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 Neurotransmission and Obesity Research

Obesity Research
 

Neuropeptides, growth hormones, and biogenic amines can contribute to obesity and its treatment in certain individuals. Neuropeptide Y (NPY), a neuronal signaling peptide that selectively binds to Y1 and Y5 neuropeptide Y receptors in the hypothalamus, induces orexigenic signals, thereby increasing food intake and decreasing energy expenditure. Ghrelin acts as an appetite-stimulating hormone and is implicated in both short- and long-term appetite and body weight regulation. Amphetamines such as ephedrine, phentermine, and mazindol were quickly shown to display food intake and appetite suppressing qualities. However many of these drugs were abandoned as treatment for obesity due to their strong stimulant properties. Other drugs such as fenfluramine and dexfenfluramine were later created. Both had a similar structure to the earlier amphetamines but demonstrated no stimulant activity. However, patients using either or a combination of both fenfluramine and dexfenfluramine developed valvular disease.

Other anti-obesity therapies have also proven unsuccessful. Serotonin reuptake inhibitors such as fluoxetine, fluvoxamine, and setraline produce weight loss but significant weight regain is shown despite continued use of the drugs. Norephedrine has been removed from weight loss drugs due to its risk of hemorrhagic stroke and ephedrine has been removed as an over-the-counter drug due to its undesirable side effects. The development of thermogenic drugs, which increase metabolic rates safely without increasing heart rate or blood pressure, has proven difficult. But the development of b3-adrenoceptor or 5-HT2C serotonin receptor agonists as anti-obesity treatments still holds promise.



Neuropeptide Y and Peptide YY Products
Galanins
Growth Hormone Releasing Factors
Tachykinins
Adrenergics
Biogenic Amine Transport Inhibitors
Serotonergics
GABAergic
Stimulants

Neuropeptide Y and Peptide YY Products

Vasoconstrictor; brain peptide that inhibits Ca2+-activated K+ channels in vascular smooth muscle; implicated in the control of blood pressure, sexual behavior and food intake; inhibits cholecystokinin- and secretin-stimulated pancreatic secretion.

Neuropeptide Y and Peptide YY Products
Product #  Product Name Notes Add to Cart
N5017 Neuropeptide Y human (hNPY; NPY)  
N3266 Neuropeptide Y porcine (NPY)  
N6269 Neuropeptide Y sheep (NPY)  
N9398 N-Acetyl-[Leu28,Leu31]-Neuropeptide Y, Fragment 24-36 Selective Y2 neuropeptide Y receptor agonist.
N6146 [Leu31,Pro34]-Neuropeptide Y human Selective Y1 and Y5 neuropeptide Y receptor agonist.
N7768 [Leu31,Pro34]-Neuropeptide Y porcine Selective Y1 and Y5 neuropeptide Y receptor agonist.
N8154 [Ala31α-Aminoisobutyryl32]-Neuropeptide Y, porcine ([Ala31, Aib32]-NPY Porcine) Y5 Neuropeptide Y receptor agonist; exhibits high affinity and selectivity.
N8404 Neuropeptide Y Fragment 19-23-[Gly1, Ser3, Gln4, Thr6, Ala31, α-Aminoisobutyryl-α-methyl-Ala32, Gln34]-Pancreatic Polypeptide human Highly selective Y5 neuropeptide Y receptor agonist.
N9407 Neuropeptide Y Fragment 3-36 human, rat, (NPY 3-36) Endogenous neuropeptide; selectively binds to Y2 and Y5 neuropeptide Y receptors.
N6521 Neuropeptide Y Fragment 13-36 porcine, (NPY 13-36) Selective Y2 neuropeptide Y receptor agonist.
N9409 Neuropeptide Y Fragment 22-36 (Ser-Ala-Leu- Arg-His-Tyr-Ile-Asn-Leu-Ile-Thr-Arg-Gln-Arg-Tyr-NH2) NPY fragment; acts as potent inhibitor of calmodulin-stimulated phosphodiesterase.
P9778 Pancreatic Polypeptide bovine Y4 Neuropeptide Y receptor agonist.
P4488 Pancreatic Polypeptide Fragment 1-17, [Ala31,α-Aminoisobutyryl32]-Neuropeptide Y Fragment 18-36 Neuropeptide Y receptor agonist.
P4363 Pancreatic Polypeptide Rana tempraria 36 amino acid peptide regulating food intake, circadian rhythms, mood, blood pressure, intestinal secretion and gut mobility.
P1306 Peptide YY human Gut hormone; inhibits both secretin and cholecystokinin-stimulated pancreatic secretion; endogenous nonselective NPY receptor agonist.
P5801 Peptide YY porcine (PYY) Gut hormone; inhibits both secretin and cholecystokinin-stimulated pancreatic secretion; endogenous nonselective NPY receptor agonist.
P220 Peptide YY Fragment 3-36 human Y2/Y5 neuropeptide Y receptor agonist.
P3365 Peptide YY Fragment 13-36 human trifluoroacetate salt Analog that mimics peptide YY (PYY) effects.
P6613 Peptide YY Fragment 13-36 porcine, rat Supresses the noradrenaline release from sympathetic nerve endings and competes with NPY for binding sites in rat brain.
P4107 [Leu31,Pro34]-Peptide YY Y1,Y4, and Y5 neuropeptide Y receptor agonist.
P3982 [Pro34]-Peptide YY NPY agonist with a preference for the Y1 and Y5 subtypes.
N8648 Neuropeptide Y Antagonist (1229U91) High affinity and selective Y1 neuropeptide Y receptor antagonist.
B174 BIBP 3226 Selective non-peptide Y1 neuropeptide Y receptor antagonist.
G8165 Galanin (1-13)-Neuropeptide Y (25-36) amide, (m32) Chimeric peptide that is a high affinity galanin receptor antagonist; this peptide is also recognized by neuropeptide Y receptors and is a Y2 neuropeptide Y agonist in rat vas deferens.
Neuropeptide Y Antibody
Product #  Product Name Species Reactivity Immunogen Application Add to Cart
N9528 Anti-Neuropeptide Y (NPY), Rabbit whole antiserum Rat, pig Synthetic porcine NPY Immunochemistry, Radioimmunoassay, Dot Blot

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Galanins

Galanin is co-localized with acetylcholine and inhibits its release; inhibits the release of glutamic acid, decreases excitability of spinal neurons; blocks voltage-activated Ca2+ channels; linked to behavioral and cognitive deficits in Alzheimer's disease.

Product #  Product Name Notes Add to Cart
G0278 Galanin human  
G5773 Galanin porcine  
G8272 Galanin rat  
G112 Galanin Fragment 1-16, porcine, rat Neuropeptide that inhibits the release of acetylcholine, dopamine, norepinephrine and other neurotransmitters.
G8916 [2-Aminobenzoyl-Gly1]-Galanin fragment, (1-10)-Lys(retro-m-Nitro-Tyr) amide, human, trifluoroacetate salt Substrate for a galanin degrading zinc-metallopeptidase from bovine spinal cord.
G9166 [D-Trp2]-Galanin fragment 1-29 human Exhibits high affinity for the GALR2 galanin receptor.
G9041 Galanin Fragment (1-13)-Bradykinin Fragment, (2-9) Amide trifluoroacetate salt Antagonist for galanin having a high specificity and affinity to the binding sites
G8041 Galanin-Like Peptide Fragment 1-60 porcine, trifluoroacetate salt Endogenous ligand that preferentially binds to the GALR2 galanin receptor.
G5024 Big Gastrin I human (Gregory Structure) Storage form of gastrin that also has biological activity.
G9020 Gastrin I human (Gastrin I, heptadecapeptide) Produced in the stomach; stimulates gastric acid secretion.
G1276 Gastrin I rat Produced in the stomach; stimulates gastric acid secretion.
G9145 [Leu15]-Gastrin I human ([Leucine15]-Gastrin I, heptadecapeptide; [Leucine15]-Little gastrin; [Leu15]-HG-17; LHG-17 Gastrin I analog with full biological activity and improved stability in aqueous solutions. Leu15 replaces Met15, which is readily oxidized resulting in loss of biological activity.
G0267 Mini Gastrin I human (HG-13) CCKB/gastrin receptor agonist. Corresponds to fragment 5-17 of human gastrin I. This form of gastrin has been isolated from tumor tissue.

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Growth Hormone Releasing Factors

Hypothalamic peptide that stimulates release of somatotropin from anterior pituitary.

Product #  Product Name Notes Add to Cart
G0644 Growth Hormone Releasing Factor bovine (GRF)  
G8895 Growth Hormone Releasing Factor human (GRF)  
G0769 Growth Hormone Releasing Factor porcine (GRF)  
G6646 Growth Hormone Releasing Factor rat (GRF)  
G6771 Growth Hormone Releasing Factor Fragment, 1-29 amide human Amidated GRF fragment that is equipotent to GRF in releasing somatotropin from anterior pituitary.
G4535 [D-Lys3]-GHRP-6 ([D-Lys3]-Growth Hormone Releasing Peptide 6 GHRP-6 antagonist.
G8903 Ghrelin rat Endogenous ligand to the orphan growth-hormone secretagogue receptor that stimulates the release of growth hormone from the pituitary.
G3902 Ghrelin human Endogenous ligand to the orphan growth-hormone secretagogue receptor that stimulates the release of growth hormone from the pituitary.

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Tachykinins


Product #  Product Name Notes Add to Cart
S6883 Substance P acetate salt hydrate NK1 tachykinin receptor agonist; potent vasodilator and hypotensive agent; induces salivation; increases capillary permeability; induces mast cell degranulation; putative neurotransmitter in sensory (pain) afferents.
S3144 [D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P (Antagonist D) NK1 tachykinin receptor antagonist
S0274 [D-Arg1,D-Trp7,9,Leu11]-Substance P acetate salt (Spantide I) Potent NK1 tachykinin receptor antagonist.
S6636 [Sar9]-Substance P NK1 tachykinin receptor agonist.
S3672 [Sar9,Met(O2)11]-Substance P Highly selective NK1 tachykinin receptor agonist.
S2275 Acetyl-[Arg6,Sar9,Met(O2)11]-Substance P, Fragment 6-11 Selective NK1 tachykinin receptor agonist.
S2314 δ-Aminovaleryl-[Pro9,Leu(N-Me)10]-Substance P, Fragment 7-11 Selective NK1 tachykinin receptor agonist.

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Adrenergics


Product #  Product Name Notes Add to Cart
B169 BRL 37344 sodium salt (BRL 37344A) Selective β3-adrenoceptor agonist.
C125 (±)-CGP-12177 hydrochloride Full agonist at β1/2-adrenoceptors and partial agonist at β3-adrenoceptors receptors.
C5976 CL 316,243 β3-Adrenoceptor agonist; anti-obesity agent. Sold with the exclusive permission of Wyeth-Ayerst Pharmaceticals.
A7257 (–)-Norepinephrine Adrenergic neurotransmitter.
S8688 SR 59230A oxalate salt β3-Adrenoceptor antagonist.

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Biogenic Amine Transport Inhibitors

Effects of Biogenic Amines on Food Intake and Obesity


Product #  Product Name Notes Add to Cart
A164 Alaprocate hydrochloride Potent and selective serotonin uptake inhibitor.
A8404 Amitriptyline hydrochloride Tricyclic antidepressant; inhibits the norepinephrine and serotonin transporters; high in vitro affinity for α1-adrenoceptors, serotonin and muscarinic acetylcholine receptors.
A129 Amoxapine Tricyclic antidepressant; inhibits uptake of norepinephrine; inhibits 5-HT2 serotonin receptors.
B102 Bupropion Inhibits the dopamine and norepinephrine transporters; does not inhibit the serotonin transporter; antidepressant.
C7861 Citalopram hydrobromide Potent and selective serotonin reuptake inhibitor; antidepressant.
C7291 Clomipramine hydrochloride Tricyclic antidepressant; inhibits serotonin and norepinephrine transporters.
D3900 Desipramine hydrochloride Tricyclic antidepressant that is a more potent inhibitor of norepinephrine reuptake than of serotonin reuptake.
D4526 Doxepin hydrochloride Tricyclic antidepressant that is a more potent inhibitor of norepinephrine uptake than of serotonin reuptake; antagonist at H1 histamine, muscarinic cholingergic and α-adrenergic receptors.
F132 Fluoxetine hydrochloride Selective serotonin reuptake inhibitor; antidepressant.
F1553 S(+)-Fluoxetine hydrochloride Selective serotonin reuptake inhibitor.
F1678 R(–)-Fluoxetine hydrochloride Selective serotonin reuptake inhibitor.
F133 Norfluoxetine hydrochloride Fluoxetine metabolite; more potent inhibitor of serotonin reuptake than fluoxetine with half-life in vivo of 5-7 days.
F2802 Fluvoxamine maleate Selective serotonin reuptake inhibitor; antidepressant.
G9659 GBR 12935 dihydrochloride Inhibits the dopamine and norepinephrine transporters; does not inhibit the serotonin transporter; binds to a nondopaminergic piperazine site in blood platelets and brain that has been identified as cytochrome P450.
I7379 Imipramine hydrochloride Tricyclic antidepressant; inhibits the serotonin and norepinephrine transporters; has little effect on the dopamine transporter.
I119 Indatraline hydrochloride (Lu 19-005) Potent dopamine, norepinephrine and serotonin reuptake inhibitor.
M9651 Maprotiline hydrochloride Selective norepinephrine reuptake inhibitor.
M2017 Mazindol Anorectic agent; dopamine, norepinephrine and serotonin reuptake inhibitor.
M0443 Mirtazapine Noradrenergic and specific serotonergic antidepressant; antagonizes selective adrenergic and serotonergic receptors so that both NE release and 5-HT1A mediated serotonergic signaling are increased.
N5536 Nefazodone hydrochloride Novel antidepressant; mixed 5-HT2A serotonin receptor antagonist/serotonin reuptake inhibitor.
N151 Nisoxetine hydrochloride Potent and selective norepinephrine reuptake inhibitor.
Q109 6-Nitroquipazine maleate Potent and selective serotonin reuptake inhibitor.
N7261 Nortriptyline hydrochloride Tricyclic antidepressant that is a more potent inhibitor of norepinephrine reuptake than of serotonin reuptake; 5-HT2 serotonin receptor antagonist.
P8813 Protriptyline hydrochloride Norepinephrine reuptake inhibitor.
R6527 Reboxetine mesylate Selective norepinephrine reuptake inhibitor.
T1692 Tianeptine sodium-potassium salt Tricyclic antidepressant; enhances serotonin uptake.
T7947 (R)-Tomoxetine hydrochloride Norepinephrine reuptake inhibitor.
T6154 Trazodone hydrochloride Antidepressant that potentiates the activity of serotonin reuptake inhibitors and has full 5-HT2C serotonin receptor agonist activity; metabolized to the 5-HT1 serotonin agonist 1-(3-Chlorophenyl) piperazine.
T3146 Trimipramine maleate Antidepressant; serotonin and norepinephrine reuptake inhibitor.
Z101 Zimelidine dihydrochloride Serotonin reuptake inhibitor.

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Serotonergics


Product #  Product Name Notes Add to Cart
C5554 1-(3-Chlorophenyl)piperazine hydrochloride (m-CPP) 5-HT2c serotonin receptor agonist; metabolite of trazodone.
C238 S(–)-Cyanopindolol hemifumarate salt 5-HT1A serotonin receptor antagonist; β3-adrenoceptor antagonist.
D7412 (±)-2,5-Dimethoxy-4-bromoamphetamine hydrobromide ((±)-DOB hydrobromide) Hallucinogenic; 5-HT2 serotonin receptor agonist.
D101 (±)-DOI hydrochloride ((±)-1-(2,5-Dimethoxy-4-iodophenyl)- 2-aminopropane hydrochloride) Potent and selective 5-HT2 serotonin receptor agonist that crosses the blood-brain barrier.
D153 R(–)-DOI hydrochloride (–)-1-(2,5-Dimethoxy-4-iodophenyl)-2-aminopropane hydrochloride Potent and selective 5-HT2 serotonin receptor agonist that crosses the blood-brain barrier; more potent enantiomer of (±)-DOI hydrochloride (D101).
S006 Ketanserin tartrate salt (R 41468 tartrate salt) Selective 5-HT2 serotonin receptor antagonist.
L107 LY-53,857 maleate salt Potent and selective 5-HT2 serotonin receptor antagonist. Manufactured and sold with the permission of Eli Lilly and Company.
M110 α-Methylserotonin maleate salt (α-Methyl-5-hydroxytryptamine maleate salt) 5-HT2 serotonin receptor agonist.
S003 1-(1-Naphthyl)piperazine hydrochloride 5-HT1 serotonin receptor agonist; 5-HT2 serotonin receptor antagonist.
P126 Pirenperone (R-47,465) 5-HT2 serotonin receptor antagonist.
S180 SB 206553 hydrochloride Potent 5-HT2B/5-HT2C serotonin receptor antagonist. Manufactured and sold under exclusive license from SmithKline Beecham Pharmaceuticals.
S8061 SB 242084 dihydrochloride Selective 5-HT2c serotonin receptor antagonist; crosses the blood-brain barrier. Manufactured and sold with the permission of SmithKline Beecham Pharmaceuticals.
V1889 VER-3323 hemifumarate salt 5-HT2C/5-HT2B serotonin receptor agonist.

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GABAergic


Product #  Product Name Notes Add to Cart
A2129 γ-Aminobutyric acid Major inhibitory neurotransmitter in brain; GABAA and GABAB receptor agonist; increases Cl- conductance.

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Stimulants


Product #  Product Name Notes Add to Cart
A5880 D-Amphetamine sulfate salt ((+)-α-Methyl-phenethylamine sulfate salt; Dextroamphetamine sulfate salt) Induces release of catecholamines and serotonin by displacing the monoamines from their vesicular storage sites; blocks catecholamine reuptake; more active isomer of amphetamine.
A1263 DL-Amphetamine sulfate salt ((±)-α-Methyl-phenethylamine sulfate salt) Induces release of catecholamines and serotonin by displacing the monoamines from their vesicular storage sites; blocks catecholamine reuptake. DEA Schedule II.
C222 Cathine hydrochloride (Pseudonorephedrine hydrochloride) from Khat shrub (Arabia, Ethiopia) Anorexic; with pharmacological effects similar to those of the amphetamines. DEA Schedule IV.
C3196 S(–)-Cathinone hydrochloride (α-Aminopropiophenone hydrochloride) Alkaloid that is the major central nervous system stimulant of the Khat shrub. Like amphetamine, it is a potent releaser of norepinephrine and dopamine from their intracellular stores. DEA Schedule I.
C8912 Cocaine free base (Ecgonine methyl ester benzoate) Inhibits the dopamine, norepinephrine, and serotonin transporters with KIs of approx. 300 nM, 900 nM, and 400 nM, respectively. Unlike amphetamines, it has no effect on catecholamine release. DEA Schedule II.
C5776 Cocaine hydrochloride Ecgonine methyl ester benzoate hydrochloride) Inhibits the dopamine, norepinephrine, and serotonin transporters with KIs of approx. 300 nM, 900 nM, and 400 nM, respectively. Unlike amphetamines, it has no effect on catecholamine release. DEA Schedule II.
E2750 (+)-Pseudoephedrine hydrochloride ((+)-ψ-Ephedrine hydrochloride; d-Isoephedrine hydrochloride) Non-selective adrenergic agonist; decongestant.
F8507 (±)-Fenfluramine hydrochloride Neurotoxic for prolonged administration or at high dosage; releases serotonin from axon terminals by a nonexocytotic mechanism; anorectic. DEA Schedule IV.
F112 (+)-Fenfluramine hydrochloride Neurotoxic on prolonged administration or at high dosage; releases serotonin from axon terminals by a nonexocytotic mechanism; anorectic. DEA Schedule IV.
H1392 Harmaline hydrochloride dihydrate CNS stimulant; may act through NMDA receptors.
H8646 Harmine CNS stimulant.
I7003 Ibogaine hydrochloride Alkaloid isolated from the African shrub, Tabernanthe iboga. CNS system stimulant; competitive inhibitor of serotonin and dopamine transport. DEA Schedule I.
M8750 (+)-Methamphetamine hydrochloride (d-N,α-Dimethylphenethylamine hydrochloride; d-Desoxyephedrine hydrochloride; Methylamphetamine hydrochloride) Sympathomimetic with more potent central effects than amphetamine. It is transported into terminals via the monoamine transporters and induces release of dopamine, norepinephrine, epinephrine, and serotonin. Serotonergic neurotoxin. DEA Schedule II.
M3404 (±)-p-Methoxyamphetamine hydrochloride (PMA hydrochloride) CNS stimulant and hallucinogen; more potent transport inhibitor and releaser of serotonin than of dopamine. DEA Schedule I.
M5037 2-(Methylamino)propiophenone hydrochloride (Methcathinone hydrochloride) Potent amphetamine-like stimulant; dimethylpropion metabolite. DEA Schedule I
M200 (±)-N-Methyl-1-(3,4-methylenedioxyphenyl)-2-butanamine hydrochloride (MBDB hydrochloride) Non-hallucinogenic; CNS stimulant; analog of MDMA. DEA Schedule I.
M2892 Methylphenidate hydrochloride (Ritalin hydrochloride) CNS stimulant; releases catecholamines; potent inhibitor of dopamine reuptake. DEA Schedule II.
M6810 D-threo-Methylphenidate hydrochloride CNS stimulant; more potent enantiomer of Methylphenidate. DEA Schedule II.
M6935 L-threo-Methylphenidate hydrochloride CNS stimulant; less potent enantiomer of Methylphenidate. DEA Schedule II.

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