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All 2 posts Subject: MDMA-Like Stimulus Effects of a-Ethyltryptamine... Please login to post Down

thallium
(Hive Bee)
05-07-04 13:39
No 505583
User Picture       MDMA-Like Stimulus Effects of a-Ethyltryptamine...
(Rated as: excellent)

MDMA-Like Stimulus Effects of alpha-Ethyltryptamine and the alpha-Ethyl Homolog of DOM
Glennon, R.A.
PHARMACOL BIOCHEM BEHAV 46(2) 459-462, 1993.

Abstract:

One-carbon homologation of phenylalkylamine or indolylalkylamine hallucinogens containing an alpha-methyl substituent typically results in a reduction of hallucinogenic potency ; however, this same structural change has little to no effect on agents that produce MDMA-like effects . In the present investigation, rats trained to discriminate 1 .5 mg/kg of MDMA (3,4-methylenedioxymethamphetamine) from saline vehicle were employed to determine if the alpha-ethyl homologs of the hallucinogens 1-(2,5-dimethoxy-4-methylphenyl)-2-aminopropane (DOM) and alpha-methyltryptamine (alpha-MeT) - that is, alpha-EH DOM (BL-3912) and alpha-EtT, respectively - would produce stimulus effects similar to those of MDMA. Although the MDMA stimulus failed to generalize to DOM (previously published) and alpha-MeT (this study), MDMA stimulus generalization occurred both to alpha-EH DOM (ED₅₀ = 1.3 mg/kg) and alpha-EtT (ED₅₀ = 3.5 mg/kg). A(+)amphetamine stimulus (training dose = 1.0 mg/kg) only partially generalized to these two agents, suggesting that the MDMA stimulus generalization involves more than a simple amphetamine-like action. As such, this is the first demonstration that classical hallucinogens can produce MDMA-like effects upon homologation and that MDMA-like stimulus effects can be associated with an indolylalkylamine. Furthermore, these results continue to support the concept that an intact methylenedioxy ring system, such as that found in MDMA and other MDMA-related agents, is not a structural requirement for drugs to produce MDMA-like effects.

(Sorry if this has been posted before, I couldn't find it in TFSE.)

Video meliora, proboque; Deteriora sequor. -Ovid

thallium
(Hive Bee)
08-30-04 21:13
No 528312
User Picture       More on Ariadne...
(Rated as: excellent)

Effects of the Phenethylamine Derivates, BL-3912, Fenfluramine, and Sch-12679, in Rats Trained with LSD as a Discriminative Stimulus
J. C. Winter
Psychopharmacology 68, 159-162 (1980)

Abstract:

Six rats were trained to discriminate the effects of LSD (100µg/kg) and saline in a two-lever choice task. They were then tested with each of three phenethylamine derivates, BL-3912 (2,5-dimethoxy-4-methyl-alpha-ethyl-phenethylamine), fenfluramine (N-ethyl-alpha-methyl-m-(trifluoro-methyl)phenetylamine, and Sch-12679 (N-methyl-1-phenyl-7,8-dimethoxy-2,3,4,5-tetra-hydro-3-benzazepine maleate). Fenfluramine and Sch-12679 yielded intermediate results, i.e., responding was not fully appropriate for either training condititon while BL-3912 substituted completely for LSD. The LSD-like effects of each of the drugs were antagonized by pretreatment with BC-105, a serotonergic antagonist known to block the stimulus effects of indole and phenetylamine hallucinogens. The present data together with concideration of the known clinical effects of BL-3912, fenfluramine, and Sch-12679 are consistent with the following conclusions: (1) a variety of drugs may substitute in whole or in part for LSD in LSD-trained rats, and (2) even complete substitution of a drug for LSD in the rat is not necessarilly associated with the production by that drug of hallucinations in man.

Video meliora, proboque; Deteriora sequor. -Ovid

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	All 2 posts		Subject: MDMA-Like Stimulus Effects of a-Ethyltryptamine...		Please login to post		Down


		thallium (Hive Bee) 05-07-04 13:39 No 505583				MDMA-Like Stimulus Effects of a-Ethyltryptamine... (Rated as: excellent)
						*MDMA-Like Stimulus Effects of alpha-Ethyltryptamine and the alpha-Ethyl Homolog of DOM* Glennon, R.A. PHARMACOL BIOCHEM BEHAV 46(2) 459-462, 1993. Abstract: One-carbon homologation of phenylalkylamine or indolylalkylamine hallucinogens containing an alpha-methyl substituent typically results in a reduction of hallucinogenic potency ; however, this same structural change has little to no effect on agents that produce MDMA-like effects . In the present investigation, rats trained to discriminate 1 .5 mg/kg of MDMA (3,4-methylenedioxymethamphetamine) from saline vehicle were employed to determine if the alpha-ethyl homologs of the hallucinogens 1-(2,5-dimethoxy-4-methylphenyl)-2-aminopropane (DOM) and alpha-methyltryptamine (alpha-MeT) - that is, alpha-EH DOM (BL-3912) and alpha-EtT, respectively - would produce stimulus effects similar to those of MDMA. Although the MDMA stimulus failed to generalize to DOM (previously published) and alpha-MeT (this study), MDMA stimulus generalization occurred both to alpha-EH DOM (ED₅₀ = 1.3 mg/kg) and alpha-EtT (ED₅₀ = 3.5 mg/kg). A(+)amphetamine stimulus (training dose = 1.0 mg/kg) only partially generalized to these two agents, suggesting that the MDMA stimulus generalization involves more than a simple amphetamine-like action. As such, this is the first demonstration that classical hallucinogens can produce MDMA-like effects upon homologation and that MDMA-like stimulus effects can be associated with an indolylalkylamine. Furthermore, these results continue to support the concept that an intact methylenedioxy ring system, such as that found in MDMA and other MDMA-related agents, is not a structural requirement for drugs to produce MDMA-like effects. (Sorry if this has been posted before, I couldn't find it in TFSE.) Video meliora, proboque; Deteriora sequor. -Ovid



		thallium (Hive Bee) 08-30-04 21:13 No 528312				More on Ariadne... (Rated as: excellent)
						Effects of the Phenethylamine Derivates, BL-3912, Fenfluramine, and Sch-12679, in Rats Trained with LSD as a Discriminative Stimulus J. C. Winter Psychopharmacology 68, 159-162 (1980) Abstract: Six rats were trained to discriminate the effects of LSD (100µg/kg) and saline in a two-lever choice task. They were then tested with each of three phenethylamine derivates, BL-3912 (2,5-dimethoxy-4-methyl-alpha-ethyl-phenethylamine), fenfluramine (N-ethyl-alpha-methyl-m-(trifluoro-methyl)phenetylamine, and Sch-12679 (N-methyl-1-phenyl-7,8-dimethoxy-2,3,4,5-tetra-hydro-3-benzazepine maleate). Fenfluramine and Sch-12679 yielded intermediate results, i.e., responding was not fully appropriate for either training condititon while BL-3912 substituted completely for LSD. The LSD-like effects of each of the drugs were antagonized by pretreatment with BC-105, a serotonergic antagonist known to block the stimulus effects of indole and phenetylamine hallucinogens. The present data together with concideration of the known clinical effects of BL-3912, fenfluramine, and Sch-12679 are consistent with the following conclusions: (1) a variety of drugs may substitute in whole or in part for LSD in LSD-trained rats, and (2) even complete substitution of a drug for LSD in the rat is not necessarilly associated with the production by that drug of hallucinations in man. Video meliora, proboque; Deteriora sequor. -Ovid

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