Description INDUCTION OF A NOVEL STATE OF MIND WITH A 5-HT2A
AGONIST AND A NMDA ANTAGONIST
Technical Field
[1] This invention concerns the human mind and ways to modify it.
Background Art
[2] The uniqueness of the human mind parts man from all other species. It is our mind that makes us human. The human mind is a miracle created by evolution, and the species Homo sapiens seems to mark the pinnacle of the evolution of species. It does not seem possible that a new species will evolve with a mind superior to the human mind. When the evolution of species had created Homo sapiens as its ultimate product, the evolution of mankind began. The uniqueness of the human mind enabled a continuous and collective process of learning, discovery and invention, which created the modern world that surrounds us.
[3] In spite of intense research, it is still a mystery how the substance matter of the human brain becomes conscious and emanates the human mind. However, scientific research has created much knowledge about the functioning of the human brain, and this knowledge enables us today to manipulate the human mind with pharmacological tools which affect the functioning of the substance matter of the brain. Such pharmacological tools, when administered to humans, are called drugs.
[4] Society, science and the law distinguish between legitimate and illegitimate uses of drugs which influence the human mind, based on the benefit their use creates for the individual and society.
[5] Currently, the only generally accepted and legitimate reason for the pharmacological manipulation of the functioning of the human brain is for the purpose to correct malfunctions. Such malfunctions of the human brain affect the mind and cause mental diseases and disorders. The treatment of such diseases and disorders is highly desirable and beneficial for the individual as well as for society. Much effort is undertaken to develop new drugs for this purpose.
[6] However, humans also seek the effects of mind altering drugs for reasons which are generally considered illegitimate. Such drugs have an effect on the human mind which the individual subjectively experiences as desirable. Objectively, however, these drugs are detrimental for the individual, because they impair the mind. Such drugs of abuse create immense problems for society and much suffering for mankind. Much effort is undertaken to prohibit and prevent such use of mind altering drugs, but the success of these efforts is unfortunately very limited.
[7] The Applicant believes that there is an additional legitimate reason to manipulate the human brain with pharmacological tools. It is for the purpose of enhancing the human mind. Such an effect would be perceived as desirable by many individuals. Since such an effect would objectively not be detrimental for the individual, but might actually be beneficial for the individual, it would also be acceptable for society.
[8] It seems to be the general consensus in science that the healthy human mind can not be further enhanced significantly by pharmacological manipulation of the brain. Indeed, there is currently no method known in the art to pharmacologically manipulate the healthy human mind in an objectively beneficial or useful way. Research to find ways to enhance the human mind with pharmacological tools is practically nonexistent.
[9] It should be noted however that non-pharmacological methods to enhance the mind have a long tradition in human history. Mental and physical exercises such as meditation and yoga were developed as ways to enhance the mind and are widely practiced. It is therefore a clear and legitimate desire of man to enhance his mind. Disclosure of Invention
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Best Mode
[41] Relatively small, sub-anesthetic doses of the NMDA antagonist are sufficient.
Generally, the doses are in the same range at which NMDA antagonists have shown neuroprotective properties and were explored in clinical trials for conditions such as stroke and traumatic brain injury. They are also in the same range in which the NMDA antagonist ketamine is used for therapeutic purposes.
[42] Research published in Anesthesiology 88(l):82-8, 1998 (PMID: 9447860) has shown that the relationship between the psychotomimetic effects of the NMDA antagonist ketamine and its steady-state venous plasma concentrations is highly linear. The Applicant has found that the most suitable and desirable dose of the NMDA antagonist is the threshold dose, or somewhat below the threshold dose, for the induction of psychotomimetic effects. The threshold dose is that dose at which the subject experiences the first psychotomimetic mental alterations caused by an NMDA antagonist, but they are mild and not troublesome. While higher doses, which cause more pronounced psychotomimetic effects, might still be useful in certain cases, they are generally considered less desirable and less suitable for the induction of the disclosed effect.
[43] The dose of the 5-HT2A agonist may be varied depending on the individual's response and the desired effect. While lower doses might be sufficient and more desirable in many cases, even high doses of the 5-HT2A agonist, which when administered alone would have a very strong hallucinogenic effect, can be used without causing hallucinations or psychosis.
[44] Thus, while the Applicant has generally worked in his research with the threshold dose of the NMDA antagonist and a clearly hallucinogenic dose of a 5-HT2A agonist to cause a pronounced effect on the mind, smaller doses of the two drugs which cause a less pronounced, more subtle effect on the mind may be quite sufficient and more desirable for many practical and therapeutic applications of the disclosed effect.
[45] The NMDA antagonist and the 5-HT2A agonist may be administered either simultaneously, or the drugs may be administered sequentially in such a way that their tissue concentrations and pharmacological effects develop uniformly and synchronously. While it is most desirable that the agonistic activity at the 5-HT2A receptor and the antagonistic activity at the NMDA receptor develop uniformly and synchronously, it may in certain cases be advantageous to cause either the 5-HT2A agonistic or NMDA antagonistic effect first, and then cause the other effect thereafter.
[46] The NMDA antagonist and the 5-HT2A agonist may be administered in any form which is physiologically compatible. The method of administration may be freely chosen from the many methods known in the art to administer a drug to a human being.
[47] While there is currently no compound know in the art which combines 5-HT2A agonistic activity and NMDA antagonistic activity in one molecule, it is contemplated that such a compound may be developed in the future. Thus, a combination of a 5-HT2A agonist and a NMDA antagonist may either be in the form of two compounds, or in the form of one compound which has both 5-HT2A agonistic and NMDA antagonistic activity. Any composition of matter which concurrently has agonistic activity at the 5-HT2A receptor and antagonistic activity at the NMDA receptor is therefore also considered as a combination of a 5-HT2A agonist and a NMDA antagonist.
[48] It should be noted that the combination of a 5-HT2A agonist and a NMDA antagonist might be usefully combined with various other drugs for the treatment of certain patients, certain diseases, disorders and conditions, or to achieve certain additional effects. Future research will certainly discover many new and useful combinations.
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