SMART DRUGS aka NOOTROPICS
Nootropics, also referred to as smart drugs, memory enhancers, neuro enhancers, cognitive enhancers, and intelligence enhancers, are drugs, supplements, nutraceuticals, and functional foods that improve one or more aspects of mental function, such as working memory, motivation, and attention. The word nootropic was coined in 1972 by the Romanian Dr. Corneliu E. Giurgea, derived from the Greek words νους nous, or “mind,” and τρέπεινtrepein meaning to bend or turn. [Wikipedia]
In 1964, Romanian chemist and psychologist Corneliu E. Giurgea synthesized piracetam which is thought to be the first of a raft of “smart drugs” of this kind. 1n 1972, Giurgea coined the word nootropic to describe drugs that fulfill the following criteria:
Nootropics are said to have noticeable positive effects on a number of different aspects of brain function; for example, they are claimed to boost vital blood flow to the brain to enhance cognitive ability and memory, as well as overall intelligence. They are also said to up the capacity of individuals to concentrate, maintain attention span, and improve motivation especially when taken on a regular schedule over a long period of time.
Nutraceutical, a portmanteau of the words “nutrition” and “pharmaceutical”, was coined in 1989 by Stephen L. DeFelice, founder and chairman of the Foundation of Innovation Medicine. The term is applied to products that range from isolated nutrients, dietary supplements and herbal products, specific diets and processed foods such as cereals, soups, and beverages. [Wikipedia]
Nootropics, also referred to as smart drugs, memory enhancers, neuro enhancers, cognitive enhancers, and intelligence enhancers, are drugs, supplements, nutraceuticals, and functional foods that improve one or more aspects of mental function, such as working memory, motivation, and attention. The word nootropic was coined in 1972 by the Romanian Dr. Corneliu E. Giurgea, derived from the Greek words νους nous, or “mind,” and τρέπεινtrepein meaning to bend or turn. [Wikipedia]
In 1964, Romanian chemist and psychologist Corneliu E. Giurgea synthesized piracetam which is thought to be the first of a raft of “smart drugs” of this kind. 1n 1972, Giurgea coined the word nootropic to describe drugs that fulfill the following criteria:
- Nootropics should boost memory and learning ability.
- They should also strengthen the ability of learned forms of behavior as well as memories to withstand forces such as hypoxiation and electroshock treatment.
- They should afford protection to the brain from a variety of injuries, either chemical or physical (for example, due to the ingestion of scopolamine or barbiturates).
- Nootropics should make the controlling mechanisms of the cortex more effective.
- Unlike other kinds of psychotropic drugs, nootropic drugs should have no sedative or stimulant effects, as well as possessing negligible side effects.
- They should also have virtually no detectable toxicity.
Nootropics are said to have noticeable positive effects on a number of different aspects of brain function; for example, they are claimed to boost vital blood flow to the brain to enhance cognitive ability and memory, as well as overall intelligence. They are also said to up the capacity of individuals to concentrate, maintain attention span, and improve motivation especially when taken on a regular schedule over a long period of time.
Nutraceutical, a portmanteau of the words “nutrition” and “pharmaceutical”, was coined in 1989 by Stephen L. DeFelice, founder and chairman of the Foundation of Innovation Medicine. The term is applied to products that range from isolated nutrients, dietary supplements and herbal products, specific diets and processed foods such as cereals, soups, and beverages. [Wikipedia]
NEUROTRANSMITTERS
Neurotransmitters are endogenous chemicals that transmit signals across a synapse from one neuron (brain cell) to another ‘target’ neuron. Neurotransmitters are packaged into synaptic vesicles clustered beneath the membrane in the axon terminal, on the presynaptic side of a synapse. Neurotransmitters are released into and diffuse across the synaptic cleft, where they bind to specific receptors in the membrane on the postsynaptic side of the synapse. Many neurotransmitters are synthesized from plentiful and simple precursors, such as amino acids, which are readily available from the diet and which require only a small number of biosynthetic steps to convert.
Most neurotransmitters are about the size of a single amino acid, but some neurotransmitters may be the size of larger proteins or peptides. A neurotransmitter is available only briefly – before rapid deactivation – to bind to the postsynaptic receptors. Deactivation may occur due to: the removal of neurotransmitter by re-uptake into the presynaptic terminal; or degradative enzymes in the synaptic cleft. Nevertheless, short-term exposure of the receptor to neurotransmitter is typically sufficient for causing a postsynaptic response by way of synaptic transmission.
In response to a threshold action potential or graded electrical potential, a neurotransmitter is released at the presynaptic terminal. Low level “baseline” release also occurs without electrical stimulation. The released neurotransmitter may then move across the synapse to be detected by and bind with receptors in the postsynaptic neuron. Binding of neurotransmitters may influence the postsynaptic neuron in either an inhibitory or excitatory way. This neuron may be connected to many more neurons, and if the total of excitatory influences is greater than that of inhibitory influences, it will also “fire”. That is to say, it will create a new action potential at its axon hillock to release neurotransmitters and pass on the information to yet another neighboring neuron.
Anandamide (N-arachidonoylethanolamine or AEA) is an endogenous cannabinoid neurotransmitter. The name is taken from the Sanskrit word (and Hinduistic religious term) ananda, which means "joy, bliss, delight", and amide. [via Wikipedia]
Acetylcholine is an organic molecule that acts as a neurotransmitter in many organisms, including the autonomic nervous system (ANS), peripheral nervous system (PNS), central nervous system (CNS) and the motor division of the somatic nervous system. In cardiac tissue acetylcholine neurotransmission has an inhibitory effect, which lowers heart rate. However, acetylcholine also behaves as an excitatory neurotransmitter at neuromuscular junctions in skeletal muscle. [via Wikipedia]
Choline is a water-soluble essential nutrient and the precursor molecule for the neurotransmitter acetylcholine, which is involved in many functions including memory and muscle control. Choline must be consumed through the diet for the body to remain healthy. It is used in the synthesis of the constructional components in the body’s cell membranes. [via Wikipedia]
Dopamine (contracted from 3,4-dihydroxyphenethylamine) is a hormone and neurotransmitter of the catecholamine and phenethylamine families that plays a number of important roles in the human brain and body. The brain includes several distinct dopamine systems, one of which plays a major role in reward-motivated behavior; others systems are involved in motor control and in controlling the release of several other important hormones. Several important diseases of the nervous system are associated with dysfunctions of the dopamine system. Parkinson’s disease, a degenerative condition causing tremor and motor impairment, has been related to the loss of dopamine-secreting neurons in the midbrain area called the substantia nigra. There is evidence that schizophrenia involves highly altered levels of dopamine activity, and the antipsychotic drugs that are frequently used to treat it have a primary effect of attenuating dopamine activity. Attention deficit hyperactivity disorder (ADHD) and restless legs syndrome (RLS) are also believed to be associated with decreased dopamine activity. [via Wikipedia]
N,N-Dimethyltryptamine (DMT or N,N-DMT) is a psychedelic compound of the tryptamine family. When ingested, DMT is able to cross the human blood-brain-barrier, allowing it to act as a powerful hallucinogenic drug that dramatically affects human consciousness. Depending on the dose and method of administration, its subjective effects can range from short-lived, milder psychedelic states to powerful immersive experiences; these are often described as a total loss of connection to external reality and an experience of encountering indescribable spiritual/alien beings and realms. It is originally derived from the essential amino acid tryptophan and is structurally analogous to the neurotransmitter serotonin (5-HT) and the hormone melatonin, and furthermore functionally analogous to other psychedelic tryptamines, such as 5-MeO-DMT, bufotenin, psilocin, and psilocybin. [via Wikipedia]
GABA (Gamma Aminobutyric Acid or γ-Aminobutyric acid) is the chief inhibitory neurotransmitter in the mammalian central nervous system. It plays the principal role in reducing neuronal excitability throughout the nervous system. In humans, GABA is also directly responsible for the regulation of muscle tone. Although in chemical terms it is an amino acid, GABA is rarely referred to as such in the scientific or medical communities, because the term “amino acid,” used without a qualifier, by convention refers to the alpha amino acids, which GABA is not, nor is it considered to be incorporated into proteins. [via Wikipedia]
Monoamine neurotransmitters are neurotransmitters and neuromodulators derived from aromatic amino acids like phenylalanine, tyrosine, tryptophan, and the thyroid hormones by the action of aromatic amino acid decarboxylase enzymes. Monoaminergic systems are involved in the regulation of cognitive processes such as emotion, arousal, and certain types of memory. Drugs used to increase the effect of monoamine may be used to treat patients with psychiatric disorders, including depression, anxiety, and schizophrenia. [via Wikipedia]
Serotonin or 5-hydroxytryptamine (5-HT) is a monoamine neurotransmitter. Biochemically derived from tryptophan, serotonin is primarily found in the gastrointestinal tract, platelets, and the central nervous system (CNS) of animals, including humans. It is popularly thought to be a contributor to feelings of well-being and happiness. Approximately 90% of the human body’s total serotonin is located in the enterochromaffin cells in the GI tract, where it is used to regulate intestinal movements. The remainder is synthesized in serotonergic neurons of the CNS, where it regulates mood, appetite, and sleep. Serotonin also has some cognitive functions, including memory and learning. Modulation of serotonin at synapses is thought to be a major action of several classes of pharmacological antidepressants. [via Wikipedia]
Tryptamine is a monoamine alkaloid found in plants, fungi, and animals. It contains an indole ring structure, and is structurally similar to the amino acid tryptophan, from which it derives its name. Tryptamine is found in trace amounts in the brains of mammals and is believed to play a role as a neuromodulator or neurotransmitter. The tryptamine chemical structure is the backbone for a group of compounds termed collectively substituted tryptamines. This group includes many biologically active compounds, including neurotransmitters and psychedelic drugs. [Wikipedia]
Neurotransmitters are endogenous chemicals that transmit signals across a synapse from one neuron (brain cell) to another ‘target’ neuron. Neurotransmitters are packaged into synaptic vesicles clustered beneath the membrane in the axon terminal, on the presynaptic side of a synapse. Neurotransmitters are released into and diffuse across the synaptic cleft, where they bind to specific receptors in the membrane on the postsynaptic side of the synapse. Many neurotransmitters are synthesized from plentiful and simple precursors, such as amino acids, which are readily available from the diet and which require only a small number of biosynthetic steps to convert.
Most neurotransmitters are about the size of a single amino acid, but some neurotransmitters may be the size of larger proteins or peptides. A neurotransmitter is available only briefly – before rapid deactivation – to bind to the postsynaptic receptors. Deactivation may occur due to: the removal of neurotransmitter by re-uptake into the presynaptic terminal; or degradative enzymes in the synaptic cleft. Nevertheless, short-term exposure of the receptor to neurotransmitter is typically sufficient for causing a postsynaptic response by way of synaptic transmission.
In response to a threshold action potential or graded electrical potential, a neurotransmitter is released at the presynaptic terminal. Low level “baseline” release also occurs without electrical stimulation. The released neurotransmitter may then move across the synapse to be detected by and bind with receptors in the postsynaptic neuron. Binding of neurotransmitters may influence the postsynaptic neuron in either an inhibitory or excitatory way. This neuron may be connected to many more neurons, and if the total of excitatory influences is greater than that of inhibitory influences, it will also “fire”. That is to say, it will create a new action potential at its axon hillock to release neurotransmitters and pass on the information to yet another neighboring neuron.
Anandamide (N-arachidonoylethanolamine or AEA) is an endogenous cannabinoid neurotransmitter. The name is taken from the Sanskrit word (and Hinduistic religious term) ananda, which means "joy, bliss, delight", and amide. [via Wikipedia]
Acetylcholine is an organic molecule that acts as a neurotransmitter in many organisms, including the autonomic nervous system (ANS), peripheral nervous system (PNS), central nervous system (CNS) and the motor division of the somatic nervous system. In cardiac tissue acetylcholine neurotransmission has an inhibitory effect, which lowers heart rate. However, acetylcholine also behaves as an excitatory neurotransmitter at neuromuscular junctions in skeletal muscle. [via Wikipedia]
Choline is a water-soluble essential nutrient and the precursor molecule for the neurotransmitter acetylcholine, which is involved in many functions including memory and muscle control. Choline must be consumed through the diet for the body to remain healthy. It is used in the synthesis of the constructional components in the body’s cell membranes. [via Wikipedia]
Dopamine (contracted from 3,4-dihydroxyphenethylamine) is a hormone and neurotransmitter of the catecholamine and phenethylamine families that plays a number of important roles in the human brain and body. The brain includes several distinct dopamine systems, one of which plays a major role in reward-motivated behavior; others systems are involved in motor control and in controlling the release of several other important hormones. Several important diseases of the nervous system are associated with dysfunctions of the dopamine system. Parkinson’s disease, a degenerative condition causing tremor and motor impairment, has been related to the loss of dopamine-secreting neurons in the midbrain area called the substantia nigra. There is evidence that schizophrenia involves highly altered levels of dopamine activity, and the antipsychotic drugs that are frequently used to treat it have a primary effect of attenuating dopamine activity. Attention deficit hyperactivity disorder (ADHD) and restless legs syndrome (RLS) are also believed to be associated with decreased dopamine activity. [via Wikipedia]
N,N-Dimethyltryptamine (DMT or N,N-DMT) is a psychedelic compound of the tryptamine family. When ingested, DMT is able to cross the human blood-brain-barrier, allowing it to act as a powerful hallucinogenic drug that dramatically affects human consciousness. Depending on the dose and method of administration, its subjective effects can range from short-lived, milder psychedelic states to powerful immersive experiences; these are often described as a total loss of connection to external reality and an experience of encountering indescribable spiritual/alien beings and realms. It is originally derived from the essential amino acid tryptophan and is structurally analogous to the neurotransmitter serotonin (5-HT) and the hormone melatonin, and furthermore functionally analogous to other psychedelic tryptamines, such as 5-MeO-DMT, bufotenin, psilocin, and psilocybin. [via Wikipedia]
GABA (Gamma Aminobutyric Acid or γ-Aminobutyric acid) is the chief inhibitory neurotransmitter in the mammalian central nervous system. It plays the principal role in reducing neuronal excitability throughout the nervous system. In humans, GABA is also directly responsible for the regulation of muscle tone. Although in chemical terms it is an amino acid, GABA is rarely referred to as such in the scientific or medical communities, because the term “amino acid,” used without a qualifier, by convention refers to the alpha amino acids, which GABA is not, nor is it considered to be incorporated into proteins. [via Wikipedia]
Monoamine neurotransmitters are neurotransmitters and neuromodulators derived from aromatic amino acids like phenylalanine, tyrosine, tryptophan, and the thyroid hormones by the action of aromatic amino acid decarboxylase enzymes. Monoaminergic systems are involved in the regulation of cognitive processes such as emotion, arousal, and certain types of memory. Drugs used to increase the effect of monoamine may be used to treat patients with psychiatric disorders, including depression, anxiety, and schizophrenia. [via Wikipedia]
Serotonin or 5-hydroxytryptamine (5-HT) is a monoamine neurotransmitter. Biochemically derived from tryptophan, serotonin is primarily found in the gastrointestinal tract, platelets, and the central nervous system (CNS) of animals, including humans. It is popularly thought to be a contributor to feelings of well-being and happiness. Approximately 90% of the human body’s total serotonin is located in the enterochromaffin cells in the GI tract, where it is used to regulate intestinal movements. The remainder is synthesized in serotonergic neurons of the CNS, where it regulates mood, appetite, and sleep. Serotonin also has some cognitive functions, including memory and learning. Modulation of serotonin at synapses is thought to be a major action of several classes of pharmacological antidepressants. [via Wikipedia]
Tryptamine is a monoamine alkaloid found in plants, fungi, and animals. It contains an indole ring structure, and is structurally similar to the amino acid tryptophan, from which it derives its name. Tryptamine is found in trace amounts in the brains of mammals and is believed to play a role as a neuromodulator or neurotransmitter. The tryptamine chemical structure is the backbone for a group of compounds termed collectively substituted tryptamines. This group includes many biologically active compounds, including neurotransmitters and psychedelic drugs. [Wikipedia]
OTHER TERMS
Bioavailability (BA) is a subcategory of absorption and is the fraction of an administered dose of unchanged drug that reaches the systemic circulation, one of the principal pharmacokinetic properties of drugs. By definition, when a medication is administered intravenously, its bioavailability is 100%. However, when a medication is administered via other routes (such as orally), its bioavailability generally decreases (due to incomplete absorption and first-pass metabolism) or may vary from patient to patient. Bioavailability is one of the essential tools in pharmacokinetics, as bioavailability must be considered when calculating dosages for non-intravenous routes of administration. [via Wikipedia]
The blood–brain barrier (BBB) is a highly selective permeability barrier that separates the circulating blood from the brain extracellular fluid (BECF) in the central nervous system (CNS). The blood–brain barrier allows the passage of water, some gases, and lipid soluble molecules by passive diffusion, as well as the selective transport of molecules such as glucose and amino acids that are crucial to neural function while preventing the entry of potential neurotoxins. [via Wikipedia]
Bioavailability (BA) is a subcategory of absorption and is the fraction of an administered dose of unchanged drug that reaches the systemic circulation, one of the principal pharmacokinetic properties of drugs. By definition, when a medication is administered intravenously, its bioavailability is 100%. However, when a medication is administered via other routes (such as orally), its bioavailability generally decreases (due to incomplete absorption and first-pass metabolism) or may vary from patient to patient. Bioavailability is one of the essential tools in pharmacokinetics, as bioavailability must be considered when calculating dosages for non-intravenous routes of administration. [via Wikipedia]
The blood–brain barrier (BBB) is a highly selective permeability barrier that separates the circulating blood from the brain extracellular fluid (BECF) in the central nervous system (CNS). The blood–brain barrier allows the passage of water, some gases, and lipid soluble molecules by passive diffusion, as well as the selective transport of molecules such as glucose and amino acids that are crucial to neural function while preventing the entry of potential neurotoxins. [via Wikipedia]