RATIONALE: Mescaline is a nonselective serotonin receptor agonist. It has relatively delayed onset of action and prolonged duration. Mescaline attenuates various behavioral parameters in rats; however, no information is available about its pharmacokinetics in rats and its relation to the behavioral changes produced by the drug. OBJECTIVES: The present study evaluates the spontaneous locomotor activity and sensorimotor gating in relation to mescaline concentrations in the serum and the brain of rats MATERIALS AND METHODS: Behavioral changes induced by mescaline [10, 20, and 100 mg/kg subcutaneously (s.c.)] were evaluated in an open-field test and testing of the prepulse inhibition of acoustic startle reaction (PPI) 15 and 60 min after drug administration. The time disposition of mescaline 20 mg/kg s.c. in rat serum and brain homogenates was analyzed by gas chromatography-mass spectrometry. RESULTS: Mescaline produced significant inhibitory effects on locomotion in low doses and a biphasic effect with the highest dose. In the PPI test, only when tested 60 min after drug administration, all doses of mescaline disrupted PPI. Besides the experimental protocol, we have observed that approximately 50% of animals receiving 100 mg/kg died within 12 h post-injection. The serum levels of mescaline rapidly increased within 30 min and subsequently quickly decreased; however, the brain concentrations reached a maximum 1 h after administration and remained high for an additional 60 min. CONCLUSIONS: Mescaline had a delayed onset of the main behavioral changes in rats compared to other hallucinogens. Behavioral changes correlated with the pharmacokinetics of the drug.

Prague Psychiatric Center Ustavní 91 181 03 Prague 8 Bohnice Czech Republic

Zobrazit více v PubMed

Forensic Sci Int. 2007 Jan 17;165(2-3):216-24 PubMed

Psychopharmacology (Berl). 2001 Jul;156(2-3):117-54 PubMed

Psychopharmacologia. 1971;22(1):64-71 PubMed

Neuropharmacology. 1999 Aug;38(8):1083-152 PubMed

Psychopharmacology (Berl). 1977 Apr 29;52(2):157-63 PubMed

Neuropharmacology. 1994 Mar-Apr;33(3-4):441-8 PubMed

Acta Neurobiol Exp (Wars). 1973;33(4):771-89 PubMed

Biol Psychiatry. 1992 Dec 1;32(11):976-91 PubMed

Pharmacol Biochem Behav. 1986 Jul;25(1):277-88 PubMed

Psychopharmacologia. 1975 May 28;42(2):163-71 PubMed

Eur J Pharmacol. 1975 Jun-Jul;32(02):156-62 PubMed

J Med Chem. 1997 Sep 12;40(19):2997-3008 PubMed

Psychopharmacology (Berl). 1979;66(3):275-80 PubMed

Experientia. 1973 May 15;29(5):571-2 PubMed

Life Sci. 1986 Sep 22;39(12):1051-8 PubMed

Psychopharmacologia. 1966;9(1):48-63 PubMed

Pharmacol Biochem Behav. 1975 Sep-Oct;3(5):923-5 PubMed

Toxicol Appl Pharmacol. 1978 Jul;45(1):49-62 PubMed

J Pharmacol Exp Ther. 1978 Jan;204(1):103-17 PubMed

J Chromatogr B Biomed Sci Appl. 1998 Apr 10;707(1-2):1-2 PubMed

Pharmacol Biochem Behav. 1995 Dec;52(4):649-54 PubMed

J Neurochem. 1995 Apr;64(4):1585-97 PubMed

Psychopharmacology (Berl). 1987;93(3):286-91 PubMed

Prog Neurobiol. 1999 Oct;59(2):107-28 PubMed

Brain Res. 1979 Feb 16;162(1):77-88 PubMed

J Pharmacol Exp Ther. 1978 Dec;207(3):837-47 PubMed

J Pharmacol Exp Ther. 2001 Jun;297(3):846-52 PubMed

Psychopharmacology (Berl). 1979 Sep;65(1):35-40 PubMed

Psychopharmacologia. 1974;39(1):43-56 PubMed

Psychopharmacology (Berl). 2006 Dec;189(3):319-29 PubMed

Behav Brain Res. 1989 Sep 1;34(3):199-211 PubMed

Tex State J Med. 1963 Sep;59:848-52 PubMed

J Pharmacol Exp Ther. 1957 Jan;119(1):78-84 PubMed

Behav Pharmacol. 1995 Dec;6(8):839-842 PubMed

Psychopharmacology (Berl). 2001 Jul;156(2-3):194-215 PubMed

Toxicol Appl Pharmacol. 1973 Jun;25(2):299-309 PubMed

Brain Res. 1997 Jun 27;761(1):97-104 PubMed

NIDA Res Monogr. 1980 Aug;32:1-198 PubMed

Behav Pharmacol. 1996 Nov;7(6):551-559 PubMed

Forensic Sci Int. 2005 Oct 4;153(1):85-91 PubMed

J Neural Transm (Vienna). 1997;104(6-7):605-14 PubMed

Pharmacol Biochem Behav. 1978 May;8(5):543-6 PubMed

Neuroscience. 1998 May;84(2):413-29 PubMed

Physiol Behav. 2005 Nov 15;86(4):546-53 PubMed

Psychopharmacology (Berl). 2004 Dec;177(1-2):46-54 PubMed

Experientia. 1970 Nov 15;26(11):1231-2 PubMed

Neuropsychopharmacology. 2001 Oct;25(4):565-75 PubMed

Psychopharmacology (Berl). 1995 Jan;117(1):41-8 PubMed

Behav Brain Res. 1993 Feb 26;53(1-2):21-33 PubMed

Psychopharmacology (Berl). 1991;105(1):69-76 PubMed

Pharmacol Ther. 2004 Feb;101(2):131-81 PubMed

Neuropsychopharmacology. 1998 May;18(5):339-51 PubMed

Eur J Pharmacol. 1983 Dec 9;96(1-2):151-4 PubMed

Pharmacol Biochem Behav. 1979 Nov;11(5):479-82 PubMed

Biol Psychiatry. 2000 Aug 1;48(3):229-37 PubMed

Life Sci. 1978 Sep 18;23(11):1175-84 PubMed

Arch Pharm (Weinheim). 2003 Jun;336(3):155-8 PubMed

Eur J Neurosci. 2000 Sep;12(9):3265-75 PubMed

Brain Res Bull. 2001 Nov 15;56(5):495-507 PubMed

Biochem Pharmacol. 1967 Jun;16(6):963-70 PubMed

Psychopharmacologia. 1964 Sep 11;6(3):163-72 PubMed

Behav Pharmacol. 2005 Mar;16(2):127-30 PubMed

J Anal Toxicol. 1998 Sep;22(5):345-54 PubMed

Psychopharmacology (Berl). 1995 May;119(2):239-45 PubMed

Psychopharmacology (Berl). 1990;100(3):417-25 PubMed

Acute pharmacological profile of 2C-B-Fly-NBOMe in male Wistar rats-pharmacokinetics, effects on behaviour and thermoregulation

Psilocin, LSD, mescaline, and DOB all induce broadband desynchronization of EEG and disconnection in rats with robust translational validity

Psilocybin disrupts sensory and higher order cognitive processing but not pre-attentive cognitive processing-study on P300 and mismatch negativity in healthy volunteers

Mephedrone (4-Methylmethcathinone): Acute Behavioral Effects, Hyperthermic, and Pharmacokinetic Profile in Rats

Behavioral, neurochemical and pharmaco-EEG profiles of the psychedelic drug 4-bromo-2,5-dimethoxyphenethylamine (2C-B) in rats