• Multipurpose Commercial panoramic tote box irradiator
• Safety features in accordance with IAEA recommendations
• Wet storage
• Tote box system, tote box sizes:480×480x900 mm
• Max. 7 m³/h capacity with the above box
• 14 m³ of target material is irradiated at the same time
• Continuous and batch mode of operation
• Co-60 (1 MCi)

• Multipurpose Commercial panoramic pallet irradiator
• Safety features in accordance with IAEA recommendations
• Wet storage
• Tote box system for pallets of sizes 1280×1000x900 mm
• Max. 20 m³/h capacity with the above box
• 9 m³ of target material is irradiated at the same time
• Continuous and batch mode of operation
• Co-60 (1 MCi)

*Availability:

1    370 - 3700 MBq from stock

2    37 - 370 MBq from stock

3    please inquire

Tritium

Notes

Our company has been engaged in preparing isotope labelled agrochemicals (pesticides) and other compounds for over thirty years.

This list comprises the most frequently sold ¹⁴C-labelled compounds with the exception of the pesticides.

These products are available also in bulk quantities.

Custom synthesis

We are ready to undertake synthesis of other compounds not listed in our catalogues. We are prepared to provide with quotation following your request. When inquiring please indicate the following required specifications, too:

• correct chemical or common name of the compounds (in case of more complicated molecules together with the formula);
• labelling isotope and position of labelling;
• required molar or specific activity;
• required activity;
• required form (net material or a solution - in the latter case the requested solvent and radiochemical concentration; requested packsize);
• whether you are able to supply synthesis route and/or protocols, references of technical literature, raw material or standard (final product and/or intermediates) analytical method (in general HPLC). All information provided by the cusotmers are handled as confidental. NDA is concluded upon customer’s reuest. Providing these results in significant reduce in price.

As a result of many years practice in this field experts of the Institute are at your disposal in answering technical questions (Synthesis Business) and issuing quotations (Commercial Department).

Opioid peptides

Other receptor ligands

Producer:

Biological Research Center
Hungarian Academy of Sciences
Isotope Laboratory “B” level

H-6701 Szeged, P.O.B. 521
Phone: (36-62) 432-232
Fax: (36-62) 432-576

Notes

Our company has been engaged in preparing isotope labelled agrochemicals (pesticides) and other compounds for over thirty years.

This list comprises the most frequently sold ¹⁴C-labelled pesticides. These compounds are the most widely used representatives of the various classes in this field but obviously, inquiries for other pesticides are also welcome.

There are several common names of these compounds, which vary depending on the country where they are applied. We use the common names given by the British Standard Institution.

Molar activities are usually set to the customer’s request and often reach 1.85 GBq/mM (50 mCi/ mM). Being these chemicals sensitive they are synthesized as custom preparation products; consequently each offer is individually submitted taking the quantity, requested molar activity, date of delivery, etc. into account.

Isotope labelled pesticides are delivered in dry ice or at natural temperature depending on the sensitivity of the labelled compound, but recommended to be stored at – 20 °C or below; the cooler the better.

There are three groups of the listed pesticides:

1st group: we have the compound of required purity in stock;
2nd group: we have the material in stock but it has to be purified;
3rd group: we have no material in stock so it has to be synthesized again.

Depending upon the availability and our manufacturing capacity the minimum quantity to be sold and the date of delivery change from time to time. For your preliminary information:

1st group: delivery within 1 – 2 week;
2nd group: delivery within 2 -3 weeks;
3rd group: delivery within 4 – 10 weeks, minimum quantity is 37 MBq.

As the current situation is changing continuously information about the required material (i.e. which group it belongs to) will be given upon inquiry.

Custom synthesis

We are ready to undertake synthesis of other compounds not listed in our catalogues. We are prepared to give quotation following your request. When inquiring please indicate the following required specifications, too:

• correct chemical or common name of the compounds (in case of more complicated molecules together with the formula);
• labelling isotope and position of labelling;
• required molar or specific activity;
• required activity;
• required form (net material or a solution - in the latter case the requested solvent and radiochemical concentration; requested packsize);
• whether you are able to supply synthesis route and/or protocols, references of technical literature, raw material or standard (final product and/or intermediates) analytical method (in general HPLC). All information provided by the cusotmers are handled as confidental. NDA is concluded upon customer’s reuest. Providing these results in significant reduce in price.

As a result of many years practice in this field experts of the Institute are at your disposal in answering technical questions (Synthesis Business) and issuing quotations (Commercial Department).

Structural formula of nor-BNI:

Ref.: Kinouchi et al. Evidence for kappa 1 opioid receptor multiplicity in the guinea pig cerebellum. Eur. J. Pharmacol. 207, 135-141 (1991). Márki et al. Tritiated kappa receptor antagonist norbinaltorphimine: synthesis and in vitro binding in three different tissues. Life Sci. 66, 43-49 (2000).

Structural formula of naltrindole:

Ref.: Portoghese et al. Design of peptidomimetic d opioid receptor antagonists using the message-address concept. J. Med. Chem. 33, 1714-1720 (1990). Yamamura et al. Characterisation of [³H]naltrindole binding to delta opioid receptors in rat brain. Life Sci., 50, PL119-124 (1992).

Structural formula of naloxone:

Ref.: Lord et al. Endogenous opioid peptides: multiple agonists and receptors. Nature 267, 495-499 (1977). Sawynok et al. Minireview on the specificity of naloxone as an opiate antagonist. Life Sci. 25, 1621-1632 (1979). Tóth et al. Preparation of (7,8,18,19,20-3H)naloxone of high specific activity. J. Label. Compd. Radiopharm. 19, 1021-1030 (1982).

Structural formula of 14-Methoxymetopon:

Ref.: Schmidhammer et al. Synthesis and biological evaluation of 14-alkoxymorphinans. 8. 14-Methoxymetopon, an extremely potent opioid agonist. Helv. Chim. Acta 81, 1784-1787 (1990). Spetea et al. Binding characteristics of [3H]14-methoxymetopon, a high affinity m-opioid receptor agonist. Eur. J. Neurosci. 18, 290-295 (2003).

Structural formula of dihydromorphine:

Ref.: Tóth et al. Preparation of 1,7,8-3H-dihydromorphine of high molecular activity and its application in opiate receptor binding experiments. Radiochem. Radioanal. Lett. 56, 209-216 (1982). Maggi et al. Antiprogestins inhibit the binding of opioids to mu-opioid receptors in nervous membrane preparations. Eur. J. Pharmacol. 301, 169-177 (1996). Benyhe et al. Affinity labelling of frog brain opioid receptors by dynorphin(1-10) chloromethyl ketone. Neuropeptides 31, 52-59 (1997)

Structural formula of cyprodime:

Ref.: Ötvös et al. Tritium labelling of cyprodime (= (-)17-(cyclopropylmethyl)-4,14-dimethoxymorphinan-6-one), a m receptor selective opioid antagonist. Helv. Chim. Acta 75, 1718-1720 (1992). Márki et al. Mu-opioid receptor specific antagonist cyprodime: characterisation by in vitro radioligand and [35S]GTPg S binding assays. Eur. J. Pharmacol. 383, 209-214 (1999).

Structural formula of buprenorphine:

Ref.: Mello et al. Buprenorphin suppresses heroin use by heroin addicts. Science, 207, 657-659 (1980). Leander Buprenorphin has potent kappa opioid receptor antagonist activity. Neuropharmacology, 26, 1445-1447 (1987). Ötvös et al. Synthesis of high specific activity [15,16-3H2]buprenorphin. J. Label. Compd. Radiopharm. 36, 79-83 (1994).

Ref.: Knox et al. Characterization and localization of gonadotropin-releasing hormone receptors in the adult female sea lamprey, Petromyzon marinus. Endocrinology 134, 492-498 (1994). Lovas et al. Direct anticancer activity of gonadotropin-releasing hormone-III. J. Pept. Res. 52, 384-389 (1998).

Structural formula of L-dihydroalprenolol:

Ref.: Williams et al. Adipocyte beta-adrenergic receptors. Identification and subcellular localisation by (-)-[³H]dihydroalprenolol binding. J. Biol. Chem. 251, 3096-3104 (1976). Randall et al. Structure and biological activity of (-)-[³H]dihydroalprenolol, a radioligand for studies of beta-adrenergic receptors. J. Med. Chem. 20, 1090-1094 (1977).

Ref.: Visconti et al. TIPP[Y], a highly selective delta ligand. Neurosci. Lett. 181, 47-49 (1994). Nevin et al. Synthesis and binding characteristics of tritiated TIPP[Y], a highly specific and stable delta opioid antagonist. Life Sci. 56, PL225-230 (1995).

Ref.: Nevin et al. Synthesis and binding characteristics of the highly specific, tritiated delta opioid antagonist [³H]TIPP. Life Sci. 53, PL57-62 (1993).

Ref.: Schiller et al. Subtleties of structure-agonist versus antagonist relationship of opioid peptides and peptidomimetics. J. Recept. Signal Transduct. Res. 19, 573-588 (1999). Szatmári et al. Synthesis and binding characteristics of [³H] H-Tyr-Tic[CH₂-NH]Cha-Phe-OH, a highly specific and stable delta-opioid antagonist. Peptides 20, 1079 1083 (1999).

Ref.: Guerrini et al. Address and message sequences for the nociceptin receptor: a structure-activity study of nociceptin(1-13)-peptide amide. J. Med. Chem. 40, 1789-1793 (1997).

Ref.: Meunier et al. Isolation and structure of the endogenous agonist of opioid receptor-like ORL₁ receptor. Nature 377, 532-535 (1995). Benyhe et al. Nociceptin binding sites in frog (Rana esculenta) brain membranes. Biochem. Biophys. Res. Commun. 260, 592-596 (1999). Varany et al. Pharmacology of [Tyr¹]nociceptin analogs: receptor binding and bioassay studies. Naunyn Schmiedebergs Arch. Pharmacol. 360, 270-277 (1999).

Ref.: Garreau et al. VV-hemorphin-7 and LVV-hemorphin-7 released during in vitro peptic haemoglobin hydrolysis are morphinomimetic peptides. Neuropeptides 28, 243-250 (1995). Szikra et al. Receptor binding properties of a hemorphin analogue in rat brain membrane preparation. Neurobiology (Bp) 4, 279-280 (1996). Yatsika et al. LVV- and VV-hemorphins: comparative levels in rat tissues. FEBS Lett. 428, 286-290 (1998).

Ref.: Wollemann et al. Characterisation of [³H]Met-Enkephalin-Arg⁶-Phe⁷ Binding to Opioid Receptors in Frog Brain Membrane Preparations. J. Neurochem. 63, 1460-1465 (1994). Benyhe et al. Met⁵-enkephalin-Arg⁶-Phe⁷, an endogenous neuropeptide, binds to multiple opioid and nonopioid sites in rat brain. Neurochem. Res. 48, 249-458 (1997). Gupta et al. Chimeric peptide of Met-enkephalin and FMRFa induces antinociception and attenuates development of tolerance to morphine antinociception. Peptides 20, 471-478 (1999).

Ref.: Bozó et al. Receptor binding and G-protein activation by new Met⁵-enkephalin-Arg⁶-Phe⁷ derived peptides. Life Sci. 66, 1241-1251 (2000).

Ref.: Hughes et al. Identification of two related pentapeptides from the brain with potent opiate agonist activity. Nature 258, 577-580 (1975). Rinne et al. Brain methionine- and leucine-enkephalin receptors in patients with dementia. Neurosci. Lett. 161, 77-80 (1993).

Ref.: Benyhe et al. Characterisation of rat brain opioid receptors by [Tyr¹-3,5-³H] d-Ala²-, Leu⁵-enkephalin binding. Neurochem. Res. 10, 627-635 (1985).

Ref.: Hughes et al. Identification of two related pentapeptides from the brain with potent opiate agonist activity. Nature 258, 577-580 (1975). Okhuto et al. Human nasal mucosal neutral enopeptidase (NEP): location, quantitation, and secretion. Am. J. Respir. Cell Mol. Biol. 9, 557-567 (1993). Rinne et al. Brain methionine- and leucine-enkephalin receptors in patients with dementia. Neurosci. Lett. 161, 77-80 (1993).

Ref.: Okada et al. Structural studies of [2 , 6 -dimethyl-l-tyrosine1]endomorphin-2 analogues: enhanced activity and cis orientation of the Dmt-Pro amide bond. Bioorg. Med. Chem. 11, 1983-1994 (2003). Tóth et al. New endomorphin analogs with m-agonist and d-antagonist properties. Pure Appl. Chem. 76, 951-957 (2004).

Ref.: Zadina et al. A potent and selective endogenous agonist for the mu-opiate receptor. Nature 386, 499-502 (1997).

Ref.: Zadina et al. A potent and selective endogenous agonist for the mu-opiate receptor. Nature 386, 499-502 (1997).

Ref.: Zadina et al. A potent and selective endogenous agonist for the mu-opiate receptor. Nature 386, 499-502 (1997). Tömböly et al. Synthesis of tritium labelled endomorphin 2 and its stability in the radioreceptor assay. Czech. J. Phys. 49/S1, 893-896 (1999). Monory et al. Specific activation of the m opioid receptor (MOR) by endomorphin 1 and endomorphin 2. Eur. J. Neurosci. 12, 577-584 (2000).

Ref.: Zadina et al. A potent and selective endogenous agonist for the mu-opiate receptor. Nature 386, 499-502 (1997). Hackler et al. Isolation of relatively large amounts of endomorphin-1 and endomorphin-2 from human brain cortex. Peptides 18, 1635-1639 (1997).

Ref.: Lung et al. Effect of modification of residues in position 3 of dynorphin A (1-11)-NH₂ on kappa receptor selectivity and potency. J. Med. Chem. 39, 2456-2460 (1996).

Ref.: Goldstein et al. Porcine pituitary dynorphin: complete amino acid sequence of the biologically active heptadecapeptide. Proc. Natl. Acad. Sci. 78, 7219-7223 (1981). Yarygin et al. Non-opioid dynorphin binding sites on secretory vesicles of a pituitary-derived cell line. Brain Res. 791, 99-107 (1998).

Structural formula of N,N(Me)2-Dmt-Tic-OH:

Ref.: Salvadori et al. Evolution of the Dmt-Tic pharmacophore: N-terminal methylated derivatives with extraordinary delta opioid antagonist activity. J. Med. Chem. 40, 3100-3108 (1997). Kertész et al. Synthesis of 2 ,6 -Dymethyltyrosine Containing Tritiated Delta Opioid-Receptor Selective Antagonist Dipeptide Ligands with Extraordinary Affinity. J. Label. Compd. Radiopharm. 41, 1083-1091 (1998). Salvadori et al. Further studies on the Dmt-Tic pharmacophore: hydrophobic substituents at the C-terminus endow delta antagonists to manifest mu agonism or mu antagonism. J. Med. Chem. 42, 5010-5019 (1999).

Ref.: Sagan et al. Differential contribution of C-terminal regions of dermorphin and dermenkephalin to opioid-sites selection and binding potency. Biochem. Biophys. Res. Commun. 163, 726-732 (1989). Carr et al. Mu and delta opioid receptor regulation of pro-opiomelanocortin peptide secretion from the rat neurointermediate pituitary in vitro. Neuropeptides 34, 69-75 (2000).

Ref.: Tóth et al. Conformationally constrained deltorphin analogs with 2-aminotetralin-2-carboxylic acid in position 3. J. Med. Chem. 40, 990-995 (1997). Kelly et al. Weaning-induced development of delta opioid receptors in rat brain: differential effects of guanine nucleotides and sodium upon ligand-receptor recognition. Br. J. Pharmacol. 125, 979-986 (1998).

Ref.: Nevin et al. Binding characteristics of the novel highly selective delta agonist, [³H]Ile^5,6deltorphin II. Neuropeptides, 26, 261-265 (1994).

Ref.: Búzás et al.: Synthesis and binding characteristic of the highly delta-specific new tritiated opioid peptide, [³H]deltorphin II. Life Sci. 50, PL75-78 (1992).

Ref.: Tóth et al. Conformationally constrained deltorphin analogs with 2-aminotetralin-2-carboxylic acid in position 3. J. Med. Chem. 40, 990-995 (1997). Kelly et al. Weaning-induced development of delta opioid receptors in rat brain: differential effects of guanine nucleotides and sodium upon ligand-receptor recognition. Br. J. Pharmacol. 125, 979-986 (1998).

Ref.: Kocsis L. et al. Nociceptin antagonism: probing the receptor by N-acetyl oligopeptides Regul. Pept.122.199-207 (2004) Gunduz O.et al. In vitro binding and functional studies of AcRYYRIK-ol and its derivatives, novel partial agonists of the nociceptin F/Q receptor Neurosignals 15. 91-101 (2006-2007)

References: Tóth et al. New endomorphin analogs with m-agonist and d-antagonist properties. Pure Appl. Chem. 76, 951-957 (2004). Keresztes A. et al: New endomorphin analogues containing alicyclic beta amino acids: Influence on bioactive conformation and pharmacological profile J.Med.Chem 51, 4270-4279 (2008)

References: Keresztes A.et al.: Synthesis, radiolabelling and receptor binding of [³H] [(1S,2R) Acpc²] endomorphin-2 Peptides 27 (2006) 3315-3321, Keresztes A. et al: New endomorphin analogues containing alicyclic beta amino acids: Influence on bioactive conformation and pharmacological profile J.Med.Chem 51, 4270-4279 (2008)

Ref.: Schiller et al. Synthesis and in vitro opioid activity profiles of DALDA analogues. Eur. J. Med. Chem. 35, 895-901 (2000). Zhao et al. Profound spinal tolerance after repeated exposure to a highly selective mu-opioid peptide agonist: role of delta-opioid receptors. J. Pharmacol. Exp. Ther. 302, 188-196 (2002). Zhao et al. Comparison of [Dmt1]DALDA and DAMGO in binding and G protein activation at mu, delta and kappa opioid receptors. J. Pharmacol. Exp. Ther. 307, 947-954 (2003).