Differential identification and localization of adenylyl cyclase and glucose transporter in brain using iodinated derivatives of forskolin

Joan D. Robbins; Nathan M. Appel; Antonio Laurenza; Ian A. Simpson; Errol B. De Souza; Kenneth B. Seamon

doi:10.1016/0006-8993(92)90354-C

Differential identification and localization of adenylyl cyclase and glucose transporter in brain using iodinated derivatives of forskolin

Joan D. Robbins, Nathan M. Appel, Antonio Laurenza, Ian A. Simpson, Errol B. De Souza, Kenneth B. Seamon

Research output: Contribution to journal › Article › peer-review

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Abstract

Two radioiodinated derivatives of forskolin, [¹²⁵I]6-IHPP-Fsk and [¹²⁵I]7-IHPP-Fsk, were synthesized as specific ligands for adenylyl cyclase and glucose transporter, respectively. [¹²⁵I]6-IHPP-Fsk bound to bovine brain homogenates with a K_d of 9 nM and binding was inhibited by forskolin but not 1,9-dideoxyforskolin, cytochalasin B, or d-glucose. [¹²⁵I]7-IHPP-Fsk bound to bovine brain homogenates at two classes of binding sites with K_d's of 56 nM and 4.7 μM; cytochalasin B and d-glucose inhibited 75% of the high affinity binding while having no effect on the low affinity binding. [¹²⁵I]6-IHPP-Fsk and [¹²⁵I]7-IHPP-Fsk were used to localize adenylyl cyclase and glucose transporter in rat brain by receptor autoradiography. The pattern of binding obtained with [¹²⁵I]6-IHPP-Fsk was similar to that observed using [³H]forskolin to detect adenylyl cyclase. In contrast, the pattern of binding obtained with [¹²⁵I]7-IHPP-Fsk was similar to that observed by others using [³H]cytochalasin B to detect glucose transporter. These iodinated ligands are selective for adenylyl cyclase and glucose transporter and require significantly shorter exposure times to yield autoradiographs than tritiated ligands.

Original language	English (US)
Pages (from-to)	148-152
Number of pages	5
Journal	Brain research
Volume	581
Issue number	1
DOIs	https://doi.org/10.1016/0006-8993(92)90354-C
State	Published - May 22 1992

All Science Journal Classification (ASJC) codes

General Neuroscience
Molecular Biology
Clinical Neurology
Developmental Biology

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10.1016/0006-8993(92)90354-C

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@article{fb1bb5c200384e69a73f05a979e7819e,

title = "Differential identification and localization of adenylyl cyclase and glucose transporter in brain using iodinated derivatives of forskolin",

abstract = "Two radioiodinated derivatives of forskolin, [125I]6-IHPP-Fsk and [125I]7-IHPP-Fsk, were synthesized as specific ligands for adenylyl cyclase and glucose transporter, respectively. [125I]6-IHPP-Fsk bound to bovine brain homogenates with a Kd of 9 nM and binding was inhibited by forskolin but not 1,9-dideoxyforskolin, cytochalasin B, or d-glucose. [125I]7-IHPP-Fsk bound to bovine brain homogenates at two classes of binding sites with Kd's of 56 nM and 4.7 μM; cytochalasin B and d-glucose inhibited 75% of the high affinity binding while having no effect on the low affinity binding. [125I]6-IHPP-Fsk and [125I]7-IHPP-Fsk were used to localize adenylyl cyclase and glucose transporter in rat brain by receptor autoradiography. The pattern of binding obtained with [125I]6-IHPP-Fsk was similar to that observed using [3H]forskolin to detect adenylyl cyclase. In contrast, the pattern of binding obtained with [125I]7-IHPP-Fsk was similar to that observed by others using [3H]cytochalasin B to detect glucose transporter. These iodinated ligands are selective for adenylyl cyclase and glucose transporter and require significantly shorter exposure times to yield autoradiographs than tritiated ligands.",

author = "Robbins, {Joan D.} and Appel, {Nathan M.} and Antonio Laurenza and Simpson, {Ian A.} and {De Souza}, {Errol B.} and Seamon, {Kenneth B.}",

note = "Funding Information: {"}Molecular Pharmacology Laboratory, Center for Biologics Evaluation and Research, Food and Drug Administration, Bethesda MD 20892 (USA), boffice of Research Resources, Center for Drug Evaluation and Research, Food and Drug Administration, Rockville MD 20857 (USA), CExperimental Diabetes, Metabolism and Nutrition Section, National Institutes of Diabetes, Digestive diseases, and Kidney, National Institutes of Health, Bethesda MD 20892 (USA) and aCentral Nervous System Diseases Research, The DuPont Merck Pharmaceutical Corporation, Wilmington DE 19880-0400 (USA)",

year = "1992",

month = may,

day = "22",

doi = "10.1016/0006-8993(92)90354-C",

language = "English (US)",

volume = "581",

pages = "148--152",

journal = "Brain research",

issn = "0006-8993",

publisher = "Elsevier B.V.",

number = "1",

}

TY - JOUR

T1 - Differential identification and localization of adenylyl cyclase and glucose transporter in brain using iodinated derivatives of forskolin

AU - Robbins, Joan D.

AU - Appel, Nathan M.

AU - Laurenza, Antonio

AU - Simpson, Ian A.

AU - De Souza, Errol B.

AU - Seamon, Kenneth B.

N1 - Funding Information: "Molecular Pharmacology Laboratory, Center for Biologics Evaluation and Research, Food and Drug Administration, Bethesda MD 20892 (USA), boffice of Research Resources, Center for Drug Evaluation and Research, Food and Drug Administration, Rockville MD 20857 (USA), CExperimental Diabetes, Metabolism and Nutrition Section, National Institutes of Diabetes, Digestive diseases, and Kidney, National Institutes of Health, Bethesda MD 20892 (USA) and aCentral Nervous System Diseases Research, The DuPont Merck Pharmaceutical Corporation, Wilmington DE 19880-0400 (USA)

PY - 1992/5/22

Y1 - 1992/5/22

N2 - Two radioiodinated derivatives of forskolin, [125I]6-IHPP-Fsk and [125I]7-IHPP-Fsk, were synthesized as specific ligands for adenylyl cyclase and glucose transporter, respectively. [125I]6-IHPP-Fsk bound to bovine brain homogenates with a Kd of 9 nM and binding was inhibited by forskolin but not 1,9-dideoxyforskolin, cytochalasin B, or d-glucose. [125I]7-IHPP-Fsk bound to bovine brain homogenates at two classes of binding sites with Kd's of 56 nM and 4.7 μM; cytochalasin B and d-glucose inhibited 75% of the high affinity binding while having no effect on the low affinity binding. [125I]6-IHPP-Fsk and [125I]7-IHPP-Fsk were used to localize adenylyl cyclase and glucose transporter in rat brain by receptor autoradiography. The pattern of binding obtained with [125I]6-IHPP-Fsk was similar to that observed using [3H]forskolin to detect adenylyl cyclase. In contrast, the pattern of binding obtained with [125I]7-IHPP-Fsk was similar to that observed by others using [3H]cytochalasin B to detect glucose transporter. These iodinated ligands are selective for adenylyl cyclase and glucose transporter and require significantly shorter exposure times to yield autoradiographs than tritiated ligands.

AB - Two radioiodinated derivatives of forskolin, [125I]6-IHPP-Fsk and [125I]7-IHPP-Fsk, were synthesized as specific ligands for adenylyl cyclase and glucose transporter, respectively. [125I]6-IHPP-Fsk bound to bovine brain homogenates with a Kd of 9 nM and binding was inhibited by forskolin but not 1,9-dideoxyforskolin, cytochalasin B, or d-glucose. [125I]7-IHPP-Fsk bound to bovine brain homogenates at two classes of binding sites with Kd's of 56 nM and 4.7 μM; cytochalasin B and d-glucose inhibited 75% of the high affinity binding while having no effect on the low affinity binding. [125I]6-IHPP-Fsk and [125I]7-IHPP-Fsk were used to localize adenylyl cyclase and glucose transporter in rat brain by receptor autoradiography. The pattern of binding obtained with [125I]6-IHPP-Fsk was similar to that observed using [3H]forskolin to detect adenylyl cyclase. In contrast, the pattern of binding obtained with [125I]7-IHPP-Fsk was similar to that observed by others using [3H]cytochalasin B to detect glucose transporter. These iodinated ligands are selective for adenylyl cyclase and glucose transporter and require significantly shorter exposure times to yield autoradiographs than tritiated ligands.

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U2 - 10.1016/0006-8993(92)90354-C

DO - 10.1016/0006-8993(92)90354-C

M3 - Article

C2 - 1498664

AN - SCOPUS:0026747849

SN - 0006-8993

VL - 581

SP - 148

EP - 152

JO - Brain research

JF - Brain research

IS - 1

ER -

Differential identification and localization of adenylyl cyclase and glucose transporter in brain using iodinated derivatives of forskolin

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