PMID- 2307237
OWN - NLM
STAT- MEDLINE
DCOM- 19900406
LR  - 20220423
IS  - 0014-5793 (Print)
IS  - 1873-3468 (Electronic)
IS  - 0014-5793 (Linking)
VI  - 261
IP  - 1
DP  - 1990 Feb 12
TI  - Characterization of the locomotor depression produced by an A2-selective 
      adenosine agonist.
PG  - 67-70
AB  - Adenosine analogs, such as N6-cyclohexyladenosine (CHA) that are selective for 
      A1-adenosine receptors, and analogs, such as 5'-N-ethylcarboxamidoadenosine 
      (NECA) that are active at both A1 and A2 receptors, cause a profound depression 
      of locomotor activity in mice via a central mechanism. The depression is 
      effectively reversed by non-selective adenosine antagonists such as theophylline. 
      We report that 2-([2-aminoethylamino) 
      carbonylethylphenylethylamino]-5'-N-ethylcarboxamidoadenosine (APEC), an amine 
      derivative of the A2-selective agonist, CGS21680, is a potent locomotor 
      depressant in mice. The in vivo pharmacology is consistent with A2-selectivity at 
      a central site of action. Two parameters indicative of locomotor activity, 
      horizontal activity and total distance travelled, were measured using a 
      computerized activity monitor. From dose-response curves it was found that APEC 
      (ED50 16 micrograms/kg) is more potent than CHA (ED50 60 micrograms/kg) and less 
      potent than NECA (ED50 2 micrograms/kg). The locomotor depression by APEC was 
      reversible by theophylline, but not by the A1-selective antagonists 
      8-cyclopentyltheophylline (CPT) and 8-cyclopentyl-1, 3-dipropyl-2-thioxanthine, 
      nor by the peripheral antagonists 8-p-sulfophenyltheophylline (8-PST) and 
      1,3-dipropyl-8-p-sulfophenylxanthine. The locomotor activity depression elicited 
      by NECA and CHA was reversed by A1-selective antagonists. These results suggest 
      that the effects of APEC are due to stimulation of A2 adenosine receptors in the 
      brain.
FAU - Nikodijevic, O
AU  - Nikodijevic O
AD  - Laboratory of Chemistry, National Inst. of Diabetes, Digestive and Kidney 
      Diseases, National Institutes of Health, Bethesda, MD 20892.
FAU - Daly, J W
AU  - Daly JW
FAU - Jacobson, K A
AU  - Jacobson KA
LA  - eng
GR  - Z99 DA999999/ImNIH/Intramural NIH HHS/United States
GR  - Z01 DK031117/ImNIH/Intramural NIH HHS/United States
GR  - Z01 DK031117-20/ImNIH/Intramural NIH HHS/United States
GR  - Z99 OD999999/ImNIH/Intramural NIH HHS/United States
GR  - Z99 DK999999/ImNIH/Intramural NIH HHS/United States
PT  - Comparative Study
PT  - Journal Article
PL  - England
TA  - FEBS Lett
JT  - FEBS letters
JID - 0155157
RN  - 0 (Phenethylamines)
RN  - 0 (Receptors, Purinergic)
RN  - 126828-50-0 
      (2-((2-aminoethylamino)carbonylethylphenylethylamino)-5'-N-ethylcarboxamidoadenosine)
RN  - 35920-39-9 (Adenosine-5'-(N-ethylcarboxamide))
RN  - 36396-99-3 (N(6)-cyclohexyladenosine)
RN  - C137DTR5RG (Theophylline)
RN  - K72T3FS567 (Adenosine)
SB  - IM
MH  - Adenosine/*analogs & derivatives/pharmacology
MH  - Adenosine-5'-(N-ethylcarboxamide)
MH  - Animals
MH  - Male
MH  - Mice
MH  - Molecular Structure
MH  - Motor Activity/*drug effects
MH  - Phenethylamines/*pharmacology
MH  - Receptors, Purinergic/drug effects/*physiology
MH  - Theophylline/pharmacology
PMC - PMC3469261
MID - NIHMS406056
EDAT- 1990/02/12 00:00
MHDA- 1990/02/12 00:01
PMCR- 2012/10/11
CRDT- 1990/02/12 00:00
PHST- 1990/02/12 00:00 [pubmed]
PHST- 1990/02/12 00:01 [medline]
PHST- 1990/02/12 00:00 [entrez]
PHST- 2012/10/11 00:00 [pmc-release]
AID - 0014-5793(90)80638-Y [pii]
AID - 10.1016/0014-5793(90)80638-y [doi]
PST - ppublish
SO  - FEBS Lett. 1990 Feb 12;261(1):67-70. doi: 10.1016/0014-5793(90)80638-y.