      cardiac sarcoplasmic reticulum (SR) fractions prepared from normal rats were 
      incubated with 25, 50 and 100 microM PCP and the enzyme activities were 
      estimated. Whereas, for in vivo studies the cardiac SR fractions prepared from 
      rats treated with PCP (10 mg/kg body wt. single dose, intra-peritoneally (i.p.)) 
      and sacrificed at different time intervals were used. PCP reduced the Ca2+ ATPase 
      activity significantly both in vitro and in vivo. A 50% inhibition of the enzyme 
      activity was obtained with 100 microM PCP in vitro. A significant reduction of SR 
      Ca2+ ATPase was also evident as early as 1 h after treatment of rats with PCP. 
      The reduction of Ca2+ ATPase activity in SR was irreversible even at 12 h after 
      treatment. The in vitro kinetic studies revealed that PCP was found to be a 
      competitive inhibitor of Ca2+ ATPase with respect to the substrate, ATP, and 
      non-competitive with respect to Ca2+ activation. These results indicate that PCP 
      alters the myocardial Ca2+ homeostasis by inhibiting the Ca2+ ATPase in cardiac 
      SR in rats. Inhibition of SR Ca2+ ATPase may result in the impairment of 
      contraction and relaxation coupling processes in the myocardium.
FAU - Pande, M
AU  - Pande M
AD  - Department of Neurology, University of Mississippi School of Medicine, Jackson 
      39216-4505, USA.
FAU - Cameron, J A
AU  - Cameron JA
FAU - Vig, P J
AU  - Vig PJ
FAU - Desaiah, D
AU  - Desaiah D
LA  - eng
GR  - T32 HL 07635/HL/NHLBI NIH HHS/United States
PT  - Journal Article
PT  - Research Support, U.S. Gov't, P.H.S.
PL  - Ireland
TA  - Toxicology
JT  - Toxicology
JID - 0361055
RN  - EC 7.2.2.10 (Calcium-Transporting ATPases)
RN  - J1DOI7UV76 (Phencyclidine)
RN  - SY7Q814VUP (Calcium)
SB  - IM
MH  - Animals
MH  - Calcium/metabolism
MH  - Calcium-Transporting ATPases/*antagonists & inhibitors
MH  - Heart/*drug effects
MH  - Male
MH  - Myocardium/enzymology
MH  - Phencyclidine/*toxicity
MH  - Rats
MH  - Rats, Sprague-Dawley
MH  - Sarcoplasmic Reticulum/*drug effects/enzymology
EDAT- 1998/10/15 00:00
MHDA- 1998/10/15 00:01
CRDT- 1998/10/15 00:00
PHST- 1998/10/15 00:00 [pubmed]
PHST- 1998/10/15 00:01 [medline]
PHST- 1998/10/15 00:00 [entrez]
AID - S0300-483X(98)00061-4 [pii]
AID - 10.1016/s0300-483x(98)00061-4 [doi]
PST - ppublish
SO  - Toxicology. 1998 Aug 21;129(2-3):95-102. doi: 10.1016/s0300-483x(98)00061-4.